A New, Second Generation Trithiol Bifunctional Chelate for 72,77As: Trithiol(b)-(Ser)2-RM2.

Journal Article (Journal Article)

Trithiol chelates are suitable for labeling radioarsenic (72As: 2.49 MeV β+, 26 h; 77As: 0.683 MeV β-, 38.8 h) to form potential theranostic radiopharmaceuticals for positron emission tomography (PET) imaging and therapy. A trithiol(b)-(Ser)2-RM2 bioconjugate and its arsenic complex were synthesized and characterized. The trithiol(b)-(Ser)2-RM2 bioconjugate was radiolabeled with no-carrier-added 77As in over 95% radiochemical yield and was stable for over 48 h, and in vitro IC50 cell binding studies of [77As]As-trithiol(b)-(Ser)2-RM2 in PC-3 cells demonstrated high affinity for the gastrin-releasing peptide (GRP) receptor (low nanomolar range). Limited biodistribution studies in normal mice were performed with HPLC purified 77As-trithiol(b)-(Ser)2-RM2 demonstrating both pancreatic uptake and hepatobiliary clearance.

Full Text

Duke Authors

Cited Authors

  • Najafi Khosroshahi, F; Feng, Y; Ma, L; Manring, S; Rold, TL; Gallazzi, FA; Kelley, SP; Embree, MF; Hennkens, HM; Hoffman, TJ; Jurisson, SS

Published Date

  • July 21, 2021

Published In

Volume / Issue

  • 32 / 7

Start / End Page

  • 1364 - 1373

PubMed ID

  • 33423467

Electronic International Standard Serial Number (EISSN)

  • 1520-4812

Digital Object Identifier (DOI)

  • 10.1021/acs.bioconjchem.0c00658


  • eng

Conference Location

  • United States