Bioorthogonal Chemistry Approach for the Theranostics of GRPR-Expressing Cancers.

ABSTRACT: Several gastrin-releasing peptide receptor (GRPR) antagonists with improved in vivo behavior have been recently developed and tested in the clinic. However, despite the generally mild side effects of peptide receptor radionuclide therapy (PRRT), toxicity has been observed due to high doses delivered to nontarget tissues, especially in the kidneys and pancreas. Previous experiences with radiolabeled peptides opened a unique opportunity to explore GRPR pretargeting using clickable bombesin antagonists. Toward this goal, we used clickable DOTA-like radiocomplexes which have been previously evaluated by our group. We functionalized a potent GRPR antagonist with a clickable TCO moiety using two different linkers. These precursors were then studied to select the compound with the highest GRPR bi

SUBMITTER: D'Onofrio A 

PROVIDER: S-EPMC9785946 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature