Scholars@Duke
Ganesan Vaidyanathan

Ganesan Vaidyanathan

Professor Emeritus in Radiology
Radiology
vaidy001@mc.duke.edu
Box 3808 Med Ctr, Radiology, Durham, NC 27710
161C 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

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

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

Preclinical Development of [211At]meta- astatobenzylguanidine ([211At]MABG) as an Alpha Particle Radiopharmaceutical Therapy for Neuroblastoma.

Journal Article Clin Cancer Res · September 15, 2022 PURPOSE: [131I]meta-iodobenzylguanidine ([131I]MIBG) is a targeted radiotherapeutic administered systemically to deliver beta particle radiation in neuroblastoma. However, relapses in the bone marrow are common. [211At]meta-astatobenzylguanidine ([211At] M ... Full text 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

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

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

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

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

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

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

Preclinical Development of [211At]meta- astatobenzylguanidine ([211At]MABG) as an Alpha Particle Radiopharmaceutical Therapy for Neuroblastoma.

Journal Article Clin Cancer Res · September 15, 2022 PURPOSE: [131I]meta-iodobenzylguanidine ([131I]MIBG) is a targeted radiotherapeutic administered systemically to deliver beta particle radiation in neuroblastoma. However, relapses in the bone marrow are common. [211At]meta-astatobenzylguanidine ([211At] M ... Full text 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

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

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

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

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

PSMA-targeted alpha therapeutic agent with fast kidney clearance

Conference JOURNAL OF NUCLEAR MEDICINE · May 1, 2019 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

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

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

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

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

(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

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

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

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 1610: Development of meta-[211At]astatobenzylguanidine ([211At]MABG) as an alpha particle emitting systemic targeted radiotherapeutic for neuroblastoma

Conference Cancer Research · August 1, 2015 AbstractBACKGROUND Neuroblastoma (NB) is a radiosensitive malignancy and NB cells express the norepinephrine transporter (NET) enabling uptake of NET ligands. The majority of relapsed NBs remain sensitive to ... Full text 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

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

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

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

Synthesis and evaluation of 18F-labeled benzylguanidine analogs for targeting the human norepinephrine transporter.

Journal Article Eur J Nucl Med Mol Imaging · February 2014 PURPOSE: Both (131)I- and (123)I-labeled meta-iodobenzylguanidine (MIBG) have been widely used in the clinic for targeted imaging of the norepinephrine transporter (NET). The human NET (hNET) gene has been imaged successfully with (124)I-MIBG positron emis ... 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

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

A radioisotope based methodology for plant-fungal interactions in the rhizosphere

Journal Article IEEE Nuclear Science Symposium Conference Record · January 1, 2013 In plant ecophysiology research there is interest in studying the biology of the rhizosphere because of its importance in plant nutrient-interactions. The rhizosphere is the zone of soil surrounding a plant's root system where microbes (such as fungi) are ... Full text Cite

Targeting breast carcinoma with radioiodinated anti-HER2 Nanobody.

Journal Article Nucl Med Biol · January 2013 Featured Publication 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 Featured Publication 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

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

Journal Article EJNMMI Res · October 29, 2012 Featured Publication 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

TARGETED ALPHA THERAPY

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

Synthesis and preliminary evaluation of n.c.a. iodoquine: a novel radiotracer with high uptake in cells with high ALDH1 expression.

Journal Article Curr Radiopharm · January 2012 Featured Publication PURPOSE: Chloroquine has demonstrated high affinity for aldehyde dehydrogenase 1A1 (ALDH1), an enzyme expressed in the highly tumorigenic CD133+ brain tumor initiating subpopulation. The purpose of this study is to report the novel synthesis of a chloroqui ... Full text Link to item Cite

Virus hunters: catching bugs in the field.

