Scholars@Duke
Michael Rod Zalutsky

Michael Rod Zalutsky

Jonathan Spicehandler, M.D. Distinguished Professor of Neuro Oncology, in the School of Medicine
Radiology
zalut001@mc.duke.edu
Box 3808 Med Ctr, Durham, NC
311 Research Drive, 161H Bryan Res Bldg, Durham, NC 27710
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Selected Publications

A third generation PSMA-targeted agent [211At]YF2: Synthesis and in vivo evaluation.

Journal Article Nucl Med Biol · 2024 INTRODUCTION: Targeted α-particle therapy agents have shown promising responses in patients who have developed resistance to β--particle emitting radionuclides, albeit off-target toxicity remains a concern. Astatine-211 emits only one α-particle per decay ... Full text Link to item Cite

PSMA-reactive NB7 single domain antibody fragment: A potential scaffold for developing prostate cancer theranostics.

Journal Article Nucl Med Biol · 2024 INTRODUCTION: Single domain antibody fragments (sdAbs) are an appealing scaffold for radiopharmaceutical development due to their small size (~15 kDa), high solubility, high stability, and excellent tumor penetration. Previously, we developed NB7 sdAb, whi ... Full text Link to item Cite

DNA Repair Inhibitors: Potential Targets and Partners for Targeted Radionuclide Therapy.

Journal Article Pharmaceutics · July 11, 2023 The present review aims to explore the potential targets/partners for future targeted radionuclide therapy (TRT) strategies, wherein cancer cells often are not killed effectively, despite receiving a high average tumor radiation dose. Here, we shall discus ... Full text Link to item Cite

Effective Treatment of Human Breast Carcinoma Xenografts with Single-Dose 211At-Labeled Anti-HER2 Single-Domain Antibody Fragment.

Journal Article J Nucl Med · January 2023 Single-domain antibody fragments (sdAbs) are attractive for targeted α-particle therapy, particularly with 211At, because of their rapid accumulation in tumor and clearance from normal tissues. Here, we evaluate the therapeutic potential of this strategy w ... Full text Link to item Cite

The Radiopharmaceutical Chemistry of the Halogen Radionuclides

Chapter · January 1, 2023 Radiohalogens are far fewer in number than radiometals, yet they have been important in radiopharmaceutical therapy since the very beginning. Indeed, radionuclides of the three heaviest naturally occurring halogens-bromine, iodine, and astatine-provide rad ... Full text Cite

Small Molecules as Vectors for Radiopharmaceutical Therapy

Chapter · January 1, 2023 Radiopharmaceutical therapy (RPT) with small molecule-based agents is already a standard-of-care in multiple clinical scenarios, including patients with metastatic, castration-resistant prostate cancer whose tumors express prostate-specific membrane antige ... Full text Cite

Site-Specific Radiohalogenation of a HER2-Targeted Single-Domain Antibody Fragment Using a Novel Residualizing Prosthetic Agent.

Journal Article J Med Chem · November 24, 2022 Because of their rapid tumor accumulation and normal tissue clearance, single-domain antibody fragments (sdAbs) are an attractive vehicle for developing radiotherapeutics labeled with the α-emitter 211At. Herein, we have evaluated iso-[211At]AGMB-PODS, a p ... Full text Link to item Cite

Brachytherapy via a depot of biopolymer-bound 131I synergizes with nanoparticle paclitaxel in therapy-resistant pancreatic tumours.

Journal Article Nat Biomed Eng · October 2022 Locally advanced pancreatic tumours are highly resistant to conventional radiochemotherapy. Here we show that such resistance can be surmounted by an injectable depot of thermally responsive elastin-like polypeptide (ELP) conjugated with iodine-131 radionu ... Full text Open Access Link to item Cite

Stapled peptides as scaffolds for developing radiotracers for intracellular targets: Preliminary evaluation of a radioiodinated MDM2-binding stapled peptide in the SJSA-1 osteosarcoma model.

Journal Article Bioorg Med Chem Lett · June 15, 2022 Stapled peptides are promising scaffolds for inhibiting protein-protein interactions in cells, including between the intracellular oncoprotein MDM2 and p53. Herein, we have investigated the potential utility of a stapled peptide, VIP116, for developing rad ... Full text Open Access Link to item Cite

Evaluation of an 131I-labeled HER2-specific single domain antibody fragment for the radiopharmaceutical therapy of HER2-expressing cancers.

Journal Article Sci Rep · February 22, 2022 Radiopharmaceutical therapy (RPT) is an attractive strategy for treatment of disseminated cancers including those overexpressing the HER2 receptor including breast, ovarian and gastroesophageal carcinomas. Single-domain antibody fragments (sdAbs) exemplifi ... Full text Link to item Cite

An Improved 211At-Labeled Agent for PSMA-Targeted α-Therapy.

Journal Article J Nucl Med · February 2022 α-Particle emitters targeting the prostate-specific membrane antigen (PSMA) proved effective in treating patients with prostate cancer who were unresponsive to the corresponding β-particle therapy. 211At is an α-emitter that may engender less toxicity than ... Full text Link to item Cite

Low-level whole-brain radiation enhances theranostic potential of single-domain antibody fragments for human epidermal growth factor receptor type 2 (HER2)-positive brain metastases.

Journal Article Neurooncol Adv · 2022 BACKGROUND: Single-domain antibody fragments (aka VHH, ~ 13 kDa) are promising delivery systems for brain tumor theranostics; however, achieving efficient delivery of VHH to intracranial lesions remains challenging due to the tumor-brain barrier. Here, we ... Full text Open Access Link to item Cite

Site-Specific and Residualizing Linker for 18F Labeling with Enhanced Renal Clearance: Application to an Anti-HER2 Single-Domain Antibody Fragment.

Journal Article J Nucl Med · November 2021 Single-domain antibody fragments (sdAbs) are promising vectors for immuno-PET; however, better methods for labeling sdAbs with 18F are needed. Herein, we evaluate a site-specific strategy using an 18F residualizing motif and the anti-epidermal growth facto ... Full text Link to item Cite

Fluorine-18 Labeling of the MDM2 Inhibitor RG7388 for PET Imaging: Chemistry and Preliminary Evaluation.

Journal Article Mol Pharm · October 4, 2021 RG7388 (Idasanutlin) is a potent inhibitor of oncoprotein murine double minute 2 (MDM2). Herein we investigated the feasibility of developing 18F-labeled RG7388 as a radiotracer for imaging MDM2 expression in tumors with positron emission tomography (PET). ... Full text Open Access Link to item Cite

Feasibility of Developing Radiotracers for MDM2: Synthesis and Preliminary Evaluation of an 18F-Labeled Analogue of the MDM2 Inhibitor SP-141.

Journal Article Pharmaceuticals (Basel) · April 13, 2021 Murine double minute 2 (MDM2), a negative regulator of the p53 tumor suppressor protein, is overexpressed in several human cancers. Herein we investigate the feasibility of developing 18F-labeled compounds based on the small molecule inhibitor SP-141 for i ... Full text Link to item Cite

Site-specific radioiodination of an anti-HER2 single domain antibody fragment with a residualizing prosthetic agent.

Journal Article Nucl Med Biol · January 2021 INTRODUCTION: As a consequence of their small size, high stability and high affinity, single domain antibody fragments (sdAbs) are appealing targeting vectors for radiopharmaceutical development. With sdAbs binding to internalizing receptors like HER2, res ... Full text Link to item Cite

Synthesis and preliminary evaluation of 211At-labeled inhibitors of prostate-specific membrane antigen for targeted alpha particle therapy of prostate cancer.

Journal Article Nucl Med Biol · 2021 INTRODUCTION: The high potency and short tissue range of α-particles are attractive features for targeted radionuclide therapy, particularly for cancers with micro-metastases. In the current study, we describe the synthesis of a series of 211At-labeled pro ... Full text Link to item Cite

Labeling single domain antibody fragments with 18F using a novel residualizing prosthetic agent - N-succinimidyl 3-(1-(2-(2-(2-(2-[18F]fluoroethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)-5-(guanidinomethyl)benzoate.

Journal Article Nucl Med Biol · 2021 INTRODUCTION: Labeling single domain antibody fragments (sdAbs) with 18F is an attractive strategy for immunoPET. Earlier, we developed a residualizing label, N-succinimidyl 3-((4-(4-fluorobutyl)-1H-1,2,3-triazol-1-yl)methyl)-5-(guanidinomethyl)benzoate ([ ... Full text Link to item Cite

Production, purification and availability of 211At: Near term steps towards global access.

Journal Article Nucl Med Biol · 2021 The promising characteristics of the 7.2-h radiohalogen 211At have long been recognized; including having chemical properties suitable for labeling targeting vectors ranging from small organic molecules to proteins, and the emission of only one α-particle ... Full text Link to item Cite

Gold Nanostars: A Novel Platform for Developing 211At-Labeled Agents for Targeted Alpha-Particle Therapy.

Journal Article Int J Nanomedicine · 2021 AIM: To develop an innovative 211At nanoplatform with high radiolabeling efficiency and low in vivo deastatination for future targeted alpha-particle therapy (TAT) to treat cancer. METHODS: Star-shaped gold nanoparticles, gold nanostars (GNS), were used as ... Full text Link to item Cite

A third generation PSMA-targeted agent [211At]YF2: Synthesis and in vivo evaluation.

Journal Article Nucl Med Biol · 2024 INTRODUCTION: Targeted α-particle therapy agents have shown promising responses in patients who have developed resistance to β--particle emitting radionuclides, albeit off-target toxicity remains a concern. Astatine-211 emits only one α-particle per decay ... Full text Link to item Cite

PSMA-reactive NB7 single domain antibody fragment: A potential scaffold for developing prostate cancer theranostics.

Journal Article Nucl Med Biol · 2024 INTRODUCTION: Single domain antibody fragments (sdAbs) are an appealing scaffold for radiopharmaceutical development due to their small size (~15 kDa), high solubility, high stability, and excellent tumor penetration. Previously, we developed NB7 sdAb, whi ... Full text Link to item Cite

DNA Repair Inhibitors: Potential Targets and Partners for Targeted Radionuclide Therapy.

Journal Article Pharmaceutics · July 11, 2023 The present review aims to explore the potential targets/partners for future targeted radionuclide therapy (TRT) strategies, wherein cancer cells often are not killed effectively, despite receiving a high average tumor radiation dose. Here, we shall discus ... Full text Link to item Cite

Effective Treatment of Human Breast Carcinoma Xenografts with Single-Dose 211At-Labeled Anti-HER2 Single-Domain Antibody Fragment.

Journal Article J Nucl Med · January 2023 Single-domain antibody fragments (sdAbs) are attractive for targeted α-particle therapy, particularly with 211At, because of their rapid accumulation in tumor and clearance from normal tissues. Here, we evaluate the therapeutic potential of this strategy w ... Full text Link to item Cite

The Radiopharmaceutical Chemistry of the Halogen Radionuclides

Chapter · January 1, 2023 Radiohalogens are far fewer in number than radiometals, yet they have been important in radiopharmaceutical therapy since the very beginning. Indeed, radionuclides of the three heaviest naturally occurring halogens-bromine, iodine, and astatine-provide rad ... Full text Cite

Small Molecules as Vectors for Radiopharmaceutical Therapy

Chapter · January 1, 2023 Radiopharmaceutical therapy (RPT) with small molecule-based agents is already a standard-of-care in multiple clinical scenarios, including patients with metastatic, castration-resistant prostate cancer whose tumors express prostate-specific membrane antige ... Full text Cite

Site-Specific Radiohalogenation of a HER2-Targeted Single-Domain Antibody Fragment Using a Novel Residualizing Prosthetic Agent.

Journal Article J Med Chem · November 24, 2022 Because of their rapid tumor accumulation and normal tissue clearance, single-domain antibody fragments (sdAbs) are an attractive vehicle for developing radiotherapeutics labeled with the α-emitter 211At. Herein, we have evaluated iso-[211At]AGMB-PODS, a p ... Full text Link to item Cite

Brachytherapy via a depot of biopolymer-bound 131I synergizes with nanoparticle paclitaxel in therapy-resistant pancreatic tumours.

Journal Article Nat Biomed Eng · October 2022 Locally advanced pancreatic tumours are highly resistant to conventional radiochemotherapy. Here we show that such resistance can be surmounted by an injectable depot of thermally responsive elastin-like polypeptide (ELP) conjugated with iodine-131 radionu ... Full text Open Access Link to item Cite

Stapled peptides as scaffolds for developing radiotracers for intracellular targets: Preliminary evaluation of a radioiodinated MDM2-binding stapled peptide in the SJSA-1 osteosarcoma model.

Journal Article Bioorg Med Chem Lett · June 15, 2022 Stapled peptides are promising scaffolds for inhibiting protein-protein interactions in cells, including between the intracellular oncoprotein MDM2 and p53. Herein, we have investigated the potential utility of a stapled peptide, VIP116, for developing rad ... Full text Open Access Link to item Cite

Evaluation of an 131I-labeled HER2-specific single domain antibody fragment for the radiopharmaceutical therapy of HER2-expressing cancers.

Journal Article Sci Rep · February 22, 2022 Radiopharmaceutical therapy (RPT) is an attractive strategy for treatment of disseminated cancers including those overexpressing the HER2 receptor including breast, ovarian and gastroesophageal carcinomas. Single-domain antibody fragments (sdAbs) exemplifi ... Full text Link to item Cite

An Improved 211At-Labeled Agent for PSMA-Targeted α-Therapy.

Journal Article J Nucl Med · February 2022 α-Particle emitters targeting the prostate-specific membrane antigen (PSMA) proved effective in treating patients with prostate cancer who were unresponsive to the corresponding β-particle therapy. 211At is an α-emitter that may engender less toxicity than ... Full text Link to item Cite

Low-level whole-brain radiation enhances theranostic potential of single-domain antibody fragments for human epidermal growth factor receptor type 2 (HER2)-positive brain metastases.

Journal Article Neurooncol Adv · 2022 BACKGROUND: Single-domain antibody fragments (aka VHH, ~ 13 kDa) are promising delivery systems for brain tumor theranostics; however, achieving efficient delivery of VHH to intracranial lesions remains challenging due to the tumor-brain barrier. Here, we ... Full text Open Access Link to item Cite

Site-Specific and Residualizing Linker for 18F Labeling with Enhanced Renal Clearance: Application to an Anti-HER2 Single-Domain Antibody Fragment.

Journal Article J Nucl Med · November 2021 Single-domain antibody fragments (sdAbs) are promising vectors for immuno-PET; however, better methods for labeling sdAbs with 18F are needed. Herein, we evaluate a site-specific strategy using an 18F residualizing motif and the anti-epidermal growth facto ... Full text Link to item Cite

Fluorine-18 Labeling of the MDM2 Inhibitor RG7388 for PET Imaging: Chemistry and Preliminary Evaluation.

Journal Article Mol Pharm · October 4, 2021 RG7388 (Idasanutlin) is a potent inhibitor of oncoprotein murine double minute 2 (MDM2). Herein we investigated the feasibility of developing 18F-labeled RG7388 as a radiotracer for imaging MDM2 expression in tumors with positron emission tomography (PET). ... Full text Open Access Link to item Cite

Feasibility of Developing Radiotracers for MDM2: Synthesis and Preliminary Evaluation of an 18F-Labeled Analogue of the MDM2 Inhibitor SP-141.

Journal Article Pharmaceuticals (Basel) · April 13, 2021 Murine double minute 2 (MDM2), a negative regulator of the p53 tumor suppressor protein, is overexpressed in several human cancers. Herein we investigate the feasibility of developing 18F-labeled compounds based on the small molecule inhibitor SP-141 for i ... Full text Link to item Cite

Site-specific radioiodination of an anti-HER2 single domain antibody fragment with a residualizing prosthetic agent.

Journal Article Nucl Med Biol · January 2021 INTRODUCTION: As a consequence of their small size, high stability and high affinity, single domain antibody fragments (sdAbs) are appealing targeting vectors for radiopharmaceutical development. With sdAbs binding to internalizing receptors like HER2, res ... Full text Link to item Cite

Synthesis and preliminary evaluation of 211At-labeled inhibitors of prostate-specific membrane antigen for targeted alpha particle therapy of prostate cancer.

Journal Article Nucl Med Biol · 2021 INTRODUCTION: The high potency and short tissue range of α-particles are attractive features for targeted radionuclide therapy, particularly for cancers with micro-metastases. In the current study, we describe the synthesis of a series of 211At-labeled pro ... Full text Link to item Cite

Labeling single domain antibody fragments with 18F using a novel residualizing prosthetic agent - N-succinimidyl 3-(1-(2-(2-(2-(2-[18F]fluoroethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)-5-(guanidinomethyl)benzoate.

Journal Article Nucl Med Biol · 2021 INTRODUCTION: Labeling single domain antibody fragments (sdAbs) with 18F is an attractive strategy for immunoPET. Earlier, we developed a residualizing label, N-succinimidyl 3-((4-(4-fluorobutyl)-1H-1,2,3-triazol-1-yl)methyl)-5-(guanidinomethyl)benzoate ([ ... Full text Link to item Cite

Production, purification and availability of 211At: Near term steps towards global access.

Journal Article Nucl Med Biol · 2021 The promising characteristics of the 7.2-h radiohalogen 211At have long been recognized; including having chemical properties suitable for labeling targeting vectors ranging from small organic molecules to proteins, and the emission of only one α-particle ... Full text Link to item Cite

Gold Nanostars: A Novel Platform for Developing 211At-Labeled Agents for Targeted Alpha-Particle Therapy.

Journal Article Int J Nanomedicine · 2021 AIM: To develop an innovative 211At nanoplatform with high radiolabeling efficiency and low in vivo deastatination for future targeted alpha-particle therapy (TAT) to treat cancer. METHODS: Star-shaped gold nanoparticles, gold nanostars (GNS), were used as ... Full text Link to item Cite

Heterogeneity and vascular permeability of breast cancer brain metastases.

Journal Article Cancer Lett · October 1, 2020 Improvements in the diagnosis and treatment of systemic breast cancer have led to a prolongation in patient survival. Unfortunately, these advances are also associated with an increased incidence of brain metastases (BM), with the result that many patients ... Full text Link to item Cite

Labeling Monoclonal Antibody with α-emitting 211At at High Activity Levels via a Tin Precursor.

Journal Article Cancer Biother Radiopharm · September 2020 Background: In a previous clinical study, the authors evaluated the potential of antitenascin C monoclonal antibody (mAb) 81C6 labeled with 211At via the prosthetic agent N-succinimidyl 3-[211At]astatobenzoate (SAB) for the treatment of primary brain tumor ... Full text Link to item Cite

Labeling a TCO-functionalized single domain antibody fragment with 18F via inverse electron demand Diels Alder cycloaddition using a fluoronicotinyl moiety-bearing tetrazine derivative.

Journal Article Bioorg Med Chem · September 1, 2020 Single domain antibody fragments (sdAbs) exhibit a rapid tumor uptake and fast blood clearance amenable for labeling with 18F (t½ = 110 min) but suffer from high kidney accumulation. Previously, we developed a method for 18F-labeling of sdAbs via trans-cyc ... Full text Link to item Cite

Delivery systems exploiting natural cell transport processes of macromolecules for intracellular targeting of Auger electron emitters.

Journal Article Nucl Med Biol · 2020 The presence of Auger electrons (AE) among the decay products of a number of radionuclides makes these radionuclides an attractive means for treating cancer because these short-range electrons can cause significant damage in the immediate vicinity of the d ... Full text Link to item Cite

Poly(ADP-Ribose)Polymerase (PARP) Inhibitors and Radiation Therapy.

Journal Article Front Pharmacol · 2020 Poly(ADP-ribose)polymerase-1 (PARP1) is a DNA repair enzyme highly expressed in the nuclei of mammalian cells, with a structure and function that have attracted interest since its discovery. PARP inhibitors, moreover, can be used to induce synthetic lethal ... Full text Link to item Cite

Observations on the Effects of Residualization and Dehalogenation on the Utility of N-Succinimidyl Ester Acylation Agents for Radioiodination of the Internalizing Antibody Trastuzumab.

Journal Article Molecules · October 30, 2019 Trastuzumab is an antibody used for the treatment of human epidermal growth factor receptor 2 (HER2)-overexpressing breast cancers. Since trastuzumab is an internalizing antibody, two factors could play an important role in achieving high uptake and prolon ... Full text Link to item Cite

Non-invasive sensitive brain tumor detection using dual-modality bioimaging nanoprobe.

Journal Article Nanotechnology · July 5, 2019 Despite decades of efforts, non-invasive sensitive detection of small malignant brain tumors still remains challenging. Here we report a dual-modality 124I-labeled gold nanostar (124I-GNS) probe for sensitive brain tumor imaging with positron emission tomo ... Full text Link to item Cite

Labeling Single Domain Antibody Fragments with Fluorine-18 Using 2,3,5,6-Tetrafluorophenyl 6-[18F]Fluoronicotinate Resulting in High Tumor-to-Kidney Ratios.

Journal Article Mol Pharm · January 7, 2019 ImmunoPET agents are being investigated to assess the status of epidermal growth factor receptor 2 (HER2) in breast cancer patients with the goal of selecting those likely to benefit from HER2-targeted therapies and monitoring their progress after these tr ... Full text Link to item Cite

Pharmacodynamic study of radium-223 in men with bone metastatic castration resistant prostate cancer.

Journal Article PLoS One · 2019 BACKGROUND: Radium-223 is a targeted alpha-particle therapy that improves survival in men with metastatic castration resistant prostate cancer (mCRPC), particularly in men with elevated serum levels of bone alkaline phosphatase (B-ALP). We hypothesized tha ... Full text Link to item Cite

The Radiopharmaceutical Chemistry of the Radioisotopes of Iodine

Chapter · January 1, 2019 Radioisotopes of iodine have been incorporated into a wide variety of radiopharmaceuticals ranging from small, low molecular weight compounds to large molecules like antibodies. Because of the routine availability of radioisotopes of iodine with different ... Full text Cite

An Efficient Method for Labeling Single Domain Antibody Fragments with 18F Using Tetrazine- Trans-Cyclooctene Ligation and a Renal Brush Border Enzyme-Cleavable Linker.

Journal Article Bioconjug Chem · December 19, 2018 Single domain antibody fragments (sdAbs) labeled with 18F have shown promise for assessing the status of oncological targets such as the human epidermal growth factor receptor 2 (HER2) by positron emission tomography (PET). Earlier, we evaluated two residu ... Full text Link to item Cite

Synthesis and Evaluation of a 18F-Labeled Triazinediamine Analogue for Imaging Mutant IDH1 Expression in Gliomas by PET.

Journal Article ACS Med Chem Lett · July 12, 2018 Mutations in the isocitrate dehydrogenase gene 1 (IDH1) are common in gliomas. Studies suggest that IDH1 mutations are early events in glioma formation and are important drivers of malignant progression. Herein, we report the synthesis and evaluation of a ... Full text Link to item Cite

d-Amino Acid Peptide Residualizing Agents for Protein Radioiodination: Effect of Aspartate for Glutamate Substitution.

Journal Article Molecules · May 20, 2018 The residualizing prosthetic agent Nε-(3-[*I]iodobenzoyl)-Lys⁵-Nα-maleimido-Gly¹-d-GEEEK ([*I]IB-Mal-d-GEEEK) showed promise for the radioiodination of monoclonal antibodies (mAbs) that bind to internalizing molecular targets. Although enhanced tumor uptak ... Full text Link to item Cite

Fluorine-18 labeling of an anti-HER2 VHH using a residualizing prosthetic group via a strain-promoted click reaction: Chemistry and preliminary evaluation.

Journal Article Bioorg Med Chem · May 1, 2018 In a previous study, we evaluated a HER2-specific single domain antibody fragment (sdAb) 2Rs15d labeled with 18F via conjugation of a residualizing prosthetic agent that was synthesized by copper-catalyzed azide-alkyne cycloaddition (CuAAC). In order to po ... Full text Link to item Cite

Synthesis and evaluation of radiolabeled AGI-5198 analogues as candidate radiotracers for imaging mutant IDH1 expression in tumors.

Journal Article Bioorg Med Chem Lett · February 15, 2018 Mutations in the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) are commonly found in gliomas. AGI-5198, a potent and selective inhibitor of the mutant IDH1 enzyme, was radiolabeled with radioiodine and fluorine-18. These radiotracers were evaluated as ... Full text Link to item Cite

Astatine-211 labeled anti-HER2 5F7 single domain antibody fragment conjugates: radiolabeling and preliminary evaluation.

Journal Article Nucl Med Biol · January 2018 INTRODUCTION: Derived from heavy chain only camelid antibodies, ~15-kDa single-domain antibody fragments (sdAbs) are an attractive platform for developing molecularly specific imaging probes and targeted radiotherapeutics. The rapid tumor accumulation and ... Full text Open Access Link to item Cite

Brush border enzyme-cleavable linkers: Evaluation for reducing renal uptake of radiolabeled prostate-specific membrane antigen inhibitors.

Journal Article Nucl Med Biol · 2018 INTRODUCTION: Radiolabeled, low-molecular-weight prostate-specific membrane antigen (PSMA) inhibitors based on the Glu-ureido pharmacophore show promise for the detection and treatment of castration-resistant prostate cancer; however, high renal retention ... Full text Link to item Cite

Fluorine-18 Labeling of the HER2-Targeting Single-Domain Antibody 2Rs15d Using a Residualizing Label and Preclinical Evaluation.

Journal Article Mol Imaging Biol · December 2017 PURPOSE: Our previous studies with F-18-labeled anti-HER2 single-domain antibodies (sdAbs) utilized 5F7, which binds to the same epitope on HER2 as trastuzumab, complicating its use for positron emission tomography (PET) imaging of patients undergoing tras ... Full text Link to item Cite

131I-labeled Anti-HER2 Camelid sdAb as a Theranostic Tool in Cancer Treatment.

Journal Article Clin Cancer Res · November 1, 2017 Purpose: Camelid single-domain antibody-fragments (sdAb) have beneficial pharmacokinetic properties, and those targeted to HER2 can be used for imaging of HER2-overexpressing cancer. Labeled with a therapeutic radionuclide, they may be used for HER2-target ... Full text Link to item Cite

A model for optimizing delivery of targeted radionuclide therapies into resection cavity margins for the treatment of primary brain cancers.

Journal Article Biomed Phys Eng Express · June 2017 Radionuclides conjugated to molecules that bind specifically to cancer cells are of great interest as a means to increase the specificity of radiotherapy. Currently, the methods to disseminate these targeted radiotherapeutics have been either systemic deli ... Full text Open Access Link to item Cite

Radiopharmaceutical chemistry of targeted radiotherapeutics, part 4: Strategies for 211At labeling at high activities and radiation doses of 211At α-particles.

Journal Article Nucl Med Biol · March 2017 INTRODUCTION: Alpha particles are radiation of high energy and short range, properties that can lead to radiolysis-mediated complications in labeling chemistry at the high radioactivity levels required for clinical application. In previous papers in this s ... Full text Link to item Cite

Synthesis and Preliminary Evaluation of 5-[18F]fluoroleucine.

Journal Article Curr Radiopharm · 2017 BACKGROUND: Amino acid transporters, such as LAT1, are overexpressed in aggressive prostate and breast carcinomas, directly influencing pathways of growth and proliferation. OBJECTIVE: The purpose of this study was to synthesize and characterize a novel 18 ... Full text Open Access Link to item Cite

Preparation, cytotoxicity, and in vivo antitumor efficacy of 111In-labeled modular nanotransporters.

Journal Article Int J Nanomedicine · 2017 PURPOSE: Modular nanotransporters (MNTs) are a polyfunctional platform designed to achieve receptor-specific delivery of short-range therapeutics into the cell nucleus by receptor-mediated endocytosis, endosome escape, and targeted nuclear transport. This ... Full text Link to item Cite

(2S)-2-(3-(1-Carboxy-5-(4-211At-Astatobenzamido)Pentyl)Ureido)-Pentanedioic Acid for PSMA-Targeted α-Particle Radiopharmaceutical Therapy.

Journal Article J Nucl Med · October 2016 UNLABELLED: Alpha-particle emitters have a high linear energy transfer and short range, offering the potential for treating micrometastases while sparing normal tissues. We developed a urea-based, 211At-labeled small molecule targeting prostate-specific me ... Full text Link to item Cite

Prostate-Specific Membrane Antigen-Targeted Radiohalogenated PET and Therapeutic Agents for Prostate Cancer.

Journal Article J Nucl Med · October 2016 Radiohalogenated agents are often the first line of pursuit in the development of new radiopharmaceuticals-whether antibodies, peptides, or small molecules-because of their ease of synthesis, lack of substantial steric perturbation of the original affinity ... Full text Link to item Cite

Anti-HER2 Single Domain Antibody 2Rs15d Labeled with F-18 Using a Residualizing Label: Preliminary Evaluation

Conference EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING · October 1, 2016 Link to item Cite

Radiolabeled inhibitors as probes for imaging mutant IDH1 expression in gliomas: Synthesis and preliminary evaluation of labeled butyl-phenyl sulfonamide analogs.

Journal Article Eur J Med Chem · August 25, 2016 INTRODUCTION: Malignant gliomas frequently harbor mutations in the isocitrate dehydrogenase 1 (IDH1) gene. Studies suggest that IDH mutation contributes to tumor pathogenesis through mechanisms that are mediated by the neomorphic metabolite of the mutant I ... Full text Open Access Link to item Cite

Preclinical Evaluation of 18F-Labeled Anti-HER2 Nanobody Conjugates for Imaging HER2 Receptor Expression by Immuno-PET.

Journal Article J Nucl Med · June 2016 UNLABELLED: The human growth factor receptor type 2 (HER2) is overexpressed in breast as well as other types of cancer. Immuno-PET, a noninvasive imaging procedure that could assess HER2 status in both primary and metastatic lesions simultaneously, could b ... Full text Link to item Cite

Injectable polypeptide micelles that form radiation crosslinked hydrogels in situ for intratumoral radiotherapy.

Journal Article J Control Release · April 28, 2016 Intratumoral radiation therapy - 'brachytherapy' - is a highly effective treatment for solid tumors, particularly prostate cancer. Current titanium seed implants, however, are permanent and are limited in clinical application to indolent malignancies of lo ... Full text Link to item Cite

Preclinical toxicity evaluation of a novel immunotoxin, D2C7-(scdsFv)-PE38KDEL, administered via intracerebral convection-enhanced delivery in rats.

Journal Article Invest New Drugs · April 2016 D2C7-(scdsFv)-PE38KDEL (D2C7-IT) is a novel immunotoxin that reacts with wild-type epidermal growth factor receptor (EGFRwt) and mutant EGFRvIII proteins overexpressed in glioblastomas. This study assessed the toxicity of intracerebral administration of D2 ... Full text Link to item Cite

Spatiotemporally photoradiation-controlled intratumoral depot for combination of brachytherapy and photodynamic therapy for solid tumor.

Journal Article Biomaterials · February 2016 In an attempt to spatiotemporally control both tumor retention and the coverage of anticancer agents, we developed a photoradiation-controlled intratumoral depot (PRCITD) driven by convection enhanced delivery (CED). This intratumoral depot consists of rec ... Full text Link to item Cite

N-Succinimidyl 3-((4-(4-[(18)F]fluorobutyl)-1H-1,2,3-triazol-1-yl)methyl)-5-(guanidinomethyl)benzoate ([(18)F]SFBTMGMB): a residualizing label for (18)F-labeling of internalizing biomolecules.

Journal Article Org Biomol Chem · January 28, 2016 Residualizing labeling methods for internalizing peptides and proteins are designed to trap the radionuclide inside the cell after intracellular degradation of the biomolecule. The goal of this work was to develop a residualizing label for the (18)F-labeli ... Full text Link to item Cite

An Anti-HER2 Nanobody Labeled with 18F Using a Residualizing Label for Assessing HER2 Status

Conference EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING · October 1, 2015 Link to item Cite

Synthesis and evaluation of 4-[18F]fluoropropoxy-3-iodobenzylguanidine ([18F]FPOIBG): A novel 18F-labeled analogue of MIBG.

Journal Article Nucl Med Biol · August 2015 INTRODUCTION: Radioiodinated meta-iodobenzylguanidine (MIBG), a norepinephrine transporter (NET) substrate, has been extensively used as an imaging agent to study the pathophysiology of the heart and for the diagnosis and treatment of neuroendocrine tumors ... Full text Link to item Cite

Abstract 1809: Next-generation brachytherapy: a preclinical study of a thermally stabilized biopolymer gel for delivering intratumoral radionuclide therapy in a pancreatic tumor mouse model

Conference Cancer Research · August 1, 2015 AbstractThe intratumoral delivery of radioactive therapeutics, a clinical technique known as brachytherapy, has proven very successful in treating solid cancers and become a prevalent option for treating pro ... Full text Cite

Stability and in vivo behavior of Rh[16aneS4-diol]211 at complex: a potential precursor for astatine radiopharmaceuticals.

Journal Article Nucl Med Biol · May 2015 INTRODUCTION: The heavy halogen (211)At is of great interest for targeted radiotherapy because it decays by the emission of short-range, high-energy α-particles. However, many astatine compounds that have been synthesized are unstable in vivo, providing mo ... Full text Link to item Cite

D-Amino acid peptide residualizing agents bearing N-hydroxysuccinimido- and maleimido-functional groups and their application for trastuzumab radioiodination.

Journal Article Nucl Med Biol · January 2015 INTRODUCTION: Proteins that undergo receptor-mediated endocytosis are subject to lysosomal degradation, requiring radioiodination methods that minimize loss of radioactivity from tumor cells after this process occurs. To accomplish this, we developed the r ... Full text Open Access Link to item Cite

Modular nanotransporters for targeted intracellular delivery of drugs: folate receptors as potential targets.

Journal Article Curr Pharm Des · 2015 The review is devoted to a subcellular drug delivery system, modular nanotransporters (MNT) that can penetrate into target cells and deliver a therapeutic into their subcellular compartments, particularly into the nucleus. The therapeutics which need such ... Full text Link to item Cite

A Plasmonic Gold Nanostar Theranostic Probe for In Vivo Tumor Imaging and Photothermal Therapy.

Journal Article Theranostics · 2015 Nanomedicine has attracted increasing attention in recent years, because it offers great promise to provide personalized diagnostics and therapy with improved treatment efficacy and specificity. In this study, we developed a gold nanostar (GNS) probe for m ... Full text Open Access Link to item Cite

Modular nanotransporters for targeted intracellular delivery of drugs: Folate receptors as potential targets

Journal Article Current Pharmaceutical Design · 2015 © 2015 Bentham Science Publishers.The review is devoted to a subcellular drug delivery system, modular nanotransporters (MNT) that can penetrate into target cells and deliver a therapeutic into their subcellular compartments, particularly into the nucleus. ... Cite

Copper signaling axis as a target for prostate cancer therapeutics.

Journal Article Cancer Res · October 15, 2014 Previously published reports indicate that serum copper levels are elevated in patients with prostate cancer and that increased copper uptake can be used as a means to image prostate tumors. It is unclear, however, to what extent copper is required for pro ... Full text Open Access Link to item Cite

Radiolabeling and in vitro evaluation of (67)Ga-NOTA-modular nanotransporter--a potential Auger electron emitting EGFR-targeted radiotherapeutic.

Journal Article Nucl Med Biol · July 2014 INTRODUCTION: Modular nanotransporters (MNTs) are vehicles designed to transport drugs from the cell surface via receptor-mediated endocytosis and endosomal escape to nucleus. Hence their conjugation to Auger electron emitters, can cause severe cell killin ... Full text Link to item Cite

Comparison of the Hypoxia PET Tracer (18)F-EF5 to Immunohistochemical Marker EF5 in 3 Different Human Tumor Xenograft Models.

Journal Article J Nucl Med · July 2014 UNLABELLED: The availability of (18)F-labeled and unlabeled 2-(2-nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl)-acetamide (EF5) allows for a comparative assessment of tumor hypoxia by PET and immunohistochemistry; however, the combined use of thes ... Full text Link to item Cite

Improved tumor targeting of anti-HER2 nanobody through N-succinimidyl 4-guanidinomethyl-3-iodobenzoate radiolabeling.

Journal Article J Nucl Med · April 2014 UNLABELLED: Nanobodies are approximately 15-kDa proteins based on the smallest functional fragments of naturally occurring heavy chain-only antibodies and represent an attractive platform for the development of molecularly targeted agents for cancer diagno ... Full text Link to item Cite

N-Succinimidyl guanidinomethyl iodobenzoate protein radiohalogenation agents: influence of isomeric substitution on radiolabeling and target cell residualization.

Journal Article Nucl Med Biol · 2014 INTRODUCTION: N-succinimidyl 4-guanidinomethyl-3-[(*)I]iodobenzoate ([(*)I]SGMIB) has shown promise for the radioiodination of monoclonal antibodies (mAbs) and other proteins that undergo extensive internalization after receptor binding, enhancing tumor ta ... Full text Link to item Cite

Abstract C86: Tethered Hsp90 inhibitors carrying optical or radioiodinated probes reveal selective internalization of ectopic Hsp90 in malignant breast tumor cells.

Conference Molecular Cancer Therapeutics · November 1, 2013 AbstractHsp90 inhibitors have demonstrated unusual selectivity for tumor cells despite its ubiquitous expression. This phenomenon has remained unexplained but could be influenced by ectopically expressed Hsp ... Full text Cite

Optical and radioiodinated tethered Hsp90 inhibitors reveal selective internalization of ectopic Hsp90 in malignant breast tumor cells.

Journal Article Chem Biol · September 19, 2013 Inhibitors of heat-shock protein 90 (Hsp90) have demonstrated an unusual selectivity for tumor cells despite its ubiquitous expression. This phenomenon has remained unexplained, but could be influenced by ectopically expressed Hsp90 in tumors. In this work ... Full text Link to item Cite

18F-EF5 PET imaging as an early response biomarker for the hypoxia-activated prodrug SN30000 combined with radiation treatment in a non-small cell lung cancer xenograft model.

Journal Article J Nucl Med · August 2013 UNLABELLED: Hypoxia is a significant therapeutic problem for solid tumors because hypoxic cells are treatment-resistant and more aggressive. Hypoxia-activated prodrugs such as SN30000 use a mechanism of activation in hypoxic cells similar to that of 2-nitr ... Full text Link to item Cite

Abstract 4341: A novel injectable polymer liquid that self-assembles into radioactive “seeds” for brachytherapy.

Conference Cancer Research · April 15, 2013 AbstractBrachytherapy seeds are made by sealing radionuclides in metal or other non-degradable material (resin or glass) and surgically implanted into the tumor tissue. Brachytherapy has shown some efficacy ... Full text Cite

Targeting breast carcinoma with radioiodinated anti-HER2 Nanobody.

Journal Article Nucl Med Biol · January 2013 INTRODUCTION: With a molecular weight an order of magnitude lower than antibodies but possessing comparable affinities, Nanobodies (Nbs) are attractive as targeting agents for cancer diagnosis and therapy. An anti-HER2 Nb could be utilized to determine HER ... Full text Link to item Cite

SIB-DOTA: a trifunctional prosthetic group potentially amenable for multi-modal labeling that enhances tumor uptake of internalizing monoclonal antibodies.

Journal Article Bioorg Med Chem · December 15, 2012 A major drawback of internalizing monoclonal antibodies (mAbs) radioiodinated with direct electrophilic approaches is that tumor retention of radioactivity is compromised by the rapid washout of iodo-tyrosine, the primary labeled catabolite for mAbs labele ... Full text Link to item Cite

Brachytherapy using injectable seeds that are self-assembled from genetically encoded polypeptides in situ.

Journal Article Cancer Res · November 15, 2012 Brachytherapy is a common clinical technique involving implantation of sealed radioactive "seeds" within a tumor to selectively irradiate the tumor mass while minimizing systemic toxicity. To mitigate the disadvantages associated with complex surgical impl ... Full text Link to item Cite

Modular nanotransporters: a versatile approach for enhancing nuclear delivery and cytotoxicity of Auger electron-emitting 125I.

Journal Article EJNMMI Res · October 29, 2012 BACKGROUND: This study evaluates the potential utility of a modular nanotransporter (MNT) for enhancing the nuclear delivery and cytotoxicity of the Auger electron emitter 125I in cancer cells that overexpress the epidermal growth factor receptor (EGFR). M ... Full text Open Access Link to item Cite

A simplified synthesis of the hypoxia imaging agent 2-(2-Nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-[(18)F]pentafluoropropyl)-acetamide ([18F]EF5).

Journal Article Nucl Med Biol · October 2012 INTRODUCTION: [(18)F]EF5 is a validated marker for PET imaging of tumor hypoxia. It is prepared by reacting a trifluoroallyl precursor with carrier-added [(18)F]F(2) gas in trifluoroacetic acid (TFA) solvent. We report here an improved radiosynthesis and p ... Full text Link to item Cite

Protein polymer hydrogels by in situ, rapid and reversible self-gelation.

Journal Article Biomaterials · July 2012 Protein-based biomaterials are an important class of materials for applications in biotechnology and medicine. The exquisite control of their composition, stereochemistry, and chain length offers unique opportunities to engineer biofunctionality, biocompat ... Full text Link to item Cite

Abstract 2884: Preclinical studies on tumor retention, antitumor efficacy and toxicity of thermally responsive polypeptide-based radionuclide intratumoral depot in nude mice

Journal Article Cancer Research · April 15, 2012 AbstractDespite clear advantages of brachytherapy over external beam radiotherapy, current implementations of this approach have several limitations. These include the need for general anesthesia or intraven ... Full text Cite

TARGETED ALPHA THERAPY

Conference RADIOTHERAPY AND ONCOLOGY · March 1, 2012 Link to item Cite

Radioimmunotargeting of malignant glioma by monoclonal antibody D2C7 reactive against both wild-type and variant III mutant epidermal growth factor receptors.

Journal Article Nucl Med Biol · January 2012 INTRODUCTION: Malignant glioma remains a significant therapeutic challenge, and immunotherapeutics might be a beneficial approach for these patients. A monoclonal antibody (MAb) specific for multiple molecular targets could expand the treatable patient pop ... Full text Link to item Cite

Modular nanotransporters: a multipurpose in vivo working platform for targeted drug delivery.

Journal Article Int J Nanomedicine · 2012 BACKGROUND: Modular nanotransporters (MNT) are recombinant multifunctional polypeptides created to exploit a cascade of cellular processes, initiated with membrane receptor recognition to deliver selective short-range and highly cytotoxic therapeutics to t ... Full text Open Access Link to item Cite

Applications of 211At and 223Ra in targeted alpha-particle radiotherapy.

Journal Article Curr Radiopharm · October 2011 Targeted radiotherapy using agents tagged with α-emitting radionuclides is gaining traction with several clinical trials already undertaken or ongoing, and others in the advanced planning stage. The most commonly used α-emitting radionuclides are 213Bi, 21 ... Full text Link to item Cite

An alternative and expedient synthesis of radioiodinated 4-iodophenylalanine.

Journal Article Appl Radiat Isot · October 2011 Radiolabeled amino acids have been used extensively in oncology both as diagnostic and therapeutic agents. In our pursuit to develop radiopharmaceuticals to target breast cancer, we were interested in determining the uptake of radioiodinated 4-iodophenylal ... Full text Link to item Cite

Colocalization of gadolinium-diethylene triamine pentaacetic acid with high-molecular-weight molecules after intracerebral convection-enhanced delivery in humans.

Journal Article Neurosurgery · September 2011 BACKGROUND: Convection-enhanced delivery (CED) permits site-specific therapeutic drug delivery within interstitial spaces at increased dosages through circumvention of the blood-brain barrier. CED is currently limited by suboptimal methodologies for monito ... Full text Link to item Cite

Astatine-211: production and availability.

Journal Article Curr Radiopharm · July 2011 The 7.2-h half life radiohalogen (211)At offers many potential advantages for targeted α-particle therapy; however, its use for this purpose is constrained by its limited availability. Astatine-211 can be produced in reasonable yield from natural bismuth t ... Full text Link to item Cite

Abstract 5306: 18F-EF5 microPET imaging of treatment response from a novel, hypoxia-selective cytotoxin SN30000 in a human lung cancer xenograft model

Journal Article Cancer Research · April 15, 2011 AbstractIntroduction: SN30000 (CEN-209) is a structural analogue of the clinically tested hypoxic cell cytotoxin tirapazamine, with improved tumor penetration and increased hypoxic cell kill activity in vitr ... Full text Cite

Molecular imaging of hypoxia.

Journal Article J Nucl Med · February 2011 A wide variety of imaging approaches have been developed in the past few decades for monitoring tumor oxygenation and hypoxia in vivo. In particular, nuclear medicine has seen the development of several radiolabeled hypoxia markers and is the preferred met ... Full text Link to item Cite

Radioiodinated O(6)-Benzylguanine derivatives containing an azido function.

Journal Article Nucl Med Biol · January 2011 INTRODUCTION: Drug resistance to alkylator chemotherapy has been primarily attributed to the DNA repair protein alkylguanine-DNA alkyltransferase (AGT); thus, personalizing chemotherapy could be facilitated if tumor AGT content could be quantified prior to ... Full text Link to item Cite

Applications of 211AT and 223RA in targeted alpha-particle radiotherapy

Journal Article Current Radiopharmaceuticals · 2011 Targeted radiotherapy using agents tagged with α-emitting radionuclides is gaining traction with several clinical trials already undertaken or ongoing, and others in the advanced planning stage. The most commonly used α-emitting radionuclides are 213Bi, 21 ... Cite

Anti-EGFRvIII monoclonal antibody armed with 177Lu: in vivo comparison of macrocyclic and acyclic ligands.

Journal Article Nucl Med Biol · October 2010 INTRODUCTION: Monoclonal antibody (mAb) L8A4 binds specifically to the epidermal growth factor receptor variant III (EGFRvIII) that is present on gliomas but not on normal tissues, and is internalized rapidly after receptor binding. Because of the short ra ... Full text Link to item Cite

Evaluation of anti-podoplanin rat monoclonal antibody NZ-1 for targeting malignant gliomas.

Journal Article Nucl Med Biol · October 2010 INTRODUCTION: Podoplanin/aggrus is a mucin-like sialoglycoprotein that is highly expressed in malignant gliomas. Podoplanin has been reported to be a novel marker to enrich tumor-initiating cells, which are thought to resist conventional therapies and to b ... Full text Link to item Cite

Radioiodinated O6-Benzylguanine Analogues Containing an Azido Function

Conference EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING · October 1, 2010 Link to item Cite

In situ growth of a PEG-like polymer from the C terminus of an intein fusion protein improves pharmacokinetics and tumor accumulation.

Journal Article Proc Natl Acad Sci U S A · September 21, 2010 This paper reports a general in situ method to grow a polymer conjugate solely from the C terminus of a recombinant protein. GFP was fused at its C terminus with an intein; cleavage of the intein provided a unique thioester moiety at the C terminus of GFP ... Full text Link to item Cite

Recombinant single-chain variable fragment antibodies against extracellular epitopes of human multidrug resistance protein MRP3 for targeting malignant gliomas.

Journal Article Int J Cancer · August 1, 2010 Multidrug resistance protein 3 (MRP3), a multidrug resistance protein identified by serial analysis of gene expression as a glioblastoma multiforme (GBM)-associated molecule, is highly expressed in GBM, but not in normal brain cells. Thus, MRP3 is a candid ... Full text Link to item Cite

Injectable intratumoral depot of thermally responsive polypeptide-radionuclide conjugates delays tumor progression in a mouse model.

Journal Article J Control Release · May 21, 2010 This study evaluated a biodegradable drug delivery system for local cancer radiotherapy consisting of a thermally sensitive elastin-like polypeptide (ELP) conjugated to a therapeutic radionuclide. Two ELPs (49 kDa) were synthesized using genetic engineerin ... Full text Link to item Cite

[Lu]-DOTA-Tyr-octreotate: A Potential Targeted Radiotherapeutic for the Treatment of Medulloblastoma.

Journal Article Curr Radiopharm · 2010 Medulloblastoma, the most common pediatric brain tumor, is difficult to treat because conventional therapeutic approaches result in significant toxicity to normal central nervous system tissues, compromising quality of life. Given the fact that medulloblas ... Full text Link to item Cite

Detection of amino-terminal extracellular domain of somatostatin receptor 2 by specific monoclonal antibodies and quantification of receptor density in medulloblastoma.

Journal Article Hybridoma (Larchmt) · December 2009 Somatostatin receptor 2 (SSTR2) is expressed by most medulloblastomas (MEDs). We isolated monoclonal antibodies (MAbs) to the 12-mer (33)QTEPYYDLTSNA(44), which resides in the extracellular domain of the SSTR2 amino terminus, screened the peptide-bound MAb ... Full text Open Access Link to item Cite

Targeting aldehyde dehydrogenase: a potential approach for cell labeling.

Journal Article Nucl Med Biol · November 2009 INTRODUCTION: To advance the science and clinical application of stem cell therapy, the availability of a highly sensitive, quantitative and translational method for tracking stem cells would be invaluable. Because hematopoetic stem cells express high leve ... Full text Link to item Cite

In situ growth of a stoichiometric PEG-like conjugate at a protein's N-terminus with significantly improved pharmacokinetics.

Journal Article Proc Natl Acad Sci U S A · September 8, 2009 The challenge in the synthesis of protein-polymer conjugates for biological applications is to synthesize a stoichiometric (typically 1:1) conjugate of the protein with a monodisperse polymer, with good retention of protein activity, significantly improved ... Full text Link to item Cite

Treatment of HER2-positive breast carcinomatous meningitis with intrathecal administration of alpha-particle-emitting (211)At-labeled trastuzumab.

Journal Article Nucl Med Biol · August 2009 INTRODUCTION: Carcinomatous meningitis (CM) is a devastating disease characterized by the dissemination of malignant tumor cells into the subarachnoid space along the brain and spine. Systemic treatment with monoclonal antibody (mAb) trastuzumab can be eff ... Full text Link to item Cite

Evaluation of an anti-p185(HER2) (scFv-C(H)2-C(H)3)2 fragment following radioiodination using two different residualizing labels: SGMIB and IB-Mal-D-GEEEK.

Journal Article Nucl Med Biol · August 2009 INTRODUCTION: A 105-kDa double mutant single-chain Fv-Fc fragment (scFv-Fc DM) derived from the anti-p185(HER2) hu4D5v8 antibody (trastuzumab; Herceptin) has been described recently. The goal of this study was to investigate whether improved tumor targetin ... Full text Link to item Cite

Labeling internalizing anti-epidermal growth factor receptor variant III monoclonal antibody with (177)Lu: in vitro comparison of acyclic and macrocyclic ligands.

Journal Article Nucl Med Biol · February 2009 INTRODUCTION: The monoclonal antibody (mAb) L8A4, reactive with the epidermal growth factor receptor variant III (EGFRvIII), internalizes rapidly in glioma cells after receptor binding. Combining this tumor-specific mAb with the low-energy beta-emitter (17 ... Full text Link to item Cite

Propargyl 4-[F]fluorobenzoate: A Putatively More Stable Prosthetic group for the Fluorine-18 Labeling of Biomolecules via Click Chemistry.

Journal Article Curr Radiopharm · January 1, 2009 Faster and more efficient approaches for radiolabeling biomolecules with short-lived (18)F are in dire need. Herein we report a new (18)F-labeled prosthetic group containing an acetylene function that permits the labeling of biomolecules via click chemistr ... Full text Link to item Cite

Engineered modular recombinant transporters: application of new platform for targeted radiotherapeutic agents to alpha-particle emitting 211 At.

Journal Article Int J Radiat Oncol Biol Phys · September 1, 2008 PURPOSE: To generate and evaluate a modular recombinant transporter (MRT) for targeting 211 At to cancer cells overexpressing the epidermal growth factor receptor (EGFR). METHODS AND MATERIALS: The MRT was produced with four functional modules: (1) human e ... Full text Link to item Cite

Astatine Radiopharmaceuticals: Prospects and Problems.

Journal Article Curr Radiopharm · September 1, 2008 For the treatment of minimum residual diseases such micrometastases and residual tumor margins that remain after debulking of the primary tumor, targeted radiotherapy using radiopharmaceuticals tagged with alpha-particle-emitting radionuclides is very attr ... Full text Link to item Cite

Intracerebral infusion of an EGFR-targeted toxin in recurrent malignant brain tumors.

Journal Article Neuro Oncol · June 2008 The purpose of this study is to determine the maximum tolerated dose (MTD), dose-limiting toxicity (DLT), and intracerebral distribution of a recombinant toxin (TP-38) targeting the epidermal growth factor receptor in patients with recurrent malignant brai ... Full text Link to item Cite

A pilot study: 131I-antitenascin monoclonal antibody 81c6 to deliver a 44-Gy resection cavity boost.

Journal Article Neuro Oncol · April 2008 The purpose of this study was to determine the feasibility and assess the efficacy and toxicity, among newly diagnosed malignant glioma patients, of administering (131)I-labeled murine antitenascin monoclonal antibody 81C6 ((131)I-81C6) into a surgically c ... Full text Link to item Cite

Preparation of Rh[16aneS4-diol](211)At and Ir[16aneS4-diol](211)At complexes as potential precursors for astatine radiopharmaceuticals. Part I: Synthesis.

Journal Article Bioconjug Chem · April 2008 The goal of this study was to evaluate a new approach that can be applied for labeling biomolecules with (211)At. Many astatine compounds that have been synthesized are unstable in vivo, providing motivation for seeking different (211)At labeling strategie ... Full text Link to item Cite

Clinical experience with alpha-particle emitting 211At: treatment of recurrent brain tumor patients with 211At-labeled chimeric antitenascin monoclonal antibody 81C6.

Journal Article J Nucl Med · January 2008 UNLABELLED: alpha-Particle-emitting radionuclides, such as (211)At, with a 7.2-h half-life, may be optimally suited for the molecularly targeted radiotherapy of strategically sensitive tumor sites, such as those in the central nervous system. Because of th ... Full text Link to item Cite

Radiolabelling of glucose-Tyr3-octreotate with 125I and analysis of its metabolism in rats: Comparison with radiolabelled DOTA-Tyr3-octreotate

Journal Article Anticancer Research · November 1, 2007 Background: Somatostatin analogues labelled with radiometals or radiohalogens are useful for the imaging and treatment of somatostatin receptor-containing tumours. In this study, the procedures for the radioiodination of glucose-Tyr3-octreotate (gluc-Tyr 3 ... Cite

Targeted alpha-particle radiotherapy with 211At-labeled monoclonal antibodies.

Journal Article Nucl Med Biol · October 2007 An attractive feature of targeted radionuclide therapy is the ability to select radionuclides and targeting vehicles with characteristics that are best suited for a particular clinical application. One combination that has been receiving increasing attenti ... Full text Link to item Cite

[I-125] iodoquine uptake in tumor cell lines with high ALDH expression

Conference EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING · October 1, 2007 Link to item Cite

Synthesis of Rh[16aneS4] At-211 and Ir[16aneS4] At-211 complexes - new prosthetic groups for labelling with astatine.

Conference EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING · October 1, 2007 Link to item Cite

Radiopharmaceutical chemistry of targeted radiotherapeutics, Part 3: alpha-particle-induced radiolytic effects on the chemical behavior of (211)At.

Journal Article J Nucl Med · July 2007 UNLABELLED: Two characteristics of alpha-particles that enhance their potential for targeted radiotherapy are their high energy and approximately cellular range. Unfortunately, these properties also can have negative consequences, confounding the productio ... Full text Link to item Cite

A kit method for the high level synthesis of [211At]MABG.

Journal Article Bioorg Med Chem · May 15, 2007 meta-[(211)At]Astatobenzylguanidine ([(211)At]MABG), an analogue of meta-iodobenzylguanidine (MIBG) labeled with the alpha-emitter (211)At, targets the norepinephrine transporter. Because MABG has been shown to have excellent characteristics in preclinical ... Full text Link to item Cite

Tumor resection cavity administered iodine-131-labeled antitenascin 81C6 radioimmunotherapy in patients with malignant glioma: neuropathology aspects.

Journal Article Nucl Med Biol · May 2007 INTRODUCTION: The neurohistological findings in patients treated with targeted beta emitters such as (131)I are poorly described. We report a histopathologic analysis from patients treated with combined external beam therapy and a brachytherapy consisting ... Full text Link to item Cite

Antitenascin-C monoclonal antibody radioimmunotherapy for malignant glioma patients.

Journal Article Expert Rev Anticancer Ther · May 2007 Adults with primary malignant glioma have an unacceptably poor outcome. Most of these tumors recur at or adjacent to the site of origin, which indicates that failure to eradicate local tumor growth is a major factor contributing to poor outcome. Therefore, ... Full text Link to item Cite

Antitenascin antibody 81C6 armed with 177Lu: in vivo comparison of macrocyclic and acyclic ligands.

Journal Article Nucl Med Biol · February 2007 INTRODUCTION: When labeled with iodine-131, the antitenascin monoclonal antibody (mAb) 81C6 has shown promise as a targeted radiotherapeutic in patients with brain tumors. Because of its more favorable gamma-ray properties, lutetium-177 might be a better l ... Full text Link to item Cite

Radiolabelling of glucose-Tyr3-octreotate with 125I and analysis of its metabolism in rats: comparison with radiolabelled DOTA-Tyr3-octreotate.

Journal Article Anticancer Res · 2007 BACKGROUND: Somatostatin analogues labelled with radiometals or radiohalogens are useful for the imaging and treatment of somatostatin receptor-containing tumours. In this study, the procedures for the radioiodination of glucose-Tyr3-octreotate (gluc-Tyr3- ... Link to item Cite

Synthesis of N-succinimidyl 4-guanidinomethyl-3-[*I]iodobenzoate: a radio-iodination agent for labeling internalizing proteins and peptides.

Journal Article Nat Protoc · 2007 This protocol describes a detailed procedure for the synthesis of N-succinimidyl 4-guanidinomethyl-3-[*I]iodobenzoate ([*I]SGMIB), an agent useful in the radio-iodination of proteins, including monoclonal Abs, and peptides that undergo internalization afte ... Full text Link to item Cite

A radioiodinated MIBG-octreotate conjugate exhibiting enhanced uptake and retention in SSTR2-expressing tumor cells.

Journal Article Bioconjug Chem · 2007 Several neuroendocrine tumors are known to express both the somatostatin receptor subtype 2 (SSTR2) and the norepinephrine transporter (NET), and radiopharmaceuticals directed toward both these targets such as MIBG and octreotide derivatives are routinely ... Full text Link to item Cite

A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211At]MABG

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · January 1, 2007 Radioiodinated MIBG has shown considerable promise as an imaging agent for cardiac and oncologic applications, and also as a targeted radio therapeutic for treating patients with neuroendocrine tumors. This radiolabeled agent, synthesized at a no-carrier-a ... Full text Cite

Tumor accumulation, degradation and pharmacokinetics of elastin-like polypeptides in nude mice.

Journal Article J Control Release · November 28, 2006 ELPs are genetically engineered, thermally responsive polypeptides that preferentially accumulate in solid tumors subjected to focused, mild hyperthermia. In this paper, we report the biodegradation, pharmacokinetics, tumor localization, and tumor spatial ... Full text Link to item Cite

A thermally responsive biopolymer for intra-articular drug delivery.

Journal Article J Control Release · October 10, 2006 Intra-articular drug delivery is the preferred standard for targeting pharmacologic treatment directly to joints to reduce undesirable side effects associated with systemic drug delivery. In this study, a biologically based drug delivery vehicle was design ... Full text Link to item Cite

Preclinical pharmacokinetic comparison of glucose-125I-Tyr3-octreotate with DOTA-125I-Tyr3-octreotate

Journal Article EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING · September 1, 2006 Link to item Cite

Tracking the in vivo fate of recombinant polypeptides by isotopic labeling.

Journal Article J Control Release · August 28, 2006 We report a method to incorporate a stable isotope (13C) and a radioactive isotope (14C) into a recombinant polypeptide during Escherichia coli culture in M9 minimal medium supplemented with universally labeled 13C- or 14C-labeled glucose. We chose a therm ... Full text Link to item Cite

Radiation-induced biologic bystander effect elicited in vitro by targeted radiopharmaceuticals labeled with alpha-, beta-, and auger electron-emitting radionuclides.

Journal Article J Nucl Med · June 2006 UNLABELLED: Recent studies have shown that indirect effects of ionizing radiation may contribute significantly to the effectiveness of radiotherapy by sterilizing malignant cells that are not directly hit by the radiation. However, there have been few inve ... Link to item Cite

Novel human IgG2b/murine chimeric antitenascin monoclonal antibody construct radiolabeled with 131I and administered into the surgically created resection cavity of patients with malignant glioma: phase I trial results.

Journal Article J Nucl Med · June 2006 UNLABELLED: Results from animal experiments have shown that human IgG2/mouse chimeric antitenascin 81C6 (ch81C6) monoclonal antibody exhibited higher tumor accumulation and enhanced stability compared with its murine parent. Our objective was to determine ... Link to item Cite

Molecular imaging of alkylguanine-DNA alkyltransferase: further evaluation of radioiodinated derivatives of O6-benzylguanine.

Journal Article Nucl Med Biol · April 2006 PURPOSE: An inverse correlation has been established between tumor levels of the DNA repair protein alkylguanine-DNA alkyltransferase (AGT) and a positive outcome after alkylator chemotherapy. Quantitative imaging of AGT could provide important information ... Full text Link to item Cite

In vitro cytotoxicity of 211At-labeled trastuzumab in human breast cancer cell lines: effect of specific activity and HER2 receptor heterogeneity on survival fraction.

Journal Article Nucl Med Biol · April 2006 INTRODUCTION: Radioimmunotherapy with anti-HER2 monoclonal antibodies (mAbs) such as trastuzumab is a promising strategy for treating HER2-positive breast and ovarian carcinoma patients. The objective of this study was to determine the cytotoxic effectiven ... Full text Link to item Cite

Salvage radioimmunotherapy with murine iodine-131-labeled antitenascin monoclonal antibody 81C6 for patients with recurrent primary and metastatic malignant brain tumors: phase II study results.

Journal Article J Clin Oncol · January 1, 2006 PURPOSE: To assess the efficacy and toxicity of intraresection cavity iodine-131-labeled murine antitenascin monoclonal antibody 81C6 (131I-m81C6) among recurrent malignant brain tumor patients. PATIENTS AND METHODS: In this phase II trial, 100 mCi of 131I ... Full text Link to item Cite

Preparation of N-succinimidyl 3-[*I]iodobenzoate: an agent for the indirect radioiodination of proteins.

Journal Article Nat Protoc · 2006 A procedure for the synthesis of N-succinimidyl 3-iodobenzoate labeled with any iodine isotope ([*I]SIB), which is an agent used in the radioiodination of proteins and peptides, from its tin precursor N-succinimidyl 3-(tri-n-butylstannyl)benzoate (STB) is ... Full text Link to item Cite

Synthesis of N-succinimidyl 4-[18F]fluorobenzoate, an agent for labeling proteins and peptides with 18F.

Journal Article Nat Protoc · 2006 This protocol describes the step-by-step procedure for the synthesis of N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB), an agent widely used for labeling proteins and peptides with the positron-emitting radionuclide 18F. The protocols for the synthesis of ... Full text Link to item Cite

Antiepidermal growth factor variant III scFv fragment: effect of radioiodination method on tumor targeting and normal tissue clearance.

Journal Article Nucl Med Biol · January 2006 INTRODUCTION: MR1-1 is a single-chain Fv (scFv) fragment that binds with high affinity to epidermal growth factor receptor variant III, which is overexpressed on gliomas and other tumors but is not present on normal tissues. The objective of this study was ... Full text Link to item Cite

Synthesis and evaluation of glycosylated octreotate analogues labeled with radioiodine and 211At via a tin precursor.

Journal Article Bioconjug Chem · 2006 Carbohydration of N-terminus and substitution of a threonine for the threoninol residue at the C-terminus of Tyr3-octreotide (TOC) has resulted in improved pharmacokinetics and tumor targeting of its radioiodinated derivatives. Yet, these peptides are very ... Full text Link to item Cite

Nepsilon-(3-[*I]Iodobenzoyl)-Lys5-Nalpha-maleimido-Gly1-GEEEK ([*I]IB-Mal-D-GEEEK): a radioiodinated prosthetic group containing negatively charged D-glutamates for labeling internalizing monoclonal antibodies.

Journal Article Bioconjug Chem · 2006 Novel methods are needed for the radiohalogenation of cell-internalizing proteins and peptides because rapid loss of label occurs after lysosomal processing when these molecules are labeled using conventional radioiodination methodologies. We have develope ... Full text Link to item Cite

Comparison of radiohaloanalogues of meta-iodobenzylguanidine (MIBG) for a combined gene- and targeted radiotherapy approach to bladder carcinoma.

Journal Article Med Chem · November 2005 Targeted radiotherapy using radiolabelled meta-iodobenzylguanidine (MIBG) is a promising treatment option for bladder cancer, restricting the effects of radiotherapy to malignant cells thereby increasing efficacy and decreasing morbidity of radiotherapy. W ... Full text Link to item Cite

Radiopharmaceutical chemistry of targeted radiotherapeutics, Part 2: radiolytic effects of 211At alpha-particles influence N-succinimidyl 3-211AT-astatobenzoate synthesis.

Journal Article J Nucl Med · August 2005 UNLABELLED: A variety of promising targeted radiotherapeutics labeled with alpha-emitters have been developed. Clinical investigation of these radiopharmaceuticals requires the production of high activity levels, which can be hindered by alpha-particle-med ... Link to item Cite

O6-3-[125I]iodobenzyl-2'-deoxyguanosine ([125I]IBdG): synthesis and evaluation of its usefulness as an agent for quantification of alkylguanine-DNA alkyltransferase (AGT).

Journal Article Bioorg Med Chem · June 2, 2005 The development of O(6)-(3-[(125)I]iodobenzyl)-2'-deoxyguanosine ([(125)I]IBdG), the glycosylated analogue of the O(6)-3-iodobenzylguanine (IBG), as an agent for the in vivo mapping of the DNA repair protein alkylguanine-DNA alkyltransferase (AGT) is descr ... Full text Link to item Cite

Dosimetry and radiographic analysis of 131I-labeled anti-tenascin 81C6 murine monoclonal antibody in newly diagnosed patients with malignant gliomas: a phase II study.

Journal Article J Nucl Med · June 2005 UNLABELLED: The objective was to perform dosimetry and evaluate dose-response relationships in newly diagnosed patients with malignant brain tumors treated with direct injections of (131)I-labeled anti-tenascin murine 81C6 monoclonal antibody (mAb) into su ... Link to item Cite

Radiopharmaceutical chemistry of targeted radiotherapeutics, part 1: effects of solvent on the degradation of radiohalogenation precursors by 211At alpha-particles.

Journal Article J Nucl Med · April 2005 UNLABELLED: The high energy and short range of alpha-particles make them attractive for targeted radiotherapy. However, these properties can be problematic when the production of high activity levels of alpha-particle-emitting radiotherapeutics is required ... Link to item Cite

No-carrier-added synthesis of a 4-methyl-substituted meta-iodobenzylguanidine analogue.

Journal Article Appl Radiat Isot · March 2005 Radioiodinated meta-iodobenzylguanidine (MIBG) is used in the diagnosis and therapy of various neuroendocrine tumors. As a part of our efforts to develop an MIBG analogue with improved characteristics for these applications, a synthesis of 3-[131I]iodo-4-m ... Full text Link to item Cite

Enhanced tumour uptake of radiolabelled antibodies by hyperthermia. Part II: Application of the thermal equivalency equation.

Journal Article Int J Hyperthermia · February 2005 Clinical application of local hyperthermia as a means for modulating drug and macro-molecular tumour uptake have been slow to develop, due in part to the difficulty in designing and comparing heating protocols. The thermal isodose formula developed by Sapa ... Full text Link to item Cite

Enhanced tumour uptake of radiolabelled antibodies by hyperthermia: Part I: Timing of injection relative to hyperthermia.

Journal Article Int J Hyperthermia · February 2005 Improving drug and macromolecular delivery of anti-cancer agents to tumours results in greater efficacy without increased toxicity. The current study was undertaken to assess the effects of the timing of injection of tumour specific and non-specific monocl ... Full text Link to item Cite

Current status of therapy of solid tumors: brain tumor therapy.

Journal Article J Nucl Med · January 2005 Treatment of malignant brain tumors with conventional approaches is largely unsuccessful because curative doses generally cannot be delivered without excessive toxicity to normal brain. Radioimmunotherapy is emerging as an attractive alternative for glioma ... Link to item Cite

Radioiodine and 211At-labeled guanidinomethyl halobenzoyl octreotate conjugates: potential peptide radiotherapeutics for somatostatin receptor-positive cancers.

Journal Article Peptides · December 2004 Derivatives of the somatostatin analogues octreotide and octreotate labeled with radioiosotopes are used in the diagnosis and therapy of somatostatin receptor (SSTR)-positive tumors. A method has been devised to synthesize {N-(4-guanidinomethyl-3-iodobenzo ... Full text Link to item Cite

Radioimmunotherapy with alpha-particle emitting radionuclides.

Journal Article Q J Nucl Med Mol Imaging · December 2004 An important consideration in the development of effective strategies for radioimmunotherapy is the nature of the radiation emitted by the radionuclide. Radionuclides decaying by the emission of alpha-particles offer the possibility of matching the cell sp ... Link to item Cite

Wet harvesting of no-carrier-added 211At from an irradiated 209Bi target for radiopharmaceutical applications

Journal Article Journal of Radioanalytical and Nuclear Chemistry · December 1, 2004 Astatine-211 is one of the most promising α-emitters for targeted cancer radiotherapy. However, research and clinical trials involving 211At-labeled radiopharmaceuticals have often been impeded due to the irregular and sometimes inconveniently low recovery ... Full text Cite

A 4-methyl-substituted meta-iodobenzylguanidine analogue with prolonged retention in human neuroblastoma cells.

Journal Article Eur J Nucl Med Mol Imaging · October 2004 PURPOSE: As a part of our efforts to develop a meta-iodobenzylguanidine (MIBG) analogue with improved characteristics for the diagnosis and treatment of neuroendocrine tumours, 3-[131I]iodo-4-methyl-benzylguanidine ([131I]MeIBG) has been developed. The pur ... Full text Link to item Cite

Evaluation of an internalizing monoclonal antibody labeled using N-succinimidyl 3-[131I]iodo-4-phosphonomethylbenzoate ([131I]SIPMB), a negatively charged substituent bearing acylation agent.

Journal Article Nucl Med Biol · October 2004 Monoclonal antibodies such as L8A4, reactive with the epidermal growth factor receptor variant III, internalize after receptor binding resulting in proteolytic degradation by lysosomes. Labeling internalizing mAbs requires the use of methodologies that res ... Full text Link to item Cite

Monoclonal antibodies for brain tumour treatment.

Journal Article Expert Opin Biol Ther · September 2004 Conventional treatment of brain tumours includes surgical, radiotherapeutic and chemotherapeutic modalities. Nonetheless, the outcome of patients with brain tumours, in particular glioblastoma, remains poor. Immunotherapy with armed or unarmed monoclonal a ... Full text Link to item Cite

Catabolism of 4-fluoro-3-iodobenzylguanidine and meta-iodobenzylguanidine by SK-N-SH neuroblastoma cells.

Journal Article Nucl Med Commun · September 2004 BACKGROUND: A fluorine substituted derivative of meta-iodobenzylguanidine (MIBG), 4-fluoro-3-iodobenzylguanidine (FIBG), is retained in SK-N-SH human neuroblastoma cells in vitro to a higher degree than the MIBG. METHOD: To investigate whether the higher r ... Full text Link to item Cite

Phase 1 trial study of 131I-labeled chimeric 81C6 monoclonal antibody for the treatment of patients with non-Hodgkin lymphoma.

Journal Article Blood · August 1, 2004 We report a phase 1 study of pharmacokinetics, dosimetry, toxicity, and response of (131)I anti-tenascin chimeric 81C6 for the treatment of lymphoma. Nine patients received a dosimetric dose of 370 MBq (10 mCi). Three patients received an administered acti ... Full text Link to item Cite

An efficient targeted radiotherapy/gene therapy strategy utilising human telomerase promoters and radioastatine and harnessing radiation-mediated bystander effects.

Journal Article J Gene Med · August 2004 BACKGROUND: Targeted radiotherapy achieves malignant cell-specific concentration of radiation dosage by tumour-affinic molecules conjugated to radioactive atoms. Combining gene therapy with targeted radiotherapy is attractive because the associated cross-f ... Full text Link to item Cite

Phase I trial study of [131]I-labeled chimeric 81C6 mAb for the treatment of patients with non-Hodgkin's lymphoma

Conference EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING · August 1, 2004 Link to item Cite

Targeted radiotherapy of brain tumours.

Journal Article Br J Cancer · April 19, 2004 The utility of external beam radiotherapy for the treatment of malignant brain tumours is compromised by the need to avoid excessive radiation damage to normal CNS tissues. This review describes the current status of targeted radiotherapy, an alternative s ... Full text Open Access Link to item Cite

Human/murine chimeric 81C6 F(ab')(2) fragment: preclinical evaluation of a potential construct for the targeted radiotherapy of malignant glioma.

Journal Article Nucl Med Biol · April 2004 We have obtained encouraging responses in recent Phase I studies evaluating (131)I-labeled human/murine chimeric 81C6 anti-tenascin monoclonal antibody (ch81C6) administered into surgically-created tumor resection cavities in brain tumor patients. However, ... Full text Link to item Cite

Meta-iodobenzylguanidine derivatives containing a second guanidine moiety.

Journal Article Bioorg Med Chem · April 1, 2004 Radioiodinated meta-iodobenzylguanidine (MIBG) is used in the diagnosis and therapy of various neuroendocrine tumors. To investigate whether an additional guanidine function in the structure of MIBG will yield analogues that may potentially enhance tumor-t ... Full text Link to item Cite

O6-3-[131I]iodobenzylguanine: improved synthesis and further evaluation of a potential agent for imaging of alkylguanine-DNA alkyltransferase.

Journal Article Bioconjug Chem · 2004 O(6)-Benzylguanine derivatives with suitable radionuclides attached to the benzyl ring are potentially useful in the noninvasive imaging of the DNA repair protein, alkylguanine-DNA alkyltransferase (AGT). Previously, O(6)-3-[(131)I]iodobenzylguanine ([(131 ... Full text Link to item Cite

Imaging drug resistance with radiolabeled molecules.

Journal Article Curr Pharm Des · 2004 A major obstacle to successful cancer chemotherapy is drug resistance. Multidrug resistance (MDR) is often seen with chemotherapeutic agents such as anthracycline derivatives, vinca alkaloids and taxanes. Multiple aspects of cellular biochemistry have been ... Full text Link to item Cite

Reagents for astatination of biomolecules: comparison of the in vivo distribution and stability of some radioiodinated/astatinated benzamidyl and nido-carboranyl compounds.

Journal Article Bioconjug Chem · 2004 An investigation has been conducted to assess the in vivo stability of a series of astatinated benzamides and astatinated nido-carborane compounds in mice. It was hypothesized that the higher bond strength of boron-astatine bonds in the nido-carboranes mig ... Full text Link to item Cite

Efficacy of intracerebral microinfusion of trastuzumab in an athymic rat model of intracerebral metastatic breast cancer.

Journal Article Clin Cancer Res · November 15, 2003 PURPOSE: The monoclonal antibody (MAb) trastuzumab (Herceptin) effectively treats HER2-overexpressing extracerebral breast neoplasms. Delivery of such macromolecule therapeutic agents to intracerebral metastases, however, is limited by the tight junctions ... Link to item Cite

In vitro cytotoxicity of (211)at-astatide and (131)I-iodide to glioma tumor cells expressing the sodium/iodide symporter.

Journal Article J Nucl Med · November 2003 UNLABELLED: The sodium/iodide symporter (NIS) has been identified as an attractive target for cancer therapy. The efficacy of (131)I-iodide for NIS-expressing tumor therapy may be limited by a combination of poor cellular retention and unfavorable physical ... Link to item Cite

Progress report of a Phase I study of the intracerebral microinfusion of a recombinant chimeric protein composed of transforming growth factor (TGF)-alpha and a mutated form of the Pseudomonas exotoxin termed PE-38 (TP-38) for the treatment of malignant brain tumors.

Journal Article J Neurooncol · October 2003 TP-38 is a recombinant chimeric targeted toxin composed of the EGFR binding ligand TGF-alpha and a genetically engineered form of the Pseudomonas exotoxin, PE-38. After in vitro and in vivo animal studies that showed specific activity and defined the maxim ... Full text Link to item Cite

Targeted radiotherapy of brain tumours

Conference BRITISH JOURNAL OF CANCER · July 1, 2003 Link to item Cite

Specific and high-level targeting of radiolabeled octreotide analogues to human medulloblastoma xenografts.

Journal Article Clin Cancer Res · May 2003 PURPOSE: The objective of this study was to determine the feasibility of exploiting the overexpression of somatostatin subtype-2 receptors (sstr(2)) on human medulloblastoma cells to develop targeted radiodiagnostics and radiotherapeutics for this disease. ... Link to item Cite

N-succinimidyl 3-[211At]astato-4-guanidinomethylbenzoate: an acylation agent for labeling internalizing antibodies with alpha-particle emitting 211At.

Journal Article Nucl Med Biol · May 2003 The objective of this study was to develop a method for labeling internalizing monoclonal antibodies (mAbs) such as those reactive to the anti-epidermal growth factor receptor variant III (EGFRvIII) with the alpha-particle emitting radionuclide (211)At. Ba ... Full text Link to item Cite

Microdosimetric analysis of alpha-particle-emitting targeted radiotherapeutics using histological images.

Journal Article J Nucl Med · May 2003 UNLABELLED: The purpose of this study was to evaluate the therapeutic efficacy and limitations of alpha-particle-emitting radiolabeled compounds by means of 2-dimensional histological images and distribution of activity on a microscopic level. METHODS: A m ... Link to item Cite

Optimizing methods for labeling biomolecules with astatine-211.

Conference ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY · March 1, 2003 Link to item Cite

Evaluation of astatine-211 labeled targeted radiotherapeutics.

Conference ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY · March 1, 2003 Link to item Cite

N-succinimidyl 3-[(131)I]iodo-4-phosphonomethylbenzoate ([(131)I]SIPMB), a negatively charged substituent-bearing acylation agent for the radioiodination of peptides and mAbs.

Journal Article Bioconjug Chem · 2003 An important criterion in design of acylation agents for the radioiodination of internalizing monoclonal antibodies (mAbs) is to maximize the retention of radioiodine in the tumor following mAb intracellular processing. We have previously shown that labeli ... Full text Link to item Cite

Vascular targeted endoradiotherapy of tumors using alpha-particle-emitting compounds: theoretical analysis.

Journal Article Int J Radiat Oncol Biol Phys · November 15, 2002 PURPOSE: To establish the theoretical framework and study the feasibility of (211)At-labeled anti-tenascin chimeric 81C6 monoclonal antibody (mAb) as anti-vascular endoradiotherapy for the treatment of glioblastoma multiforme (GBM) tumors. METHODS AND MATE ... Full text Link to item Cite

Sodium-iodide symporter (NIS)-mediated accumulation of [(211)At]astatide in NIS-transfected human cancer cells.

Journal Article Nucl Med Biol · October 2002 The cellular expression of the sodium iodide symporter (NIS) has been shown to confer iodide-concentrating capacity in non-thyroid cell types. We examined the role of NIS in the uptake of the alpha-particle emitting radiohalide [(211)At]astatide in the UVW ... Full text Link to item Cite

Phase II Trial of Murine 131I-Labeled Antitenascin Monoclonal Antibody 81C6 Administered Into Surgically Created Resection Cavities of Patients With Newly Diagnosed Malignant Gliomas

Journal Article Journal of Clinical Oncology · March 1, 2002 PURPOSE: To assess the efficacy and toxicity of intraresection cavity 131I-labeled murine antitenascin monoclonal antibody 81C6 and determine its true response rate among patients with newly diagnosed malignant glioma. Full text Cite

Phase II trial of murine (131)I-labeled antitenascin monoclonal antibody 81C6 administered into surgically created resection cavities of patients with newly diagnosed malignant gliomas.

Journal Article J Clin Oncol · March 1, 2002 PURPOSE: To assess the efficacy and toxicity of intraresection cavity (131)I-labeled murine antitenascin monoclonal antibody 81C6 and determine its true response rate among patients with newly diagnosed malignant glioma. PATIENTS AND METHODS: In this phase ... Full text Link to item Cite

Improved xenograft targeting of tumor-specific anti-epidermal growth factor receptor variant III antibody labeled using N-succinimidyl 4-guanidinomethyl-3-iodobenzoate.

Journal Article Nucl Med Biol · January 2002 Monoclonal antibodies (mAbs) such as the tumor-specific anti-epidermal growth factor receptor variant III (EGFRvIII) that are internalized and degraded after cell binding necessitate the use of radioiodination methods that minimize the loss of radioactivit ... Full text Link to item Cite

Imaging of pheochromocytoma in 2 dogs using p-[18F] fluorobenzylguanidine.

Journal Article Vet Radiol Ultrasound · 2002 p-[18F]Fluorobenzylguanidine ([18F]PFBG) is a norepinephrine analog that has been developed as a positron emission tomography (PET) imaging radiopharmaceutical. Myocardial sympathetic innervation, neuroendocrine structures, and tumors can be noninvasively ... Full text Link to item Cite

Positively charged templates for labeling internalizing antibodies: comparison of N-succinimidyl 5-iodo-3-pyridinecarboxylate and the D-amino acid peptide KRYRR.

Journal Article Nucl Med Biol · October 2001 Receptor-mediated internalization of monoclonal antibodies (mAbs), such as those specific for the epidermal growth factor receptor variant III (EGFRvIII), can lead to rapid loss of radioactivity from the target cell. In the current study, the anti-EGFRvIII ... Full text Link to item Cite

High-level production of alpha-particle-emitting (211)At and preparation of (211)At-labeled antibodies for clinical use.

Journal Article J Nucl Med · October 2001 UNLABELLED: In vitro and in vivo studies in human glioma models suggest that the antitenascin monoclonal antibody 81C6 labeled with the 7.2-h-half-life alpha-particle emitter (211)At might be a valuable endoradiotherapeutic agent for the treatment of brain ... Link to item Cite

Long term response in a patient with neoplastic meningitis secondary to melanoma treated with (131)I-radiolabeled antichondroitin proteoglycan sulfate Mel-14 F(ab')(2): a case study.

Journal Article Cancer · May 1, 2001 Even with novel chemotherapeutic agents and external beam radiation therapy, the prognosis of neoplastic meningitis secondary to malignant melanoma is still dismal. The authors report a case study of a 46-year-old white female who presented with progressiv ... Link to item Cite

Targeting a genetically engineered elastin-like polypeptide to solid tumors by local hyperthermia.

Journal Article Cancer Res · February 15, 2001 Elastin-like polypeptides (ELPs) are biopolymers of the pentapeptide repeat Val-Pro-Gly-Xaa-Gly that undergo an inverse temperature phase transition. They are soluble in aqueous solutions below their transition temperature (T1) but hydrophobically collapse ... Link to item Cite

Biological evaluation of ring- and side-chain-substituted m-iodobenzylguanidine analogues.

Journal Article Bioconjug Chem · 2001 A number of ring- and side-chain-substituted m-iodobenzylguanidine analogues were evaluated for their lipophilicity, in vitro stability, uptake by SK-N-SH human neuroblastoma cells in vitro, and biodistribution in normal mice. As expected, the lipophilicit ... Full text Link to item Cite

A polar substituent-containing acylation agent for the radioiodination of internalizing monoclonal antibodies: N-succinimidyl 4-guanidinomethyl-3-[131I]iodobenzoate ([131I]SGMIB).

Journal Article Bioconjug Chem · 2001 The objective of this study was to develop an acylation agent for the radioiodination of monoclonal antibodies that would maximize retention of the label in tumor cells following receptor- or antigen-mediated internalization. The strategy taken was to add ... Full text Link to item Cite

Synthesis of ring- and side-chain-substituted m-iodobenzylguanidine analogues.

