A New, Second Generation Trithiol Bifunctional Chelate
for 72,77As: Trithiol(b)-(Ser)2‑RM2
Posted on 2021-01-11 - 06:13
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.
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Najafi Khosroshahi, Firouzeh; Feng, Yutian; Ma, Li; Manring, Simon; Rold, Tammy L.; Gallazzi, Fabio A.; et al. (2021). A New, Second Generation Trithiol Bifunctional Chelate
for 72,77As: Trithiol(b)-(Ser)2‑RM2. ACS Publications. Collection. https://doi.org/10.1021/acs.bioconjchem.0c00658
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AUTHORS (11)
- FNFirouzeh Najafi KhosroshahiYFYutian FengLMLi MaSMSimon ManringTRTammy L. RoldFGFabio A. GallazziSKSteven P. KelleyMEMary F. EmbreeHHHeather M. HennkensTHTimothy J. HoffmanSJSilvia S. Jurisson