Journal Article Cell · December 9, 2011 Densely populated areas in rural China require constant vigilance and state-of-the-art technology to stop new pandemics in their tracks. Hurdles are not only scientific in some parts of the developing world. ... Full text Link to item Cite

Dam controversy: Remaking the Mekong.

Journal Article Nature · October 19, 2011 Full text Link to item Cite

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

Journal Article Curr Radiopharm · October 2011 Featured Publication 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 Featured Publication 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

Apes in Africa: The cultured chimpanzees.

Journal Article Nature · August 17, 2011 Full text Link to item Cite

Clinical spectrum and prognosis of follicular lymphoma with blastoid transformation: case series and a review of the literature.

Journal Article Ann Hematol · August 2011 Follicular lymphoma (FL) with blastoid transformation (FL-BT) is a rare entity. FL-BT has a dismal prognosis due to intrinsic biological characteristics, lack of evidence-based therapeutic guidelines, and exclusion from clinical trials. In order to underst ... Full text Link to item Cite

Science in Africa: The wheat stalker.

Journal Article Nature · June 29, 2011 Full text Link to item Cite

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

Journal Article Nucl Med Biol · January 2011 Featured Publication 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 Featured Publication 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 Featured Publication 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 Featured Publication 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

A case of curative-intent hepatectomy for colon cancer metastatic to the scapula and liver.

Journal Article Anticancer Res · February 2010 Colon cancer is the second leading cause of cancer death in the United States. Patients with colon cancer metastatic to liver and bone are deemed non-curable and have a poor prognosis. We present a case of recurrent colon cancer with synchronous hepatic an ... Link to item Cite

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

Journal Article Curr Radiopharm · 2010 Featured Publication 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

Stop and go FOLFOX plus bevacizumab chemotherapy in the first-line treatment of metastatic colorectal cancer.

Journal Article Oncology · 2010 BACKGROUND: Infusional 5-fluorouracil, leucovorin and oxaliplatin (FOLFOX) plus bevacizumab chemotherapy is commonly implemented in the first-line treatment of metastatic colorectal cancer. A stop and go oxaliplatin strategy has been recommended to reduce ... Full text Link to item Cite

Targeting aldehyde dehydrogenase: a potential approach for cell labeling.

Journal Article Nucl Med Biol · November 2009 Featured Publication 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

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 Featured Publication 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 Featured Publication 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

Radiation dose estimates of [125I] and [131I] – iodoquine, a putative radiotracer targeting cells with high ALDH expression

Conference Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2009 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 Featured Publication 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

DOTA-SIB, A TRIFUNCTIONAL PROSTHETIC GROUP FOR MULTI-MODAL LABELING

Journal Article JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS · January 1, 2009 Link to item Cite

Meta-iodobenzylguanidine and analogues: chemistry and biology.

Journal Article Q J Nucl Med Mol Imaging · December 2008 Featured Publication Meta-iodobenzylguanidine (MIBG) is a structural analogue of the neurotransmitter norepinephrine (NE) and is taken up by cells rich in sympathetic neurons by an active uptake process mediated by the NE transporter, which is referred to as uptake-1. It is a ... Link to item Cite

Practical outcomes of applying ensemble machine learning classifiers to High-Throughput Screening (HTS) data analysis and screening.

Journal Article J Chem Inf Model · November 2008 Over the years numerous papers have presented the effectiveness of various machine learning methods in analyzing drug discovery biological screening data. The predictive performance of models developed using these methods has traditionally been evaluated b ... Full text Link to item Cite

TMPRSS2-ERG fusion, a common genomic alteration in prostate cancer activates C-MYC and abrogates prostate epithelial differentiation.

Journal Article Oncogene · September 11, 2008 The high prevalence of TMPRSS2-ERG rearrangements ( approximately 60%) in prostate cancer (CaP) leads to androgenic induction of the ETS-related gene (ERG) expression. However, the biological functions of ERG overexpression in CaP remain to be understood. ... 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 Featured Publication 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 Featured Publication 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

Comparative study of machine-learning and chemometric tools for analysis of in-vivo high-throughput screening data.

Journal Article J Chem Inf Model · August 2008 High-throughput screening (HTS) has become a central tool of many pharmaceutical and crop-protection discovery operations. If HTS screening is carried out at the level of the intact organism, as is commonly done in crop protection, this strategy has the po ... Full text Link to item Cite

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

Journal Article Nucl Med Biol · October 2007 Featured Publication 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

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

Journal Article Bioorg Med Chem · May 15, 2007 Featured Publication 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

Identification and biochemical studies on novel non-nucleoside inhibitors of the enzyme adenosine kinase.

Journal Article Protein J · April 2007 The enzyme adenosine kinase (AK) plays a key role in the regulation of intracellular and extracellular concentration of adenosine (Ado), which exhibits potent hormonal activity in cardiovascular, nervous and immune systems. In view of the pharmacological e ... Full text 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 Featured Publication 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 Featured Publication 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 Featured Publication 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

Targeted drug delivery for neuroblastoma using MIBG.

Conference CANCER RESEARCH · April 1, 2006 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 Featured Publication 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

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

Journal Article Nat Protoc · 2006 Featured Publication 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 Featured Publication 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 Featured Publication 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 Featured Publication 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 Featured Publication 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

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 Featured Publication 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

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

Journal Article Appl Radiat Isot · March 2005 Featured Publication 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

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

Journal Article Peptides · December 2004 Featured Publication 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

Astatine-211 Labeled Radiopharmaceuticals, invited

Journal Article Transactions of the American Nuclear Society · December 1, 2004 Featured Publication 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 Featured Publication 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 Featured Publication 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

A validated chiral HPLC method for the enantiomeric separation of tolterodine tartarate.

Journal Article J Pharm Biomed Anal · September 3, 2004 An isocratic chiral HPLC method was developed for the separation of tolterodine tartarate enantiomers. The mobile phase consists of n-hexane and isopropyl alcohol in the ratio of 980:20 (v/v) with 1 ml diethylamine and 0.6 ml trifluoroacetic acid. Chiralce ... 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 Featured Publication 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

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 Featured Publication 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

The Ras-related protein AGS1/RASD1 suppresses cell growth.

Journal Article Oncogene · July 29, 2004 AGS1/RASD1 is a Ras-related protein identified as a dexamethasone-inducible cDNA and as a signal regulator in various functional and protein-interaction screens. As an initial approach to define the role of AGS1/RASD1 as a Ras-family member, we determined ... Full text Link to item Cite

InfoEvolve: moving from data to knowledge using information theory and genetic algorithms.

Journal Article Ann N Y Acad Sci · May 2004 InfoEvolve is a unified suite of data mining and empirical modeling tools capable of discovering low-bias and low-variance solutions to complex processes. The method is based on a common set of principles involving information theory and genetic algorithms ... Full text Link to item Cite

Meta-iodobenzylguanidine derivatives containing a second guanidine moiety.

Journal Article Bioorg Med Chem · April 1, 2004 Featured Publication 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 Featured Publication 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 Featured Publication 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

A validated LC method for imatinib mesylate.

Journal Article J Pharm Biomed Anal · December 4, 2003 An isocratic reversed-phase liquid chromatography method with UV detection has been developed for the purity evaluation of imatinib mesylate in bulk drug. The method is selective and is capable of detecting all process intermediates and other related compo ... Full text Link to item Cite

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

Journal Article Clin Cancer Res · May 2003 Featured Publication 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 Featured Publication 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

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 Featured Publication 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

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 Featured Publication 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

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

Journal Article Bioconjug Chem · 2001 Featured Publication 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 Featured Publication 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 Featured Publication 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

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

Journal Article Curr Pharm Des · September 2000 Featured Publication 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 and astatination of octreotide by conjugation labeling.

