Synthesis and biological characterization of AQPazide, a novel biotinylated photoaffinity probe for the study of the human platelet throm☐ ane A 2 receptor

…, JW Turek, GC Le Breton, K Antonakis

Index: Halmos, Therese; Turek, Joseph W.; Le Breton, Guy C.; Antonakis, Kostas Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 20 p. 2963 - 2968

Full Text: HTML

Citation Number: 9

Abstract

SQBAzide, a biotinylated, azido derivative of the TXA2 receptor antagonist, SQ31, 491, was synthesized and characterized. The compound specifically inhibited human platelet aggregation mediated by TXA2 receptor activation and irreversibly labeled platelet TXA2 receptors upon exposure to ultraviolet light. This probe should prove to be of significant value for the study of the receptor-ligand binding domain.