Journal Article Bioconjug Chem · 2001 With the goal of developing MIBG analogues with improved targeting properties especially for oncologic applications, several radioiodinated ring- and side-chain-substituted MIBG analogues were synthesized. Except for 3-[(131)I]iodo-4-nitrobenzylguanidine a ... Full text Link to item Cite

Increased binding affinity enhances targeting of glioma xenografts by EGFRvIII-specific scFv.

Journal Article Int J Cancer · December 15, 2000 Combinatorial variation of CDR3 of V(H) and V(L), followed by phage display, was used to select affinity mutants of the parental anti-epidermal growth factor receptor-vIII (EGFRvIII) scFv MR1. One mutant, MR1-1(scFv), had increased specific binding affinit ... Full text Link to item Cite

Phase I trial results of iodine-131-labeled antitenascin monoclonal antibody 81C6 treatment of patients with newly diagnosed malignant gliomas.

Journal Article J Clin Oncol · November 15, 2000 PURPOSE: To determine the maximum-tolerated dose (MTD) of iodine-131 ((131)I)-labeled 81C6 antitenascin monoclonal antibody (mAb) administered clinically into surgically created resection cavities (SCRCs) in malignant glioma patients and to identify any ob ... Full text Link to item Cite

Astatine-211-labeled radiotherapeutics: an emerging approach to targeted alpha-particle radiotherapy.

Journal Article Curr Pharm Des · September 2000 Targeted radiotherapy or endoradiotherapy is an appealing approach to cancer treatment because of the potential for delivering curative doses of radiation to tumor while sparing normal tissues. Radionuclides that decay by the emission of alpha-particles su ... Full text Link to item Cite

Dosimetry and microdosimetry of targeted radiotherapy.

Journal Article Curr Pharm Des · September 2000 Dosimetry in targeted radiotherapy (TR) uses different calculation methods, whose degree of refinement is closely conditioned by the particular objective sought. It is more generally performed to establish a correlation between the quantity of radiation de ... Full text Link to item Cite

Radioiodination via D-amino acid peptide enhances cellular retention and tumor xenograft targeting of an internalizing anti-epidermal growth factor receptor variant III monoclonal antibody.

Journal Article Cancer Res · August 15, 2000 The mutant epidermal growth factor receptor variant III (EGFRvIII) has been found on gliomas and other tumors but not on normal tissues, including those that express the wild-type receptor. Monoclonal antibodies (mAbs) specific for EGFRvIII are rapidly int ... Link to item Cite

Exposure of human osteosarcoma and bone marrow cells to tumour-targeted alpha-particles and gamma-irradiation: analysis of cell survival and microdosimetry.

Journal Article Int J Radiat Biol · August 2000 PURPOSE: This study was designed to compare the cytotoxic effects of an alpha-emitting radioimmunoconjugate, which binds to osteosarcoma but not to bone marrow cells, with those of external gamma-irradiation. MATERIALS AND METHODS: The human osteosarcoma c ... Full text Link to item Cite

Synergistic interaction between anti-p185HER-2 ricin A chain immunotoxins and radionuclide conjugates for inhibiting growth of ovarian and breast cancer cells that overexpress HER-2.

Journal Article Clin Cancer Res · August 2000 Radionuclide conjugates or ricin A chain (RTA) immunotoxins that target pl85HER-2 have partially inhibited the growth of human ovarian cancer xenografts in athymic mice but generally have not cured mice bearing human tumor transplants. The present study wa ... Link to item Cite

Radioiodination and astatination of octreotide by conjugation labeling.

Journal Article Nucl Med Biol · May 2000 Octreotide was coupled to 3-iodobenzoyl and 3-iodonicotinoyl moieties to obtain [N-(3-iodobenzoyl)-D-Phe(1)]octreotide (IBO) and [N-(3-iodonicotinoyl)-D-Phe(1)]octreotide (INO), respectively. The IC(50) values for the binding of IBO and INO to CA20948 rat ... Full text Link to item Cite

Genetically engineered biopolymer conjugate for thermal targeting of anticancer therapeutics.

Journal Article ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY · March 26, 2000 Link to item Cite

Genetically engineered polypeptide carrier for thermal targeting of anticancer therapeutics

Journal Article American Chemical Society, Polymer Preprints, Division of Polymer Chemistry · March 1, 2000 The thermally-responsive carrier, an elastin-like polypeptide (ELP), is an oligomer of a Val-Pro-Gly-Xaa-Gly pentapeptide repeat. Below a specific, inverse phase transition temperature (Tt), ELPs are highly soluble in aqueous solution. However, upon raisin ... Cite

Dosimetry and dose-response relationships in newly diagnosed patients with malignant gliomas treated with iodine-131-labeled anti-tenascin monoclonal antibody 81C6 therapy.

Journal Article Int J Radiat Oncol Biol Phys · March 1, 2000 PURPOSE: The objective of this study was to perform the dosimetry and evaluate the dose-response relationships in newly diagnosed patients with malignant brain tumors treated by direct injections of (131)I-labeled 81C6 monoclonal antibody (MAb) into surgic ... Full text Link to item Cite

Radioiodination and astatination of octreotide by conjugation labeling

Journal Article Journal of Inorganic Biochemistry · February 29, 2000 Octreotide was coupled to 3-iodobenzoyl and 3-iodonicotinoyl moieties to obtain [N-(3-iodobenzoyl)-D-Phe1]octreotide (IBO) and [N-(3-iodonicotinoyl)-D-Phe1]octreotide (INO), respectively. The IC50 values for the binding of IBO and INO to CA20948 rat pancre ... Cite

Radiohalogens for radioimmunotherapy

Chapter · January 1, 2000 The selective delivery of cytotoxic radionuclides to malignant cell populations is the central objective of radioimmunotherapy. The impact of radioimmunotherapy on the clinical management of cancer has generally been limited, particularly for the treatment ... Cite

Radiolabeled guanine derivatives for the in vivo mapping of O(6)-alkylguanine-DNA alkyltransferase: 6-(4-[(18)F]Fluoro-benzyloxy)-9H-purin-2-ylamine and 6-(3-[(131)I]Iodo-benzyloxy)-9H-purin-2-ylamine.

Journal Article Bioconjug Chem · 2000 Two radiolabeled analogues of 6-benzyloxy-9H-purin-2-ylamine (O(6)-benzylguanine; BG) potentially useful in the in vivo mapping of O(6)-alkylguanine-DNA alkyltransferase (AGT) were synthesized. Fluorine-18 labeling of the known 6-(4-fluoro-benzyloxy)-9H-pu ... Full text Link to item Cite

Radioiodinated antibody targeting of the HER-2/neu oncoprotein: effects of labeling method on cellular processing and tissue distribution.

Journal Article Nucl Med Biol · October 1999 Monoclonal antibody (MAb) internalization can have a major effect on tumor retention of radiolabel. Two anti-HER-2/neu MAbs (TA1 and 520C9) were radioiodinated using the iodogen, N-succinimidyl 5-iodo-3-pyridinecarboxylate (SIPC), and tyramine-cellobiose ( ... Full text Link to item Cite

Radiotoxicity of systemically administered 211At-labeled human/mouse chimeric monoclonal antibody: a long-term survival study with histologic analysis.

Journal Article Int J Radiat Oncol Biol Phys · September 1, 1999 PURPOSE: The antitenascin human/mouse chimeric monoclonal antibody labeled with the alpha-particle-emitting radionuclide 211At is of interest as an endoradiotherapeutic agent for the treatment of brain tumors. To facilitate the investigation of 211At-label ... Full text Link to item Cite

211At- and 131I-labeled bisphosphonates with high in vivo stability and bone accumulation.

Journal Article J Nucl Med · July 1999 UNLABELLED: Bisphosphonates were synthesized for use as carriers for astatine and iodine radioisotopes to target bone neoplasms. METHODS: Radiohalogenated activated esters were coupled to the amino group in the side chain of the bisphosphonate. The bisphos ... Link to item Cite

125I-labeled anti-epidermal growth factor receptor-vIII single-chain Fv exhibits specific and high-level targeting of glioma xenografts.

Journal Article Clin Cancer Res · June 1999 A single-chain antibody fragment, MR1(scFv), with specific binding to epidermal growth factor receptor-vIII (EGFRvIII), was produced, radiolabeled, and evaluated for biodistribution in human glioma-bearing athymic mice. The mutant receptor EGFRvIII has a d ... Link to item Cite

Astatine-211 labeling of internalizing anti-EGFRvIII monoclonal antibody using N-succinimidyl 5-[211At]astato-3-pyridinecarboxylate.

Journal Article Nucl Med Biol · May 1999 Monoclonal antibodies (MAbs) such as the anti-epidermal growth factor variant III (EGFRvIII) MAb L8A4 are rapidly internalized, which can lead to rapid loss of radioactivity from the tumor cell. The aim of this study was to evaluate the potential utility o ... Full text Link to item Cite

Synthesis, purification, and in vitro stability of 211At- and 125I-labeled amidobisphosphonates.

Journal Article Nucl Med Biol · May 1999 A method is described for preparing 211At- and radioiodinated amidobisphosphonates. The active esters N-succinimidyl 3-(tri-methylstannyl) benzoate (ATE) and N-succinimidyl 5-(tri-methylstannyl)-3-pyridinecarboxylate (SPC) were used as precursors. The isol ... Full text Link to item Cite

Dosimetry of 131I-labeled 81C6 monoclonal antibody administered into surgically created resection cavities in patients with malignant brain tumors.

Journal Article J Nucl Med · April 1999 UNLABELLED: The objective of this study was to perform the dosimetry of 131I-labeled 81C6 monoclonal antibody (MAb) in patients with recurrent malignant brain tumors, treated by direct injections of MAb into surgically created resection cavities (SCRCs). M ... Link to item Cite

Low molecular weight radiopharmaceuticals: Radiohalogenated MIBG and IUdR analogues.

Journal Article ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY · March 21, 1999 Link to item Cite

Preparation and characterization of anti-tenascin monoclonal antibody-streptavidin conjugates for pretargeting applications.

Journal Article Bioconjug Chem · 1999 Radioimmunopretargeting is based on the separate injection of a modified mAb and the radionuclide and most frequently exploits the very high avidity of biotin for streptavidin (SA). Currently, we are evaluating the therapeutic potential of directly labeled ... Full text Link to item Cite

Radioiodinated D-peptides as prosthetic groups for radiolabeling internalizing antibodies

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · January 1, 1999 Cite

211At- and 131I-labeled bisphosphonates with high in vivo stability and bone accumulation

Journal Article Journal of Nuclear Medicine · 1999 Bisphosphonates were synthesized for use as carriers for astatine and iodine radioisotopes to target bone neoplasms. Methods: Radiohalogenated activated esters were coupled to the amino group in the side chain of the bisphosphonate. The bisphosphonate 3-am ... Cite

125I-labeled anti-epidermal growth factor receptor-vIII single-chain Fv exhibits specific and high-level targeting of glioma xenografts

Journal Article Clinical Cancer Research · 1999 A single-chain antibody fragment, MR1(scFv), with specific binding to epidermal growth factor receptor-vIII (EGFRvIII), was produced, radiolabeled, and evaluated for biodistribution in human glioma-bearing athymic mice. The mutant receptor EGFRvIII has a d ... Cite

Octreotide analogues labeled with radioiodine and astatine-211

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · January 1, 1999 Cite

Human IgG2 constant region enhances in vivo stability of anti-tenascin antibody 81C6 compared with its murine parent.

Journal Article Clin Cancer Res · October 1998 The in vivo properties of radiolabeled chimeric monoclonal antibodies (mAbs) with human IgG1 and IgG3 constant regions generally are similar to those of their corresponding murine construct. In contrast, we have observed that chimeric anti-tenascin mAb 81C ... Link to item Cite

Survival and DNA damage in Chinese hamster V79 cells exposed to alpha particles emitted by DNA-incorporated astatine-211.

Journal Article Radiat Res · September 1998 Asynchronous Chinese hamster V79 lung fibroblasts were incubated at 37 degrees C for 30 min with the thymidine analog 5-[211At]astato-2'-deoxyuridine (211AtdU, exposure from DNA-incorporated activity) or with [211At]astatide (211At-, exposure from extracel ... Link to item Cite

The effects of local hyperthermia on the catabolism of a radioiodinated chimeric monoclonal antibody.

Journal Article Clin Cancer Res · September 1998 Local hyperthermia has been shown to increase the tumor uptake and tumor:normal tissue ratios of radiolabeled monoclonal antibodies (mAbs) in athymic mouse xenograft models. The current study was undertaken to determine whether this behavior was related in ... Link to item Cite

Preparation of 5-[131I]iodo- and 5-[211At]astato-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) uracil by a halodestannylation reaction.

Journal Article Nucl Med Biol · July 1998 To circumvent the in vivo instability of 5-iodo-2'-deoxyuridine (IUdR), a 2'-fluorine-substituted analogue, 5-iodo-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil (FIAU) recently has been introduced. To facilitate the preparation of radioiodinated FIAU ... Full text Link to item Cite

Toxicity to neuroblastoma cells and spheroids of benzylguanidine conjugated to radionuclides with short-range emissions.

Journal Article Br J Cancer · June 1998 Radiolabelled meta-iodobenzylguanidine (MIBG) is selectively taken up by tumours of neuroendocrine origin, where its cellular localization is believed to be cytoplasmic. The radiopharmaceutical [131I]MIBG is now widely used in the treatment of neuroblastom ... Full text Open Access Link to item Cite

Iodine-131-labeled antitenascin monoclonal antibody 81C6 treatment of patients with recurrent malignant gliomas: phase I trial results.

Journal Article J Clin Oncol · June 1998 PURPOSE: To determine the maximum-tolerated dose (MTD) of iodine 131 (131I)-labeled 81C6 monoclonal antibody (mAb) in brain tumor patients with surgically created resection cavities (SCRCs) and to identify any objective responses to this treatment. METHODS ... Full text Link to item Cite

Blocking [211At]astatide accumulation in normal tissues: preliminary evaluation of seven potential compounds.

Journal Article Nucl Med Biol · May 1998 Normal tissue accumulation of 211At must be minimized during targeted radiotherapy with 211At-labeled compounds. Therefore, we investigated the ability of seven compounds to block normal organ uptake of [211At]astatide in mice: potassium iodide, sodium thi ... Full text Link to item Cite

Targeted therapy using astatinated radiopharmaceuticals.

Journal Article ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY · April 2, 1998 Link to item Cite

The class III variant of the epidermal growth factor receptor (EGFRvIII): characterization and utilization as an immunotherapeutic target.

Journal Article J Neurovirol · April 1998 Any immunotherapeutic approach to cancer cell eradication is based upon the specific recognition of neoplastic cells and the sparing of surrounding normal tissue; perhaps nowhere is this distinction more important than within the central nervous system, du ... Full text Link to item Cite

Cytotoxicity of alpha-particle-emitting astatine-211-labelled antibody in tumour spheroids: no effect of hyperthermia.

Journal Article Br J Cancer · March 1998 The high linear energy transfer, alpha-particle-emitting radionuclide astatine-211 (211At) is of interest for certain therapeutic applications; however, because of the 55- to 70-microm path length of its alpha-particles, achieving homogeneous tracer distri ... Full text Open Access Link to item Cite

The cytotoxicity and microdosimetry of astatine-211-labeled chimeric monoclonal antibodies in human glioma and melanoma cells in vitro.

Journal Article Radiat Res · February 1998 The cytotoxicity of alpha-particle-emitting endoradiotherapeutic compounds is of increasing interest because clinical evaluation of these potential therapeutic agents is commencing. Astatine-211 is a radionuclide with a 7.2-h half-life that emits 5.87 and ... Link to item Cite

Astatine-211-labeled biotin conjugates resistant to biotinidase for use in pretargeted radioimmunotherapy.

Journal Article Nucl Med Biol · February 1998 We report herein the preparation and biological evaluation of two radioastatinated biotin conjugates, (3-[211At]astatobenzoyl)norbiotinamide and ((5-[211At]astato-3-pyridinyl)carbonyl)norbiotinamide. Both conjugates were stable in the presence of human ser ... Full text Link to item Cite

Effects of specific activity on meta-[(131)I]iodobenzylguanidine kinetics in isolated rat heart.

Journal Article Nucl Med Biol · January 1998 The effects of specific activity of meta-[(131)I]iodobenzylguanidine (MIBG) were studied in uptake-2 blocked isolated perfused rat heart. [(131)I]MIBG was administered in the perfusate as an 8-min pulse, followed by an 80-min washout period. Kinetic analys ... Full text Link to item Cite

Iodopyridine-for-iodobenzene substitution for use with low molecular weight radiopharmaceuticals: application to m-iodobenzylguanidine.

Journal Article Bioconjug Chem · 1998 Substituting a pyridine ring for a benzene ring in the acylation agent N-succinimidyl 3-iodobenzoate has resulted in a useful approach for the radiohalogenation of monoclonal antibodies, peptides, and labeled biotin conjugates. It was hypothesized that suc ... Full text Link to item Cite

Microdosimetry of astatine-211 using histological images: application to bone marrow.

Journal Article Radiat Res · December 1997 A method is presented for calculating the small-scale dosimetry of 211At in red bone marrow using chord-length distributions obtained from digitized histological images. This study used histological samples of bone marrow from beagle dogs to convey morphol ... Link to item Cite

In vitro and in vivo behavior of radiolabeled chimeric anti-EGFRvIII monoclonal antibody: comparison with its murine parent.

Journal Article Nucl Med Biol · October 1997 The mutant version of the epidermal growth factor receptor EGFRvIII has been found on gliomas and other tumors, but not on normal tissues. Radioiodinated murine (mu) L8A4 monoclonal antibody (MAb) specifically targets EGFRvIII xenografts in vivo when label ... Full text Link to item Cite

Cytotoxicity of alpha-particle-emitting 5-[211At]astato-2'-deoxyuridine in human cancer cells.

Journal Article Int J Radiat Biol · July 1997 This study was performed to determine the cytotoxicity of alpha-particle-emitting 5-[211At]astato-2-deoxyuridine (i.e. [211At]AUdR) for monolayers of D-247 MG human glioma cells and SK-MEL-28 human melanoma cells. Cells in exponential growth were exposed t ... Full text Link to item Cite

A New Route to Guanidines from Bromoalkanes

Journal Article The Journal of Organic Chemistry · July 1, 1997 Full text Cite

Radioiodinated antibody targeting of the HER-2/neu oncoprotein.

Journal Article Nucl Med Biol · July 1997 The HER-2/neu oncogene encodes a 185 kDa phosphoglycoprotein that is overexpressed in breast, ovarian and other cancers. Seven monoclonal antibodies reactive with oncoprotein were labeled with 131I. In vitro experiments with SKOv3 9002-18 cells determined ... Full text Link to item Cite

Growth factor receptors as molecular targets for cancer diagnosis and therapy.

Journal Article Q J Nucl Med · June 1997 Growth factor receptors are of great interest as molecular targets for the diagnosis and treatment of cancer. Growth factor receptors are frequently over expressed on malignant cell populations since many cellular oncogenes encode either growth factors or ... Link to item Cite

A method for labeling internalizing antibodies with astatine-211.

Journal Article JOURNAL OF NUCLEAR MEDICINE · May 1, 1997 Link to item Cite

Improved targeting of an anti-epidermal growth factor receptor variant III monoclonal antibody in tumor xenografts after labeling using N-succinimidyl 5-iodo-3-pyridinecarboxylate.

Journal Article Cancer Res · April 15, 1997 Monoclonal antibody (mAb) L8A4, specific for the tumor-associated mutant epidermal growth factor receptor variant III (EGFRvII), is internalized and degraded after cell binding. Four paired-label experiments were performed in athymic mice bearing EGFRvIII- ... Link to item Cite

Tissue distribution and radiation dosimetry of astatine-211-labeled chimeric 81C6, an alpha-particle-emitting immunoconjugate.

Journal Article Nucl Med Biol · April 1997 A paired-label study was performed in athymic mice bearing subcutaneous D-54 MG human glioma xenografts to compare the localization of human/mouse anti-tenascin chimeric antibody 81C6 labeled by reaction with N-succinimidyl 3-[211At]astatobenzoate and N-su ... Full text Link to item Cite

Fluorine-18-labeled [Nle4,D-Phe7]-alpha-MSH, an alpha-melanocyte stimulating hormone analogue.

Journal Article Nucl Med Biol · February 1997 The alpha-melanocyte stimulating hormone (alpha-MSH) analogue [Nle4,D-Phe7]-alpha-MSH was labeled with 18F using N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) in > 80% radiochemical yield. The IC50 values of [Nle4,D-Phe7]-alpha-MSH and para-fluorobenzoyl ... Full text Link to item Cite

No-carrier-added iodine-131-FIBG: evaluation of an MIBG analog.

Journal Article J Nucl Med · February 1997 UNLABELLED: The purpose of this study was to evaluate the properties of 4-fluoro-3-[131I]iodobenzylguanidine ([131I]FIBG), a potential neuroendocrine tumor and myocardial imaging radiopharmaceutical. METHODS: The binding of [131I]FIBG and [125I]MIBG was co ... Link to item Cite

Preparation and biological evaluation of an astatine-211 labeled biotin conjugate: biotinyl-3-[211 At]astatoanilide.

Journal Article Nucl Med Biol · February 1997 Biotinyl-3-[211 At]astatoanilide ([211 At]AtBA) was prepared in more than 80% yield by destannylation. In vitro, [211 At]AtBA exhibited a high affinity for streptavidin, and was stable after incubation in human serum, cerebrospinal fluid and distilled wate ... Full text Link to item Cite

3-[211At]astato-4-fluorobenzylguanidine: a potential therapeutic agent with prolonged retention by neuroblastoma cells.

Journal Article Br J Cancer · 1997 An analogue of meta-iodobenzylguanidine (MIBG) in which an aromatic hydrogen was replaced with fluorine has been found to possess many properties similar to those of the parent compound. Moreover, 4-fluoro-3-iodobenzylguanidine (FIBG) was retained in vitro ... Full text Open Access Link to item Cite

Method for radioiodination of proteins using N-succinimidyl 3-hydroxy-4-iodobenzoate.

Journal Article Bioconjug Chem · 1997 A conjugation method has been developed for the radioiodination of proteins which should be adaptable to kit formulation. m-Hydroxybenzoic acid was converted to 3-hydroxy-4-[131I]iodobenzoic acid in 65% radiochemical yield using Chloramine-T as the oxidant ... Full text Link to item Cite

Local hyperthermia improves uptake of a chimeric monoclonal antibody in a subcutaneous xenograft model.

Journal Article Clin Cancer Res · January 1997 This study was undertaken to determine the effect of local hyperthermia on the tissue distribution of a chimeric human/mouse IgG2 monoclonal antibody, 81C6, reactive with the extracellular matrix protein tenascin, which is expressed at high levels in gliom ... Link to item Cite

A local hyperthermia treatment which enhances antibody uptake in a glioma xenograft model does not affect tumour interstitial fluid pressure.

Journal Article Int J Hyperthermia · 1997 Solid tumours have an elevated interstitial fluid pressure (IFP) due to the lack of normal lymphatics, increased permeability of tumour vasculature and an expanding cell population within a potentially limited space. This elevated IFP has been proposed to ... Full text Link to item Cite

Synthesis and preliminary biological evaluation of (3-iodobenzoyl)norbiotinamide and ((5-iodo-3-pyridinyl)carbonyl)norbiotinamide: two radioiodinated biotin conjugates with improved stability.

Journal Article Bioconjug Chem · 1997 A new class of radioiodinated biotin conjugated is described in which the amido bond between biotin and the labeled prosthetic group is reversed. One conjugate, (3-[125I]iodobenzoyl)norbiotinamide (4c, [125I]IBB) was labeled with Na125I in one step from (3 ... Full text Link to item Cite

Uptake and retention kinetics of para-fluorine-18-fluorobenzylguanidine in isolated rat heart.

Journal Article J Nucl Med · December 1996 UNLABELLED: Para-[18F]fluorobenzylguanidine ([18F]PFBG) is a newly developed tracer for imaging myocardial sympathetic neuronal innervation. This study investigated the uptake and retention mechanisms of [18F]PFBG in perfused, isolated rat heart. METHODS: ... Link to item Cite

Radioiodination of internalizing monoclonal antibodies using N-succinimidyl 5-iodo-3-pyridinecarboxylate.

Journal Article Cancer Res · November 1, 1996 Monoclonal antibodies (mAbs) that internalize following binding to cell-surface receptors require radiolabeling approaches that minimize loss of radioactivity from the cell after intracellular processing. One class of internalizing mAbs of great interest f ... Link to item Cite

Targeted therapy using alpha emitters.

Journal Article Phys Med Biol · October 1996 Radionuclides such as 211At and 212Bi which decay by the emission of alpha-particles are attractive for certain applications of targeted radiotherapy. The tissue penetration of 212Bi and 211At alpha-particles is equivalent to only a few cell diameters, off ... Full text Link to item Cite

A method for the radiohalogenation of internalizing antibodies.

Journal Article JOURNAL OF NUCLEAR MEDICINE · October 1, 1996 Link to item Cite

Evaluation of meta-[211At]astatobenzylguanidine in an athymic mouse human neuroblastoma xenograft model.

Journal Article Nucl Med Biol · August 1996 A paired-label biodistribution was performed in athymic mice bearing SK-N-SH human neuroblastoma xenografts to compare the tissue uptake of meta-[211At]astatobenzylguanidine ([211At]MABG) and [131I]MIBG. Significantly higher (p < 0.05) uptake of [211At]MAB ... Full text Link to item Cite

Intrathecal 131I-labeled antitenascin monoclonal antibody 81C6 treatment of patients with leptomeningeal neoplasms or primary brain tumor resection cavities with subarachnoid communication: phase I trial results.

Journal Article Clin Cancer Res · June 1996 We aimed to determine the maximum tolerated dose (MTD) of 131I-labeled 81C6 in patients with leptomeningeal neoplasms or brain tumor resection cavities with subarachnoid communication and to identify any objective responses. 81C6 is a murine IgG monoclonal ... Link to item Cite

The effects of clinically relevant hyperthermic temperatures on the kinetic binding parameters of a monoclonal antibody.

Journal Article Nucl Med Biol · May 1996 Hyperthermia is a therapeutic modality under investigation for its ability to increase absolute levels of tumor uptake of radiolabeled monoclonal antibodies (MAbs). We have investigated whether hyperthermia may affect the binding parameters of MAbs. The ef ... Full text Link to item Cite

Localisation of [131I]MIBG in nude mice bearing SK-N-SH human neuroblastoma xenografts: effect of specific activity.

Journal Article Br J Cancer · May 1996 The biodistribution of no-carrier-added (n.c.a.) meta-[131I]iodobenzylguanidine ([131I]MIBG) and that prepared by the standard isotopic exchange method were compared in athymic mice bearing SK-N-SH human neuroblastoma xenografts. No advantage in tumour upt ... Full text Open Access Link to item Cite

Chimeric anti-tenascin antibody 81C6: increased tumor localization compared with its murine parent.

Journal Article Nucl Med Biol · May 1996 When labeled using the Iodogen method, a chimeric antibody composed of the human IgG2 constant region and the variable regions of murine anti-tenascin 81C6 exhibited superior uptake in human glioma xenografts compared with its murine parent. In the current ... Full text Link to item Cite

Radiotoxicity of systematically administered [211At]astatide in B6C3F1 and BALB/c (nu/nu) mice: a long-term survival study with histologic analysis.

Journal Article Int J Radiat Oncol Biol Phys · April 1, 1996 PURPOSE: The present study undertook to establish the dose (LD) of systematically administered (via tail vein) sodium [211At]astatide that would kill 10% (LD10) of exposed animals in two mouse models and to evaluate the resulting histologic lesions. METHOD ... Full text Link to item Cite

5-[211 At]astato-2'-deoxyuridine, an alpha particle-emitting endoradiotherapeutic agent undergoing DNA incorporation.

Journal Article Cancer Res · March 15, 1996 When labeled with the subcellular range Auger electron emitters 125I and 123I, the thymidine analogue 5-iodo-2'deoxyuridine (IUdR) is highly cytotoxic but only to cells going through S-phase during exposure to these radiopharmaceuticals. Since 211 At emits ... Link to item Cite

Particle-emitting endoradiotherapeutic agent undergoing DNA incorporation

Journal Article Cancer Research · March 15, 1996 When labeled with the subcellular range Auger electron emitters 125I and 123I, the thymidine analogue 5-iodo-2′-deoxyuridine (IUdR) is highly cytotoxic but only to cells going through S-phase during exposure to these radiopharmaceuticals. Since 211At emits ... Cite

Evaluation of an internal cyclotron target for the production of 211At via the 209Bi (alpha,2n)211 at reaction.

Journal Article Appl Radiat Isot · February 1996 Astatine-211 is a 7.2 h half-life alpha-emitting radionuclide which has shown great promise for targeted radiotherapy. It is generally produced by cyclotron bombardment of bismuth metal targets with 28 MeV alpha-particles via the 209Bi(alpha,2n)211 At reac ... Full text Link to item Cite

No-carrier-added (4-fluoro-3-[131I]iodobenzyl)guanidine and (3-[211At]astato-4-fluorobenzyl)guanidine.

Journal Article Bioconjug Chem · 1996 With 3-bromo-4-fluorotoluene as starting material, [4-fluoro-3-(trimethylsilyl)benzyl]guanidine was prepared in five steps in 1.5% overall yield. Radioiodination of this silicon precursor using N-chlorosuccinimide in trifluoroacetic acid at room temperatur ... Full text Link to item Cite

Labeling of Monoclonal Antibodies (MAbs) with N-Succinimidyl 3-hydroxy-4-[131I]iodobenzoate (mSHIB)

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · 1996 Cite

Radioimmunotherapy with alpha-particle emitting radioimmunoconjugates.

Journal Article Acta Oncol · 1996 Radionuclides which decay by the emission of alpha-particles are attractive for certain radioimmunotherapeutic applications. These include the treatment of lymphomas, compartmentally spread malignancies such as ovarian cancer and neoplastic meningitis, and ... Full text Link to item Cite

Catabolism of Label from an F(ab')2 Fragment Radioiodinated Using N-Succinimidyl 3-iodobenzoate and Iodogen Methods

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · 1996 Cite

Abundant tyrosine residues in the antigen binding site in anti-osteosarcoma monoclonal antibodies TP-1 and TP-3: Application to radiolabeling.

Journal Article Acta Oncol · 1996 The variable (V) genes of TP-1 and TP-3 MAbs have been cloned and sequenced. Because of the potential use of these antibodies in the diagnosis and treatment of osteosarcoma, it is important to determine the presence and position of amino acid residues that ... Full text Link to item Cite

Enhanced binding and inertness to dehalogenation of alpha-melanotropic peptides labeled using N-succinimidyl 3-iodobenzoate.

Journal Article Bioconjug Chem · 1996 Two peptides of potential utility for targeting melanoma cells, alpha-melanocyte-stimulating hormone (alpha-MSH) and its more potent analogue [Nle4,D-Phe7]-alpha-MSH, were radioiodinated in 45-65% yield using N-succinimidyl 3-[125I]iodobenzoate (SIB). To d ... Full text Link to item Cite

Evaluation of an internal cyclotron target for the production of 211at via the 209Bi (α,2n)211at reaction

Journal Article Applied Radiation and Isotopes · 1996 Astatine-211 is a 7.2 h half-life α-emitting radionuclide which has shown great promise for targeted radiotherapy. It is generally produced by cyclotron bombardment of bismuth metal targets with 28 MeV α-particles via the 209Bi(α, 2n)211At reaction. In ord ... Cite

Para-[18F]fluorobenzylguanidine kinetics in a canine coronary artery occlusion model.

Journal Article J Nucl Cardiol · 1996 BACKGROUND: The kinetics of para-[18F]fluorobenzylguanidine ([18F]PFBG) were investigated in a canine coronary artery occlusion model. METHODS AND RESULTS: Five dogs were imaged by positron emission tomography (PET) before and after complete surgical ligat ... Full text Link to item Cite

Radioimmunotherapy of breast cancer xenografts with monoclonal antibody ICR12 against c-erbB2 p185: comparison of iodogen and N-succinimidyl 4-methyl-3-(tri-n-butylstannyl)benzoate radioiodination methods.

Journal Article Cancer Res · December 1, 1995 C-erbB2 p185 is a proto-oncogene product expressed in 25-30% of human invasive breast cancers that is associated with poor prognosis and resistance to endocrine therapy and chemotherapy. It is minimally expressed in normal adult tissues (M. F. Press et al. ... Link to item Cite

Tumor-specific anti-epidermal growth factor receptor variant III monoclonal antibodies: use of the tyramine-cellobiose radioiodination method enhances cellular retention and uptake in tumor xenografts.

Journal Article Cancer Res · October 1, 1995 Amplification and rearrangement of the epidermal growth factor receptor (EGFR) gene are characteristics of many types of tumors. One class of EGFR mutations, EGFRvIII, is characterized by an in-frame deletion resulting in a truncated external domain of the ... Link to item Cite

Fluorine-18 labeled chemotactic peptides: a potential approach for the PET imaging of bacterial infection.

Journal Article Nucl Med Biol · August 1995 A potent chemotactic peptide, formyl-norleucyl-leucyl-phenylalanyl-norleucyl-tyrosyl-lysine was derivatized by reaction with N-succinimidyl 4-fluorobenzoate. This derivatized peptide bound to human polymorphonuclear leukocytes in vitro and exhibited biolog ... Full text Link to item Cite

Cloning and sequencing of V genes from anti-osteosarcoma monoclonal antibodies TP-1 and TP-3: location of lysine residues and implications for radiolabeling.

Journal Article Nucl Med Biol · August 1995 Monoclonal antibodies TP-1 and TP-3 are of potential utility for the radioimmunodiagnosis of osteosarcoma in both human and canine patients. The V genes of these antibodies were cloned and sequenced and to facilitate radiolabeling of these proteins, the lo ... Full text Link to item Cite

Monoclonal antibodies against EGFRvIII are tumor specific and react with breast and lung carcinomas and malignant gliomas.

Journal Article Cancer Res · July 15, 1995 Despite molecular biological advances in understanding human cancers, translation into therapy has been less forthcoming; targeting neoplastic cells still requires that tumor-specific markers, preferably those on the cell surface, be identified. The epider ... Link to item Cite

Preparation and preliminary evaluation of 4-[211At]astato-N-piperidinoethyl benzamide.

Journal Article Nucl Med Biol · May 1995 The potential therapeutic agent, 4-[211At]astato-N-piperidinoethyl benzamide (4-APAB) was synthesized via a halodestannylation reaction. Radiochemical yields were 69% for a 5 min reaction and reached 74% by 25 min, whereas 82% radiochemical yields were obt ... Full text Link to item Cite

Validation of 4-[fluorine-18]fluoro-3-iodobenzylguanidine as a positron-emitting analog of MIBG.

Journal Article J Nucl Med · April 1995 UNLABELLED: This study evaluates the potential utility of 4-[18F]fluoro-3-iodobenzylguanidine ([18F]FIBG) as an MIBG analog. METHODS: In vitro assays of tracer binding were carried out using the SK-N-SH human neuroblastoma cell line in a paired-label forma ... Link to item Cite

Uptake mechanisms of meta-[123I]iodobenzylguanidine in isolated rat heart.

Journal Article Nucl Med Biol · January 1995 In order to clarify the uptake and retention mechanisms of radioiodinated meta-iodobenzylguanidine (MIBG) in heart, the kinetics of no-carrier-added [123I]MIBG were studied in the isolated working rat heart in interaction with pharmacologic agents. The tra ... Full text Link to item Cite

Enhanced tumour uptake and in vitro radiotoxicity of no-carrier-added [131I]meta-iodobenzylguanidine: implications for the targeted radiotherapy of neuroblastoma.

Journal Article Eur J Cancer · 1995 In vitro and in vivo neuroblastoma models were used to determine whether improvements in tumour targeting in vivo and therapeutic efficacy in vitro could result from the use of no-carrier-added (n.c.a.) [131I]MIBG. Results were compared with use of the con ... Full text Link to item Cite

No-carrier-added meta-[123I]iodobenzylguanidine: synthesis and preliminary evaluation.

Journal Article Nucl Med Biol · January 1995 No-carrier-added [123I]MIBG was prepared from 3-(trimethylsilyl)benzylguanidine in 80-90% yield. Binding of this tracer to SK-N-SH human neuroblastoma cells maintained a constant level of > 50% over 2-3 log activity range. In comparison, the binding of [12 ... Full text Link to item Cite

Meta-[131I]iodobenzylguanidine uptake and meta-[211At]astatobenzylguanidine treatment in human medulloblastoma cell lines.

Journal Article J Neurooncol · 1995 Uptake of radioiodinated meta-iodobenzylguanidine (MIBG) has been demonstrated in the neural crest tumors, including neuroblastoma, pheochromocytoma, and carcinoid tumors, and is presently in use diagnostically and therapeutically in these settings. Cells ... Full text Link to item Cite

Hyperthermic modulation of radiolabelled antibody uptake in a human glioma xenograft and normal tissues.

Journal Article Int J Hyperthermia · 1995 These experiments investigate the biodistribution of radiolabelled MAb in a human glioma xenograft model after 4 h of local hyperthermia (HT) with a twofold purpose: to maximize the ratio of cumulative isotope activity in tumour relative to normal tissues, ... Full text Link to item Cite

Phase I studies of treatment of malignant gliomas and neoplastic meningitis with 131I-radiolabeled monoclonal antibodies anti-tenascin 81C6 and anti-chondroitin proteoglycan sulfate Me1-14 F (ab')2--a preliminary report.

Journal Article J Neurooncol · 1995 The advent of monoclonal antibody (MAb) technology has made Ehrlich's postulate of the 'magic bullet' an attainable goal. Although specific localization of polyvalent antibodies to human gliomas was demonstrated in the 1960s, the lack of specific, high aff ... Full text Link to item Cite

Quantitation of 211At in small volumes for evaluation of targeted radiotherapy in animal models.

Journal Article Nucl Med Biol · January 1995 We have evaluated SPECT and two planar imaging methods, geometric mean (GM) and buildup factor (BF), for their potential to quantitate in vivo 211At distributions in rat spinal subarachnoid spaces using phantom studies. The use of medium-energy collimators ... Full text Link to item Cite

Catabolism of radioiodinated murine monoclonal antibody F(ab')2 fragment labeled using N-succinimidyl 3-iodobenzoate and Iodogen methods.

Journal Article Bioconjug Chem · 1995 The F(ab')2 fragment of monoclonal antibody (MAb) Me1-14 was labeled with 125I using the Iodogen method and by reaction with N-succinimidyl 3-[125I]iodobenzoate (SIB). The labeled catabolites generated after exposure to tissue homogenates in vitro and foll ... Full text Link to item Cite

Cytotoxicity of alpha-particle-emitting m-[211At]astatobenzylguanidine on human neuroblastoma cells.

Journal Article Cancer Res · October 15, 1994 Radioiodinated m-iodobenzylguanidine (MIBG) has been used with only limited success for the treatment of neural crest tumors including neuroblastoma. Use of an MIBG analogue labeled with 211At could be advantageous because of the shorter range and higher l ... Link to item Cite

(4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography.

Journal Article J Med Chem · October 14, 1994 The aims of this investigation were to develop a no-carrier-added (nca) synthesis of (4-[18F]-fluoro-3-iodobenzyl)guanidine ([18F]FIBG) and to evaluate its potential as an MIBG analogue useful for positron emission tomography. [18F]FIBG was prepared in fou ... Full text Link to item Cite

Preclinical evaluation and PET imaging of 18F-labeled Mel-14 F(ab')2 fragment in normal dogs.

Journal Article Nucl Med Biol · October 1994 The F(ab')2 fragment of monoclonal antibody Mel-14, reactive with human melanomas and gliomas, was labeled with 18F using two acylation agents, N-succinimidyl 8-[(4'-[18F]fluorobenzyl)amino]suberate (SFBS) and N-succinimidyl 4-[18F]fluorobenzoate (SFB). Th ... Full text Link to item Cite

PET imaging of osteosarcoma in dogs using a fluorine-18-labeled monoclonal antibody Fab fragment.

Journal Article J Nucl Med · September 1994 UNLABELLED: Four dogs with histologically confirmed osteogenic sarcoma were studied with PET following intravenous injection of the 18F-labeled Fab fragment of TP-3, a monoclonal antibody specific for human and canine osteosarcomas. METHODS: The antibody f ... Link to item Cite

Radioimmunotherapy of neoplastic meningitis in rats using an alpha-particle-emitting immunoconjugate.

Journal Article Cancer Res · September 1, 1994 Because of their short range and high linear energy transfer, alpha-particles may be particularly effective in the treatment of neoplastic meningitis. Monoclonal antibody 81C6 was labeled with alpha-particle-emitting 211At using N-succinimidyl3-[211At]asta ... Link to item Cite

Generation and characterization of a mouse/human chimeric antibody directed against extracellular matrix protein tenascin.

Journal Article J Neuroimmunol · July 1994 The murine anti-tenascin monoclonal antibody 81C6, following iodination, has been shown to be an efficient localizing and therapeutic agent in both subcutaneous and intracranial human glioma xenograft models in athymic mice and rats. Similarly, effective m ... Full text Link to item Cite

Meta-[211At]astatobenzylguanidine: further evaluation of a potential therapeutic agent.

Journal Article Int J Cancer · June 15, 1994 Meta-[211At]astatobenzylguanidine ([211At]MABG) is an astatinated analogue of meta-iodobenzylguanidine (MIBG) that could be of value for therapeutic applications. The initial goal of this study was to determine whether [211At]MABG is taken up, like MIBG, b ... Full text Link to item Cite

QUANTITATIVE IMAGING OF AT-211 RADIOTHERAPEUTIC AGENTS IN SMALL VOLUMES

Journal Article JOURNAL OF NUCLEAR MEDICINE · May 1, 1994 Link to item Cite

QUANTITATIVE MEASUREMENTS FOR SMALL ORGANS OF MONKEY

Journal Article JOURNAL OF NUCLEAR MEDICINE · May 1, 1994 Link to item Cite

Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine.

Journal Article Nucl Med Commun · April 1994 Meta-iodobenzylguanidine (MIBG) is a drug which is selectively accumulated by the uptake-1 process in adrenergic tissues. When labelled with 131I, it may be used for the targetted radiotherapy of tumours such as phaeochromocytoma and neuroblastoma. This pa ... Full text Link to item Cite

Mouse/human chimeric Me1-14 antibody: genomic cloning of the variable region genes, linkage to human constant region genes, expression, and characterization.

