Synthesis and Evaluation of Novel ⁶⁸Ga-Labeled [D-Phe⁶,Leu¹³ψThz¹⁴]bombesin(6-14) Analogs for Cancer Imaging with Positron Emission Tomography.

ABSTRACT: Gastrin-releasing peptide receptor (GRPR) is overexpressed in various cancers and is a promising target for cancer diagnosis and therapy. However, the high pancreas uptake and/or metabolic instability observed for most reported GRPR-targeted radioligands might limit their clinical applications. Our group recently reported a GRPR-targeted antagonist tracer, [⁶⁸Ga]Ga-TacsBOMB2 ([⁶⁸Ga]Ga-DOTA-Pip-D-Phe⁶-Gln⁷-Trp⁸-Ala⁹-Val¹⁰-Gly¹¹-His¹²-Leu¹³ψThz¹⁴-NH₂), which showed a minimal pancreas uptake in a preclinical mouse model. In this study, we synthesized four derivatives with unnatural amino acid substitutions (Tle¹⁰-derived Ga-LW01158, NMe-His¹²

SUBMITTER: Wang L 

PROVIDER: S-EPMC11124507 | biostudies-literature | 2024 May

REPOSITORIES: biostudies-literature