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Trithiols and their arsenic compounds for potential use in diagnostic and therapeutic radiopharmaceuticals.

Publication ,  Journal Article
DeGraffenreid, AJ; Feng, Y; Barnes, CL; Ketring, AR; Cutler, CS; Jurisson, SS
Published in: Nucl Med Biol
May 2016

INTRODUCTION: Arsenic-72 ((72)As; 2.49MeV β(+), 26h) and (77)As (0.683MeV β(-), 38.8h) have nuclear properties useful for positron emission tomography (PET) and radiotherapy applications, respectively. Their half-lives are sufficiently long for targeting tumors with antibodies, as well as peptides. Potential radiopharmaceuticals based on radioarsenic require development of suitable bifunctional chelates for stable conjugation of arsenic to vectors under in vivo conditions at high dilution. METHODS: The thiophilic nature of arsenic led to the synthesis and characterization of a simple trithiol ligand and its arsenic complex, and radiolabeling studies at the no carrier added (NCA) (77)As level. RESULTS: (1)H- and (13)C-NMR spectroscopy, electrospray ionization mass spectrometry (ESI-MS), and single crystal X-ray diffraction were used to characterize the trithiol ligand and its arsenic(III) complex. Radiotracer studies with no carrier added (NCA) (77)As resulted in high radiolabeling yields (>96%) with high in vitro stability. CONCLUSIONS: The high yield and stability of a single NCA (77)As trithiol complex indicates that this framework is suitable for developing matched pair agents for non-invasive in vivo PET imaging and radiotherapy of tumors with (72,77)As. This is the first reported chelate developed for NCA radioarsenic and studies are underway for developing a trithiol bifunctional chelate conjugated to a targeting vector, such as a peptide or monoclonal antibody.

Duke Scholars

Published In

Nucl Med Biol

DOI

EISSN

1872-9614

Publication Date

May 2016

Volume

43

Issue

5

Start / End Page

288 / 295

Location

United States

Related Subject Headings

  • Temperature
  • Sulfhydryl Compounds
  • Radiotherapy
  • Radiopharmaceuticals
  • Radiochemistry
  • Positron-Emission Tomography
  • Nuclear Medicine & Medical Imaging
  • Molecular Conformation
  • Models, Molecular
  • Drug Stability
 

Citation

APA
Chicago
ICMJE
MLA
NLM
DeGraffenreid, A. J., Feng, Y., Barnes, C. L., Ketring, A. R., Cutler, C. S., & Jurisson, S. S. (2016). Trithiols and their arsenic compounds for potential use in diagnostic and therapeutic radiopharmaceuticals. Nucl Med Biol, 43(5), 288–295. https://doi.org/10.1016/j.nucmedbio.2016.01.005
DeGraffenreid, Anthony J., Yutian Feng, Charles L. Barnes, Alan R. Ketring, Cathy S. Cutler, and Silvia S. Jurisson. “Trithiols and their arsenic compounds for potential use in diagnostic and therapeutic radiopharmaceuticals.Nucl Med Biol 43, no. 5 (May 2016): 288–95. https://doi.org/10.1016/j.nucmedbio.2016.01.005.
DeGraffenreid AJ, Feng Y, Barnes CL, Ketring AR, Cutler CS, Jurisson SS. Trithiols and their arsenic compounds for potential use in diagnostic and therapeutic radiopharmaceuticals. Nucl Med Biol. 2016 May;43(5):288–95.
DeGraffenreid, Anthony J., et al. “Trithiols and their arsenic compounds for potential use in diagnostic and therapeutic radiopharmaceuticals.Nucl Med Biol, vol. 43, no. 5, May 2016, pp. 288–95. Pubmed, doi:10.1016/j.nucmedbio.2016.01.005.
DeGraffenreid AJ, Feng Y, Barnes CL, Ketring AR, Cutler CS, Jurisson SS. Trithiols and their arsenic compounds for potential use in diagnostic and therapeutic radiopharmaceuticals. Nucl Med Biol. 2016 May;43(5):288–295.
Journal cover image

Published In

Nucl Med Biol

DOI

EISSN

1872-9614

Publication Date

May 2016

Volume

43

Issue

5

Start / End Page

288 / 295

Location

United States

Related Subject Headings

  • Temperature
  • Sulfhydryl Compounds
  • Radiotherapy
  • Radiopharmaceuticals
  • Radiochemistry
  • Positron-Emission Tomography
  • Nuclear Medicine & Medical Imaging
  • Molecular Conformation
  • Models, Molecular
  • Drug Stability