Journal Article Hybridoma · April 1994 Murine monoclonal antibody Me1-14, which recognizes an epitope on chondroitin proteoglycan sulfate expressed in malignant glioma and melanoma, has been used for radioimmunolocalization and therapy both in animal models and in patients. Here, we report the ... Full text Link to item Cite

Pinhole collimation for ultra-high-resolution, small-field-of-view SPECT.

Journal Article Phys Med Biol · March 1994 The objective of this investigation was to evaluate small-field-of-view, ultra-high-resolution pinhole collimation for a rotating-camera SPECT system that could be used to image small laboratory animals. Pinhole collimation offers distinct advantages over ... Full text Link to item Cite

Improved synthesis of N-succinimidyl 4-[18F]fluorobenzoate and its application to the labeling of a monoclonal antibody fragment.

Journal Article Bioconjug Chem · 1994 Our previously reported method for the 18F labeling of antibodies using N-succinimidyl 4-[18F]fluorobenzoate (SFB) involved a rather long synthesis time. Here we present an improved method for the synthesis of SFB which reduces the synthesis time by about ... Full text Link to item Cite

Monoclonal antibody F(ab')2 fragment labeled with N-succinimidyl 2,4-dimethoxy-3-halobenzoates: in vivo comparison of iodinated and astatinated fragments.

Journal Article Nucl Med Biol · January 1994 N-Succinimidyl 3-[211At]astato-2, 4-dimethoxybenzoate (SADMB) was prepared from a trialkylstannyl precursor in about 70-75% yield. With either trimethyl or tri-n-butylstannyl precursor, no temporal effect was found in the astatodestannylation yield. Howeve ... Full text Link to item Cite

Catabolism of label from Mel-14 F(ab')2 fragment radiohalogenated using N-succinimidyl 3-halobenzoates

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · January 1, 1994 Cite

Synthesis and preliminary evaluation of para- and meta-[18F]fluorobenzylguanidine.

Journal Article Nucl Med Biol · January 1994 meta-[18F]Fluorobenzylguanidine ([18F]MFBG) and para-[18F]fluorobenzylguanidine ([18F]PFBG) were synthesized in three steps beginning with a fluoro for nitro exchange reaction on 3- and 4-nitrobenzonitrile, respectively. Overall radiochemical yields were 1 ... Full text Link to item Cite

Meta-[211At]astatobenzylguanidine: Further validation of in vitro and in vivo uptake mechanisms

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · 1994 Cite

Fluorine-18 labeled chemotactic peptide: A potential agent for the PET imaging of focal infection

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · January 1, 1994 Cite

(4-[18F]fluoro-3-iodobenzyl)guanidine, a potential mibg analogue for positron emission tomography

Journal Article Journal of Medicinal Chemistry · 1994 The aims of this investigation were to develop a no-carrier-added (nca) synthesis of (4-[18F]-fluoro-3-iodobenzyl)guanidine ([18F]FIBG) and to evaluate its potential as an MIBG analogue useful for positron emission tomography. [18F]FIBG was prepared in fou ... Cite

PARA-[F-18]FLUOROBENZYLGUANIDINE ([F-18]PFBG) - FURTHER EVALUATION OF A POTENTIAL PET RADIOTRACER IN DOGS

Conference PROCEEDINGS OF THE XVI INTERNATIONAL CANCER CONGRESS - FREE PAPERS AND POSTERS, TOMES 1-4 · January 1, 1994 Link to item Cite

RADIONUCLIDE THERAPY - A REVIEW

Conference HADRONTHERAPY IN ONCOLOGY · January 1, 1994 Link to item Cite

Meta-[211At]astatobenzylguanidine: Further validation of in vitro and in vivo uptake mechanisms

Conference Journal of Labelled Compounds and Radiopharmaceuticals · January 1, 1994 Cite

Radioiodination of a monoclonal antibody using N-succinimidyl 5-iodo-3-pyridinecarboxylate.

Journal Article Nucl Med Biol · October 1993 The potential utility of N-succinimidyl 5-iodo-3-pyridinecarboxylate (SIPC) for the radioiodination of monoclonal antibodies was investigated. Paired-label studies were performed using the anti-tenascin antibody 81C6 in athymic mice bearing subcutaneous D- ... Full text Link to item Cite

Measuring astatine-211 distributions with SPECT.

Journal Article Phys Med Biol · August 1993 We have investigated standard SPECT techniques (rotating gamma cameras, multi-hole collimators, and filtered backprojection reconstruction) for imaging astatine-211 distributions. Since 211At emits alpha particles, this nuclide has potential for use in rad ... Full text Link to item Cite

Distribution and dosimetry of I-123-labeled monoclonal antibody 81C6 in patients with anaplastic glioma.

Journal Article Invest Radiol · June 1993 RATIONALE AND OBJECTIVES: Monoclonal antibody 81C6 reacts with the extracellular matrix antigen, tenascin, present on gliomas and other tumors, as well as several normal tissues, including spleen and liver tissue. Single photon emission computed tomography ... Link to item Cite

N-succinimidyl 4-methyl-3-(tri-n-butylstannyl)benzoate: synthesis and potential utility for the radioiodination of monoclonal antibodies.

Journal Article Nucl Med Biol · May 1993 N-succinimidyl 4-methyl-3-(tri-n-butylstannyl)benzoate (MATE) was synthesized in two steps from 4-methyl-3-iodobenzoic acid. Radioiododestannylation of MATE proceeded more slowly than N-succinimidyl 3-(tri-n-butylstannyl)benzoate (ATE), but for reaction pe ... Full text Link to item Cite

MEASURING ASTATINE-211 DISTRIBUTIONS WITH SPECT

Journal Article JOURNAL OF NUCLEAR MEDICINE · May 1, 1993 Link to item Cite

INVITRO CYTOTOXICITY OF M-[AT-211]ASTATOBENZYLGUANIDINE (MABG)

Journal Article JOURNAL OF NUCLEAR MEDICINE · May 1, 1993 Link to item Cite

GENERATION AND CHARACTERIZATION OF MOUSE-HUMAN CHIMERIC MEL-14 ANTIBODY

Journal Article JOURNAL OF IMMUNOLOGY · April 15, 1993 Link to item Cite

No-carrier-added synthesis of meta-[131I]iodobenzylguanidine.

Journal Article Appl Radiat Isot · March 1993 No-carrier-added meta-[131I]iodobenzylguanidine ([131I]MIBG) was prepared starting with two different metallated precursors. Attempted preparation of 3-(tri-n-butylstannyl)benzylguanidine was not successful. An alternate two-step strategy using 3-(tri-n-bu ... Full text Link to item Cite

Radioiodination of proteins using N-succinimidyl 4-hydroxy-3-iodobenzoate.

Journal Article Bioconjug Chem · 1993 N-Succinimidyl 4-hydroxy-3-[131I]iodobenzoate ([131I]SHIB) was synthesized from 4-hydroxybenzoic acid in two steps. The overall radiochemical yield was 40-56%. A monoclonal antibody (mAb) was labeled in 10-15% yield by reaction with [131I]SHIB. The specifi ... Full text Link to item Cite

Localization of fluorine-18-labeled Mel-14 monoclonal antibody F(ab')2 fragment in a subcutaneous xenograft model.

Journal Article Cancer Res · September 15, 1992 Positron emission tomography is an imaging method that might improve the effectiveness of radioimmunoscintigraphy and might provide more accurate estimates of monoclonal antibody dosimetry prior to therapy. Because of its widespread availability, 2-h half- ... Link to item Cite

Immunoreactivity, pharmacokinetics and bone marrow dosimetry of intrathecal radioimmunoconjugates.

Journal Article Int J Cancer · August 19, 1992 Ten patients with neoplastic meningitis were treated with a variety of 131I-monoclonal antibody (MAb) conjugates, chosen to bind to their particular malignancy. Pharmacokinetic studies revealed that MAbs leave the ventricular compartment, enter the sub-ara ... Full text Link to item Cite

Fluorine-18-labeled monoclonal antibody fragments: a potential approach for combining radioimmunoscintigraphy and positron emission tomography.

Journal Article J Nucl Med · August 1992 Monoclonal antibody fragments labeled with 18F could be useful for PET if selective tumor uptake could be achieved within a few half-lives of this nuclide. To evaluate this possibility, the F(ab')2 fragment of Mel-14, an antibody reactive with gliomas and ... Link to item Cite

Labeling proteins with fluorine-18 using N-succinimidyl 4-[18F]fluorobenzoate.

Journal Article Int J Rad Appl Instrum B · April 1992 Two methods were investigated for the no-carrier-added synthesis of N-succinimidyl 4-[18F]fluorobenzoate (S[18F]FB). The first, an attempted nucleophilic aromatic substitution by [18F]fluoride on N-succinimidyl 4-nitrobenzoate was unsuccessful. The second ... Full text Link to item Cite

Fluorine-18-antimyosin monoclonal antibody fragments: preliminary investigations in a canine myocardial infarct model.

Journal Article J Nucl Med · April 1992 The purpose of this study was to determine in a canine model whether selective myocardial infarct uptake of 18F-labeled antimyosin monoclonal antibody fragments could be achieved in a time frame compatible with the short half-life of this nuclide. Antimyos ... Link to item Cite

1-(m-[211At]astatobenzyl)guanidine: synthesis via astato demetalation and preliminary in vitro and in vivo evaluation.

Journal Article Bioconjug Chem · 1992 No-carrier-added 1-(m-[211At]astatobenzyl)guanidine ([211At]MABG) was synthesized by astato demetalation using two different routes. The overall yield for the two-step approach from 3-(tri-n-butylstannyl)benzylamine was 13%. N-Chlorosuccinimide-mediated as ... Full text Link to item Cite

4-Fluorobenzylamine and phenylalanine methyl ester conjugates of 2-nitroimidazole: evaluation as hypoxic cell radiosensitizers.

Journal Article Int J Radiat Oncol Biol Phys · 1992 We have synthesized two 2-nitroimidazole derivatives and evaluated their hypoxic radiosensitization properties. The first, a 4-fluorobenzylamine conjugate of 2-nitroimidazole (PK-110), was designed so that it could also be labeled with the F-18 and used fo ... Full text Link to item Cite

1-(m-[211At]astatobenzyl)guanidine: Synthesis via astato demetalation and preliminary in vitro and in vivo evaluation

Journal Article Bioconjugate Chemistry · 1992 No-carrier-added 1-(m-[211At]astatobenzyl)guanidine ([211At]MABG) was synthesized by astato demetalation using two different routes. The overall yield for the two-step approach from 3-(tri-n-butylstannyl)benzylamine was 13%. N-Chlorosuccinimide-mediated as ... Cite

Improved therapeutic efficacy of a monoclonal antibody radioiodinated using N-succinimidyl-3-(tri-n-butylstannyl)benzoate.

Journal Article Cancer Res · August 15, 1991 Improvements in efficacy of radioimmunotherapy will require increased tumor uptake relative to normal tissue. We previously demonstrated that labeling the IgG2b glioma-reactive antitenascin monoclonal antibody 81C6 with 131I using N-succinimidyl-3-(tri-n-b ... Link to item Cite

Radioiodination and astatination of monoclonal antibodies using heterocyclic acylation agents

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · April 5, 1991 Cite

Aromatic acylation reagents for use in the radioiodination of proteins

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · April 5, 1991 Cite

Fluorine-18 labeling of monoclonal antibodies and fragments with preservation of immunoreactivity.

Journal Article Bioconjug Chem · 1991 A new method is reported for labeling proteins with the positron-emitting nuclide 18F. Initially, 4-[18F]-fluorobenzylamine was prepared in two steps from aqueous [18F]fluoride in high yield. The 18F acylation agent was formed by reaction of this product w ... Full text Link to item Cite

N-succinimidyl 5-(trialkylstannyl)-3-pyridinecarboxylates: a new class of reagents for protein radioiodination.

Journal Article Bioconjug Chem · 1991 N-Succinimidyl 5-(trialkylstannyl)-3-pyridinecarboxylates (alkyl = Me, Bu) have been prepared and used as a precursor to label N-succinimidyl 5-[131I]iodo-3-pyridinecarboxylate (SIPC). SIPC was obtained in greater than 80% yield from either the methyl or b ... Full text Link to item Cite

Radiolocalization of human pancreatic tumors in athymic mice by monoclonal antibody DU-PAN 1.

Journal Article Cancer Res · November 15, 1990 Monoclonal antibodies that selectively bind to pancreatic tumors may be useful in the therapy and diagnosis of pancreatic carcinoma. In this study we have examined the tumor localization of radioiodinated DU-PAN 1, a mouse monoclonal antibody that is selec ... Link to item Cite

Intrathecal administration of 131I radiolabelled monoclonal antibody as a treatment for neoplastic meningitis.

Journal Article Br J Cancer · October 1990 Fifteen patients with neoplastic meningitis received a single intrathecal injection of between 11 and 60 mCi of a 131I radiolabelled monoclonal antibody (MoAb), chosen for its immunoreactivity to tumour. Major toxicity was manifest as nausea, vomiting and ... Full text Link to item Cite

Monoclonal antibody and F(ab')2 fragment delivery to tumor in patients with glioma: comparison of intracarotid and intravenous administration.

Journal Article Cancer Res · July 1, 1990 Non-i.v. delivery of radiolabeled monoclonal antibodies (MAbs) has been shown to increase tumor uptake and decrease dose to normal tissues. In this study, we have examined the potential advantage of intracarotid (i.c.) versus i.v. administration for the de ... Link to item Cite

Comparative tissue distribution in mice of the alpha-emitter 211At and 131I as labels of a monoclonal antibody and F(ab')2 fragment.

Journal Article Cancer Res · June 15, 1990 Because it decays by the emission of short-range, high-energy alpha-particles, the radiohalogen 211At might be a particularly useful nuclide for some types of radioimmunotherapy. However, no suitable gamma-emitting nuclide of astatine exists which would pe ... Link to item Cite

Anti-synthetic peptide antibody reacting at the fusion junction of deletion-mutant epidermal growth factor receptors in human glioblastoma.

Journal Article Proc Natl Acad Sci U S A · June 1990 We have investigated human gliomas that amplify and rearrange the epidermal growth factor receptor gene, with generation of an in-frame deletion mutation of 802 nucleotides in the external domain. This in-frame deletion mutation generates a local amino aci ... Full text Link to item Cite

RADIOIODINATION AND ASTATINATION OF MONOCLONAL-ANTIBODIES

Journal Article ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY · April 22, 1990 Link to item Cite

Enhanced delivery of a monoclonal antibody F(ab')2 fragment to subcutaneous human glioma xenografts using local hyperthermia.

Journal Article Cancer Res · March 15, 1990 The purpose of this study was to investigate the effects of tumor-localized hyperthermia at 42 degrees C on the tissue distribution of radioiodinated monoclonal antibody F(ab')2 fragments. Paired-label biodistribution measurements were performed in athymic ... Link to item Cite

Radioimmunotherapy of intracerebral human glioma xenografts with 131I-labeled F(ab')2 fragments of monoclonal antibody Mel-14.

Journal Article Cancer Res · March 15, 1990 The administration of radiolabeled monoclonal antibodies to improve the treatment of malignant gliomas is dependent upon achieving effective tumor radiation dose while sparing normal tissues. We have evaluated the efficacy of 131I-labeled F(ab')2 fragment ... Link to item Cite

Radioiodination of antibodies via N-succinimidyl 2,4-dimethoxy-3-(trialkylstannyl)benzoates.

Journal Article Bioconjug Chem · 1990 We have previously shown that use of N-succinimidyl 3-iodobenzoate (SIB) for radioiodination of monoclonal antibodies (MAbs) decreases the loss of radioiodine in vivo compared to MAbs labeled by using conventional methods. Herein, the synthesis of N-succin ... Full text Link to item Cite

Protein radiohalogenation: observations on the design of N-succinimidyl ester acylation agents.

Journal Article Bioconjug Chem · 1990 In previous studies we have demonstrated that antibodies radioiodinated with N-succinimidyl 3-iodobenzoate (SIB) are less susceptible to loss of radioiodine in vivo than antibodies iodinated directly by electrophilic substitution on their tyrosine residues ... Full text Link to item Cite

Rhenium heptasulfide: a potential carrier system for radiation synovectomy.

Journal Article Int J Rad Appl Instrum B · 1990 Rhenium sulfide colloid was prepared by the thiosulfate acid reduction method and assessed for its applicability as a particle carrier for use in radiation synovectomy. In vitro stability studies demonstrated that greater than 95% of the 186Re activity rem ... Full text Link to item Cite

Labeling monoclonal antibodies with halogen nuclides.

Journal Article Acta Radiol Suppl · 1990 Most studies with radiohalogenated monoclonal antibodies have involved the use of the iodine nuclides 131I and 123I. Methods are being developed for labeling antibodies with radioiodine that result in a decreased loss of the nuclide from the protein in viv ... Link to item Cite

Enhanced tumor localization and in vivo stability of a monoclonal antibody radioiodinated using N-succinimidyl 3-(tri-n-butylstannyl)benzoate.

Journal Article Cancer Res · October 15, 1989 Loss of radiolabel after in vivo administration of labeled monoclonal antibodies (MAbs) to cancer patients is a likely cause of the low levels of tumor uptake of MAb which have been observed. In this study, we have evaluated the utility of N-succinimidyl 3 ... Link to item Cite

Labeling monoclonal antibodies and F(ab')2 fragments with the alpha-particle-emitting nuclide astatine-211: preservation of immunoreactivity and in vivo localizing capacity.

Journal Article Proc Natl Acad Sci U S A · September 1989 alpha-Particles such as those emitted by 211At may be advantageous for radioimmunotherapy since they are radiation of high linear energy transfer, depositing high energy over a short distance. Here we describe a strategy for labeling monoclonal antibodies ... Full text Link to item Cite

Pharmacokinetics and tumor localization of 131I-labeled anti-tenascin monoclonal antibody 81C6 in patients with gliomas and other intracranial malignancies.

Journal Article Cancer Res · May 15, 1989 We previously have reported that radioiodinated anti-tenascin monoclonal antibody 81C6 exhibits therapeutic potential against both s.c. and intracranial human glioma xenografts in athymic mice and rats. Herein we report the selective tumor localization of ... Link to item Cite

RADIOHALOGENATION OF ANTIBODIES

Journal Article ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY · April 9, 1989 Link to item Cite

Synthesis of radioiodinated N-succinimidyl iodobenzoate: optimization for use in antibody labelling.

Journal Article Int J Rad Appl Instrum A · 1989 N-succinimidyl-3-(tri-n-butylstannyl)benzoate (m-BuATE), N-succinimidyl-3-(tri-methylstannyl)benzoate (m-MeATE) and N-succinimidyl-4-(tri-n-butylstannyl)benzoate (p-BuATE) were synthesized and radioiodinated using either N-chlorosuccinimide (NCS) or t-buty ... Full text Link to item Cite

Labeling proteins using aryl iodide acylation agents: influence of meta vs para substitution on in vivo stability.

Journal Article Int J Rad Appl Instrum B · 1989 The effect of para vs meta substitution on the biological behavior of an intact antibody and an F(ab')2 fragment was investigated. Paired-label studies were performed using 81C6 IgG and OC 125 F(ab')2 labeled using the N-succinimidyl esters of both p-[125I ... Full text Link to item Cite

Pharmacokinetics of a radioiodinated monoclonal antibody F(ab')2 fragment in a xenograft model with circulating antigen.

Journal Article Int J Rad Appl Instrum B · 1989 The pharmacokinetics of 131I-labeled OC 125 F(ab')2 antibody fragment were investigated in athymic mice bearing OVCAR-3 ovarian carcinoma xenografts, a model in which the CA 125 antigen is present in serum. Nine antibody doses between 0.1 and 650 microgram ... Full text Link to item Cite

Pharmacokinetics of a radioiodinated monoclonal antibody F(ab')2 fragment in a xenograft model with circulating antigen

Journal Article Nuclear Medicine and Biology · January 1, 1989 The pharmacokinetics of 131 I-labeled OC 125 F(ab') 2 antibody fragment were investigated in athymic mice bearing OVCAR-3 ovarian carcinoma xenografts, a model in which the CA 125 antigen is present in serum. Nine antibody doses between 0.1 an 650 μg wer ... Cite

No-Carrier-Added Astatination of N-Succinimidyl-3-(Tri-n-Butylstannyl) Benzoate (ATE) Via Electrophilic Destannylation1

Journal Article Radiochimica Acta · January 1, 1989 The no-carrier-added synthesis of N-succinimidyl 3–[211 At]astato-benzoate from N-succinimidyl 3-(tri-w-butylstannyl)benzoate (ATE) is described. The nature of the solvent in which the 211At was isolated from the target was an important factor influencing ... Full text Cite

Comparative localization of murine monoclonal antibody Me1-14 F(ab')2 fragment and whole IgG2a in human glioma xenografts.

Journal Article Cancer Res · October 15, 1988 Monoclonal antibodies (MAbs) targeted to glioma-associated antigens may allow the selective delivery of imaging and therapeutic agents to brain tumors; the use of MAb fragments may be a strategy to further improve tumor uptake of such agents relative to no ... Link to item Cite

ASTATINE-211 LABELED MONOCLONAL-ANTIBODY - A POTENTIAL AGENT FOR RADIOIMMUNOTHERAPY

Journal Article EUROPEAN JOURNAL OF NUCLEAR MEDICINE · August 1, 1988 Link to item Cite

Treatment of intracranial human glioma xenografts with 131I-labeled anti-tenascin monoclonal antibody 81C6.

Journal Article Cancer Res · May 15, 1988 Lack of tumor specificity renders current modalities for treating malignant glioma ineffective. The administration of 131I-labeled monoclonal antibody (Mab) 81C6, which reacts with the glioma-associated extracellular matrix antigen, tenascin, to nude mice ... Link to item Cite

Radiohalogenation of a monoclonal antibody using an N-succinimidyl 3-(tri-n-butylstannyl)benzoate intermediate.

Journal Article Cancer Res · March 15, 1988 N-Succinimidyl 3-(tri-n-butylstannyl)benzoate (ATE) was elevated for its utility in the radiohalogenation of monoclonal antibodies. The F(ab')2 fragment of monoclonal antibody OC 125 was labeled with 125I using the ATE reagent and with 131I using a convent ... Link to item Cite

Therapeutic efficacy of antiglioma mesenchymal extracellular matrix 131I-radiolabeled murine monoclonal antibody in a human glioma xenograft model.

Journal Article Cancer Res · February 1, 1988 The development of Mabs, particularly those reactive with primary brain tumors but not with normal brain, provides a potential means of delivering therapeutic agents selectively to human malignant gliomas. Mab 81C6, an IgG2b immunoglobulin, which defines a ... Link to item Cite

Therapeutic Efficacy of Antiglioma Mesenchymal Extracellular Matrix 131I-Radiolabeled Murine Monoclonal Antibody in a Human Glioma Xenograft Model

Journal Article Cancer Research · January 1, 1988 The development of Mabs, particularly those reactive with primary brain tumors but not with normal brain, provides a potential means of delivering therapeutic agents selectively to human malignant gliomas. Mab 81C6 an IgG2b immunoglobulin, which defines an ... Cite

The localisation of radiolabelled murine monoclonal antibody 81C6 and its Fab fragment in human glioma xenografts in athymic mice.

Journal Article Br J Neurosurg · 1988 The localisation of the radioiodinated Fab fragment of monoclonal antibody (Mab) 81C6, reactive with a glioma-associated extracellular matrix antigen, was studied in athymic mice bearing subcutaneous and intracranial xenografts of D-54 MG glioma cells. In ... Full text Link to item Cite

Astatination of proteins using an N-succinimidyl tri-n-butylstannyl benzoate intermediate.

Journal Article Int J Rad Appl Instrum A · 1988 A method is described for labeling proteins with 7.2 h half-life 211 At. The alpha particle-emitting nuclide was coupled to goat IgG using an N-succinimidyl 3-(tri-n-butylstannyl) benzoate intermediate. The reaction and purification sequence requires about ... Full text Link to item Cite

Influence of circulating antigen on blood pool activity of a radioiodinated monoclonal antibody.

Journal Article Int J Rad Appl Instrum B · 1988 Athymic mice with and without circulating CA 125 antigen were injected with 0.1-100 micrograms of 131I-labeled OC 125 F(ab')2 antibody fragment. Both the blood clearance of 131I activity and the change in serum CA 125 were monitored over 24 h. Influence of ... Full text Link to item Cite

Effect of radioiodination on the binding of monoclonal antibody DF3 to breast carcinoma cells.

Journal Article Int J Rad Appl Instrum B · 1988 The murine monoclonal antibody (MAb) designated DF3 is an IgG1 prepared against a membrane enriched fraction of human breast carcinoma. MAb DF3 reacts with a family of large molecular weight glycoproteins expressed by 78% of breast cancer cells and 95% of ... Full text Link to item Cite

Use of liposomes as carriers for radiation synovectomy.

Journal Article Int J Rad Appl Instrum B · 1988 Using [99mTc]pertechnetate as an aqueous space marker, the permeability of liposomes composed of seven different mixtures of distearoylphosphatidylcholine (DSPC) and sphingomyelin (SM) was determined. Liposomes containing 20-33% SM were the least permeable ... Full text Link to item Cite

Influence of circulating antigen on blood pool activity of a radioiodinated monoclonal antibody

Journal Article Nuclear Medicine and Biology · January 1, 1988 Athymic mice with and without circulating CA 125 antigen were injected with 0.1-100 μg of 131 I-labeled OC 125 F(ab') 2 antibody fragment. Both the blood clearance of 131 I activity and the change in serum CA 125 were monitored over 24 h. Influence of C ... Cite

Use of liposomes as carriers for radiation synovectomy

Journal Article Nuclear Medicine and Biology · January 1, 1988 Using [ 99m Tc]pertechnetate as an aqueous space marker, the permeability of liposomes composed of seven different mixtures of distearoylphosphatidylcholine (DSPC) and sphingomyelin (SM) was determined. Liposomes containing 20-33% SM were the least permeab ... Cite

Synthesis of N-succinimidyl-2,4-dimethoxy-3-(tri-N-butylstannyl) benzoate via regio-specifically generated lithium 2,4-dimethoxy-3-lithiobenzoate

Journal Article Tetrahedron Letters · January 1, 1988 Lithium 2,4-dimethoxy-3-lithiobenzoate can be efficiently generated from 2,4-dimethoxy-3-bromobenzoic acid in THF at -100°C. © 1988. ... Full text Cite

Synovectomy of the rheumatoid knee using intra-articular injection of dysprosium-165-ferric hydroxide macroaggregates.

Journal Article J Bone Joint Surg Am · September 1987 One hundred and eleven patients who had seropositive rheumatoid arthritis and persistent synovitis of the knee were treated with intra-articular injection of 270 millicuries of dysprosium-165 bound to ferric hydroxide macroaggregates. A two-year follow-up ... Link to item Cite

Evaluation of indium-111 chloride as a radiopharmaceutical for joint imaging in a rabbit model of arthritis.

Journal Article Invest Radiol · September 1987 The potential use of 111In-chloride as a radiopharmaceutical for quantitating the extent of synovitis was investigated in a rabbit model of antigen-induced arthritis. Rabbits with monoarticular disease were injected with 111In-chloride and imaged at 30 min ... Full text Link to item Cite

Comparative localization of glioma-reactive monoclonal antibodies in vivo in an athymic mouse human glioma xenograft model.

Journal Article J Neuroimmunol · May 1987 Radioiodinated murine monoclonal antibodies (Mabs) 81C6, Me 1-14, C12, D12, and E9, made against or reactive with human gliomas but not normal brain, and Mab UJ13A, a pan-neuroectodermal Mab reactive with normal human glial and neural cells, were evaluated ... Full text Link to item Cite

Comparison of monoclonal antibody delivery to intracranial glioma xenografts by intravenous and intracarotid administration.

Journal Article Cancer Res · April 1, 1987 Monoclonal antibody 81C6, which is directed against a human gliomamesenchymal extracellular matrix antigen, was used to evaluate the potential advantage of intracarotid (i.c.) administration versus i.v. delivery to D-54 MG human glioma intracranial xenogra ... Link to item Cite

Characterization of liposomes containing iodine-125-labeled radiographic contrast agents.

Journal Article Invest Radiol · February 1987 Multilamellar liposomes were prepared containing either iodine-125-labeled (125I) diatrizoate or 125-I labeled iotrol in their aqueous phase. The in vitro permeabilities of liposomes containing both contrast agents were measured in the presence of saline a ... Full text Link to item Cite

Use of radiolabeled monoclonal anti-B1 antibody for B lymphocyte imaging in rhesus monkeys.

Journal Article Int J Rad Appl Instrum B · 1987 Imaging tissues rich in B lymphocytes in man using a radiolabeled monoclonal anti-B cell antibody would be extremely useful in the clinical staging of non-Hodgkins lymphomas. Studies were done in rhesus monkeys using radiolabeled monoclonal anti-B1 antibod ... Full text Link to item Cite

A method for the radiohalogenation of proteins resulting in decreased thyroid uptake of radioiodine.

Journal Article Int J Rad Appl Instrum A · 1987 A procedure is described for the radioiodination of proteins using an iodinated derivative of N-succinimidyl 3-(tri-n-butylstannyl) benzoate (ATE). Adequate removal of unreacted ATE from [125I]ATE was necessary for optimal protein radioiodination. Labeling ... Full text Link to item Cite

Specific imaging of human brain tumor xenografts utilizing radiolabelled monoclonal antibodies (MAbs).

Journal Article Nuklearmedizin · December 1986 At the present time, specific imaging and treatment of central nervous system malignancies is not possible. The development of monoclonal hybridoma technology may provide the solution to this problem. We have utilized human glioma-derived cell lines (HGCL) ... Link to item Cite

Properties of multilamellar liposomes containing99mTcO4-: Effect of distearoylphosphatidylcholine to sphingomyelin ratio

Journal Article Nuclear Medicine and Biology · December 1, 1986 Multilamellar liposomes composed of eight different mixtures of distearoylphosphatidylcholine (DSPC) and sphingomyelin (SM) were prepared containing [99mTc]pertechnetate. The in vitro permeability of the liposome preparations in buffer and serum were measu ... Cite

Pharmacokinetics of radiolabeled monoclonal antibody B6.2 in patients with metastatic breast cancer.

Journal Article Cancer Res · June 1986 Thirteen patients with metastatic breast carcinoma were given injections of 50-1593 micrograms of 131I-monoclonal antibody (MAb) B6.2 immunoglobulin G and F(ab')2 for pharmacokinetic evaluation and radioimmunoimaging. Blood clearance of the 131I-MAb-B6.2 w ... Link to item Cite

Treatment of rheumatoid synovitis of the knee with intraarticular injection of dysprosium 165-ferric hydroxide macroaggregates.

Journal Article Arthritis Rheum · February 1986 One hundred eight knees of 93 patients with seropositive rheumatoid arthritis and persistent synovitis of the knee were treated with an intraarticular injection of 270 mCi of dysprosium 165 bound to ferric hydroxide macroaggregate. Leakage of radioactivity ... Full text Link to item Cite

Radioiodination of DF3 antibody: Optimization using in vitro binding assays

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · January 1, 1986 Cite

Properties of multilamellar liposomes containing 99mTcO4-: effect of distearoylphosphatidylcholine to sphingomyelin ratio.

Journal Article Int J Rad Appl Instrum B · 1986 Multilamellar liposomes composed of eight different mixtures of distearoylphosphatidylcholine (DSPC) and sphingomyelin (SM) were prepared containing [99mTc]pertechnetate. The in vitro permeability of the liposome preparations in buffer and serum were measu ... Full text Link to item Cite

Radiation synovectomy with 165Dy-FHMA: lymph node uptake and radiation dosimetry calculations.

Journal Article Int J Nucl Med Biol · 1986 The lymph node uptake of 165Dy was measured in 25 patients treated by radiation synovectomy via intra-articular injection of 165Dy-ferric hydroxide macroaggregates (FHMA). An average of 0.12% of the injected dose was found in the inguinal lymph nodes 19h p ... Full text Link to item Cite

Radiohalogenation of monoclonal antibodies

Journal Article International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology · January 1986 Full text Cite

Radioiodinated ganglioside GM1: a potential tool for the investigation of ganglioside function in vivo.

Journal Article Pharmacol Res Commun · October 1985 Ganglioside GM1 was labeled with 125I either directly or after conjugation to tyramine. Direct iodination of the sphingosine chain resulted in a compound which dehalogenated rapidly both in vitro and in vivo. The binding of the 125I[GM1-tyramine] conjugate ... Full text Link to item Cite

Research and clinical potential of receptor based radiopharmaceuticals.

Journal Article J Nucl Med · June 1985 Receptors are proteins that have specific binding affinity for substances that produce a physiological event in the body. Receptor-binding radiotracers are being used increasingly to study the function of receptors in health and disease. This review summar ... Link to item Cite

Radioiodinated B6.2 monoclonal antibody: further characterization of a potential radiopharmaceutical for the identification of breast tumors.

Journal Article Int J Nucl Med Biol · 1985 A monoclonal antibody (B6.2) directed against human breast carcinomas and its F(ab')2 and Fab' fragments were labeled with 125I using Iodogen. Solid phase radioimmunoassay was used to evaluate the in vitro binding of the labeled antibodies to a human breas ... Full text Link to item Cite

Distribution and mechanism of uptake of 111InCl3 in a tumor model for lymph node metastases.

Journal Article Int J Nucl Med Biol · 1985 The localization of 111In activity in the tumor and draining lymph nodes of the H-4-II-E ACI rat hepatoma was investigated following the injection of 111In-chloride. In this tumor model, the tumors metastasize to the regional lymph nodes in male rats only. ... Full text Link to item Cite

Monoclonal antibodies to tissue-specific cell surface antigens. I. Characterization of an antibody to a prostate tissue antigen.

Journal Article Clin Immunol Immunopathol · November 1984 Monoclonal antibodies were raised to PC-3 human prostate adenocarcinoma cells, and one hybridoma, designated F77-129, was extensively purified and used to characterize a PC-3 antigen. The F77-129 antibody also showed serological reactivity with the Du-145 ... Full text Link to item Cite

Interaction of monoclonal antibodies with cell surface antigens of human ovarian carcinomas.

Journal Article Cancer Res · July 1984 Two monoclonal antibodies, OC 125 and OC 133, bind to distinct determinants on the surface of human epithelial ovarian carcinoma cell lines. OC 125 and OC 133 recognize determinants on molecules with molecular weights greater than 200,000 and 80,000, respe ... Link to item Cite

211At radiocolloid therapy: further observations and comparison with radiocolloids of 32P, 165Dy, and 90Y.

Journal Article Int J Radiat Oncol Biol Phys · March 1984 We compared the therapeutic efficacy of alpha and beta emitting radiocolloids for the treatment of experimental malignant ascites. 211At is an almost pure alpha-emitter. As 211At-tellurium colloid, the dose survival curve is linear and extrapolates through ... Full text Link to item Cite

Receptor-mediated radiopharmaceuticals

Journal Article Trends in Pharmacological Sciences · January 1, 1984 The development of radiotracers with defined affinities for specific receptor systems is a potentially useful approach to the design of radiopharmaceuticals for nuclear medicine. Radiolabelled ligands, such as hormones and neurotransmitters, are being synt ... Full text Cite

211At radiocolloid therapy: Further observations and comparison with radiocolloids of 32P, 165Dy, and 90Y

Journal Article International Journal of Radiation Oncology, Biology, Physics · 1984 We compared the therapeutic efficacy of α and β emitting radiocolloids for the treatment of experimental malignant ascites. 211At is an almost pure α- emitter. As 211At-tellurium colloid, the dose survival curve is linear and extrapolates through the origi ... Cite

Radiolocalization of human mammary tumors in athymic mice by a monoclonal antibody.

Journal Article Cancer Res · February 1983 Monoclonal antibody B6.2 reacts with a protein found on the surface of primary and metastatic human mammary tumors. B6.2 immunoglobulin G (IgG) was purified, F(ab')2 and Fab' fragments were generated by pepsin digestion, and the IgG and its fragments were ... Link to item Cite

Synthesis of 11C-dl-tryptophan and its purification using high-pressure liquid chromatography

Journal Article The International Journal Of Applied Radiation And Isotopes · January 1, 1981 Carbon-11-dl-tryptophan has been produced from 11C-cyanide using a modified Bücherer-Strecker technique for synthesis and a high-pressure liquid chromatographic system for purification. More than 80 preparations have been run with an average radiochemical ... Full text Cite

Positron emission tomography for the evaluation of pancreatic disease.

Journal Article Semin Nucl Med · October 1980 Efficient techniques for native-labeling of amino acids have been combined successfully with emission tomography to yield significant improvements in pancreatic imaging. Carbon-11-labeled tryptophan appears to be the best agent available currently for imag ... Full text Link to item Cite

PREPARATION OF BR-77 AND BR-76 L-DOPA AND 5-HYDROXYTRYPTOPHAN ANALOGS

Conference JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS · 1979 Cite

Preparation of 77Br and 76Br L-DOPA and 5-hydroxytryptophan analogues

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · January 1, 1979 Cite

N-13 NITROUS-OXIDE FOR CEREBRAL IMAGING STUDIES

Conference JOURNAL OF NUCLEAR MEDICINE · 1978 Cite

Nitrogen-13 nitrous oxide for cerebral imaging studies

Journal Article Journal of Nuclear Medicine · January 1, 1978 Cite

Synthesis of a non labile astatine protein conjugate

Journal Article Journal of Labelled Compounds and Radiopharmaceuticals · December 1, 1977 Cite

Organ distribution of 99mTc-labelled aminethiols.

Journal Article Int J Nucl Med Biol · January 1977 Full text Link to item Cite

Structure of N=81 nuclei: Levels of Nd141 and Ce139 populated in beta decay

Journal Article Physical Review C · January 1, 1976 The nuclear level structure of Nd141 and Ce139 has been investigated by studying the decay of 20.9-min Pm141 produced via the Pr141(He3,3 n) reaction and the decay of 4.5-h Pr139 produced by the Pr140(, n)Pr139 reaction. For the Pm141 decay, singles and an ... Full text Cite

Angular correlation of x rays: L-M cascades of plutonium

Journal Article Physical Review A · January 1, 1975 Angular correlations between L and M x rays in Pu239 obtained from a radioactive source of 32-yr Cm243 were measured using Si(Li) and Ge(Li) detectors. The measured angular-correlation coefficients A22=(8.5±1.5)×10-2 for the Lβ1-M cascade and A22=(7.7±2.0) ... Full text Cite

Decay of 5.8-min Pmm140 and 10-sec Pmg140 to levels of Nd140

Journal Article Physical Review C · January 1, 1975 The nuclear level structure of Nd140 has been investigated by studying the decay of 5.8-min Pmm140 and 10-sec Pmg140 with Ge(Li) γ-ray detectors. Sources were produced via the Pr141(He3, 4n)) reaction. The study of Pmg140 decay utilized a helium-jet recoil ... Full text Cite

Comparison of techniques for the determination of the L2-L3X Coster-Kronig transition probability

Journal Article Physical Review A · January 1, 1975 The value of the Coster-Kronig transition probability for Z=73 has been determined by eight variations of the K-L x-ray coincidence technique. The effect of a correction for unwanted Lη-Kα2 coincidence events in the Lα-K coincidence spectrum is discussed. ... Full text Cite

Angular correlation between K and L x rays in tantalum

Journal Article Physical Review A · January 1, 1975 Angular correlations between K and L x rays in Ta obtained from the electron-capture decay of W181 were measured using two different experimental systems. High-resolution Si(Li) x-ray detectors were used to detect L x rays. K x rays were detected with a hi ... Full text Cite

Search for an anisotropy between Ll x rays and γ rays in the decay of Cm243

Journal Article Physical Review C · January 1, 1975 The anisotropy of Ll x rays and γ rays of Pu239 following the decay of Cm243 has been investigated. A Ge(Li) crystal with 250 eV resolution at 5.9 keV was used to detect Ll x rays. A NaI(T1) crystal was used to detect six γ rays between 210 and 285 keV. Th ... Full text Cite

Experimental determination of the L2-L3X Coster-Kronig transition probability in europium, plutonium, and curium

Journal Article Physical Review A · January 1, 1975 The L2-L3X Coster-Kronig transition probability for Z=63, 94, and 96 has been measured by the L-x-ray K-x-ray coincidence technique. The value measured in Eu63 was corrected for the presence of an unresolved L x-ray component in the L x-ray group. The valu ... Full text Cite

Measurement of the angular correlation between L-M X-ray cascades

Journal Article Physics Letters A · September 23, 1974 The angular correlation between Lβ1 and several M4 X-rays of plutonium has been measured with semiconductor detectors. The angular correlation coefficient obtained is A22 = (8.5 ± 1.5) × 10-2. This value is compared with theory. © 1974. ... Full text Cite

K-L X-ray angular correlations in Cm, Pu and Eu

Journal Article Phys. Rev. A, Gen. Phys. (USA) · 1974 Angular correlations between K and L X-rays in Cm, Pu, and Eu have been measured. Corrected angular correlation coefficients are tabulated. The results are compared with similar studies for other elements and with theoretical predictions ... Full text Link to item Cite

On-line determination of transport time of a helium-jet system

Journal Article Nucl. Instrum. Methods (Netherlands) · 1974 A rapid and accurate method for determining the recoil transport time of a helium-jet system by measuring the output activity ratio of two nuclides produced in a single charged particle bombardment with known cross-section is given. The minimum transport t ... Cite

On-line determination of transport time of a helium-jet system

Journal Article Nuclear Instruments and Methods · January 1, 1974 A rapid and accurate method for determining the recoil transport time of a helium-jet system by measuring the output activity ratio of two nuclides produced in a single charged particle bombardment with known cross-section is given. The minimum transport t ... Full text Cite

Measurement of the angular correlation between L-M X-ray cascades

Journal Article Phys. Lett. A (Netherlands) The angular correlation between Lβ1 and several M4 X-rays of plutonium has been measured with semiconductor detectors. The angular correlation coefficient obtained is A22=(8.5±1.5)×10-2. This value is compared with theory ... Cite