Journal Article Nucl Med Biol · May 2000 Featured Publication 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

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

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 Featured Publication 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

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

Octreotide analogues labeled with radioiodine and astatine-211

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

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 Featured Publication 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 Featured Publication 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

Targeted therapy using astatinated radiopharmaceuticals.

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

Delivery of antisense oligonucleotides using HPMA polymer: synthesis of A thiol polymer and its conjugation to water-soluble molecules.

Journal Article Bioconjug Chem · 1998 Here, we report the synthesis and characterization of an HPMA-based polymer for use as a carrier for the delivery of water soluble drugs. The polymer contains active-sulfhydryl groups for coupling of ligands through a disulfide linkage. The polymer can als ... 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 Featured Publication 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 Featured Publication 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

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

Journal Article Int J Radiat Biol · July 1997 Featured Publication 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

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

Journal Article Nucl Med Biol · February 1997 Featured Publication 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 Featured Publication 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

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 Featured Publication 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

Targeted therapy using alpha emitters.

Journal Article Phys Med Biol · October 1996 Featured Publication 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

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

Journal Article Nucl Med Biol · August 1996 Featured Publication 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

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 Featured Publication 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

Iodine-120-mIBG: Production and NCA labelling of a new PET radiotracer.

Journal Article JOURNAL OF NUCLEAR MEDICINE · May 1, 1996 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 Featured Publication 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

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

Journal Article Bioconjug Chem · 1996 Featured Publication 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

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 Featured Publication 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 Featured Publication 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

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

Journal Article J Nucl Med · April 1995 Featured Publication 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 Featured Publication 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 Featured Publication 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 Featured Publication 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 Featured Publication 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

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

Journal Article Nucl Med Biol · January 1995 Featured Publication 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

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

Journal Article Cancer Res · October 15, 1994 Featured Publication 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 Featured Publication 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 Featured Publication 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

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

Journal Article Int J Cancer · June 15, 1994 Featured Publication 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

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

Journal Article Nucl Med Commun · April 1994 Featured Publication 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

Preparation and screening of an arrayed human genomic library generated with the P1 cloning system.

Journal Article Proc Natl Acad Sci U S A · March 29, 1994 We describe here the construction and initial characterization of a 3-fold coverage genomic library of the human haploid genome that was prepared using the bacteriophage P1 cloning system. The cloned DNA inserts were produced by size fractionation of a Sau ... 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 Featured Publication 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 Featured Publication 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

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

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

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

Measuring astatine-211 distributions with SPECT.

Journal Article Phys Med Biol · August 1993 Featured Publication 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

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

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

Journal Article Appl Radiat Isot · March 1993 Featured Publication 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 Featured Publication 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

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

Journal Article J Nucl Med · August 1992 Featured Publication 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 Featured Publication 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

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

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

Aromatic acylation reagents for use in the radioiodination of proteins

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

RADIOIODINATION AND ASTATINATION OF MONOCLONAL-ANTIBODIES

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

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

Journal Article Bioconjug Chem · 1990 Featured Publication 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 Featured Publication 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

Reaction of Cyclopropanamines with Hypochlorite

Journal Article Journal of Organic Chemistry · April 1, 1989 Featured Publication Ethylene was formed in 65% yield when l-(l-piperidino)cyclopropanol, 6, was treated with hypochlorite. This observation raised the possibility that 1-aminocyclopropanecarboxylic acids (ACCs) could yield ethylene by a mechanism that involves (1) decarboxyla ... Full text Cite

Decarboxylation of 1-Aminocyclopropanecarboxylic Acid and Its Derivatives

Journal Article Journal of Organic Chemistry · April 1, 1989 Featured Publication The question of whether the title compounds could be decarboxylated to cyclopropanone derivatives was answered in the affirmative by the following observations. (1) Compound 11a was decarboxylated by 1,2,3-indantrione in acetonitrile, benzene, or methanol. ... Full text Cite