Synthesis and Preclinical Evaluation of a Bispecific PSMA-617/RM2 Heterodimer Targeting Prostate Cancer.

ABSTRACT: Prostate-specific membrane antigen (PSMA) and gastrin-releasing peptide receptor (GRPR) have been used for diagnostic molecular imaging/therapy of prostate cancer (PCa). To address tumor heterogeneity, we synthesized and evaluated a bispecific PSMA/GRPR ligand (3) combining PSMA-617 (1) and the GRPR antagonist RM2 (2) with the radiometal chelator DOTA. 3 was radiolabeled with ⁶⁸Ga ([⁶⁸Ga]Ga-3) and ¹⁷⁷Lu ([¹⁷⁷Lu]Lu-3). [⁶⁸Ga]Ga-3 was tested in the following PCa cell lines for receptor affinity, time kinetic cell-binding/specificity, and cell-internalization: PC-3 and LNCaP. Compared to the monomers (1 and 2), ligand 3 showed specific cell binding, similar receptor aff

SUBMITTER: Liolios C 

PROVIDER: S-EPMC11571012 | biostudies-literature | 2024 Nov

REPOSITORIES: biostudies-literature