A High-Affinity ⁶⁴Cu-Labeled Ligand for PET Imaging of Hepsin: Design, Synthesis, and Characterization.

ABSTRACT: Hepsin, a cell surface serine protease, is a potential biomarker for the detection of prostate cancer due to its high expression in prostate cancer but not in normal prostate. This study aimed to develop a radioligand for positron emission tomography (PET) imaging of hepsin. Six leucine-arginine (Leu-Arg) dipeptide derivatives (two diastereomers for each of three ligands) were synthesized and evaluated for their binding affinities and selectivity for hepsin. Based on the binding assay, a ^natCu-1,4,7,10-tetraazacyclododecane-N,N',N″,N‴-tetraacetic acid (DOTA)-conjugated ligand (3B) was selected for the development of a PET radioligand. [⁶⁴Cu]3B was synthesized by labeling the DOTA-conjugated compound 11B with [⁶⁴

SUBMITTER: Park JH 

PROVIDER: S-EPMC9503212 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature