Design, Synthesis, and Evaluation of a New Chemotype Fluorescent Ligand for the P2Y₂ Receptor.

ABSTRACT: The P2Y₂ receptor (P2Y₂R) is a target for diseases including cancer, idiopathic pulmonary fibrosis, and atherosclerosis. However, there are insufficient P2Y₂R antagonists available for validating P2Y₂R function and future drug development. Evaluation of how (R)-5-(7-chloro-2-((2-ethoxyethyl)amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-1-methyl-4-thioxo-3,4-dihydropyrimidin-2(1H)-one, a previously published thiazole-based analogue of AR-C118925, binds in a P2Y₂R homology model was used to design new P2Y₂R antagonist scaffolds. One P2Y₂R antagonist scaffold retained millimolar affinity for the P2Y₂R and upon further functionalization with terminal carboxylic acid groups a

SUBMITTER: Knight R 

PROVIDER: S-EPMC11247638 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature