A Structure-Activity Relationship Study of Bimodal BODIPY-Labeled PSMA-Targeting Bioconjugates.

ABSTRACT: The aim of this study was to identify a high-affinity BODIPY peptidomimetic that targets the prostate-specific membrane antigen (PSMA) as a potential bimodal imaging probe for prostate cancer. For the structure-activity study, several BODIPY (difluoroboron dipyrromethene) derivatives with varying spacers between the BODIPY dye and the PSMA Glu-CO-Lys binding motif were prepared. Corresponding affinities were determined by competitive binding assays in PSMA-positive LNCaP cells. One compound was identified with comparable affinity (IC₅₀ =21.5±0.1 nM) to Glu-CO-Lys-Ahx-HBED-CC (PSMA-11) (IC₅₀ =18.4±0.2 nM). Radiolabeling was achieved by Lewis-acid-mediated ¹⁹ F/¹⁸ F exchange in moderate molar activities (∼0.7 MBq nmol^-1 ) and high radioc

SUBMITTER: Stemler T 

PROVIDER: S-EPMC8453963 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature