⁶⁸Ga-Labeled [Thz¹⁴]Bombesin(7-14) Analogs: Promising GRPR-Targeting Agonist PET Tracers with Low Pancreas Uptake.

ABSTRACT: With overexpression in various cancers, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer imaging and therapy. However, the high pancreas uptake of reported GRPR-targeting radioligands limits their clinical application. Our goal was to develop ⁶⁸Ga-labeled agonist tracers for detecting GRPR-expressing tumors with positron emission tomography (PET), and compare them with the clinically validated agonist PET tracer, [⁶⁸Ga]Ga-AMBA. Ga-TacBOMB2, TacBOMB3, and TacBOMB4, derived from [Thz¹⁴]Bombesin(7-14), were confirmed to be GRPR agonists by a calcium mobilization study, and their binding affinities (K_i(GRPR)) were determined to be 7.62 ± 0.19, 6.02 ± 0.59, and 590 ± 36.5 nM, respectively, via in vitro competition binding

SUBMITTER: Wang L 

PROVIDER: S-EPMC9962964 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature