Synthesis and biological characterization of SQBAzide, a novel biotinylated photoaffinity probe for the study of the human platelet thromboxane A(2) receptor

Authors
Halmos, T Turek, JW Le Breton, GC Antonakis, K
Citation
T. Halmos et al., Synthesis and biological characterization of SQBAzide, a novel biotinylated photoaffinity probe for the study of the human platelet thromboxane A(2) receptor, BIOORG MED, 9(20), 1999, pp. 2963-2968
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
20
Year of publication
1999
Pages
2963 - 2968
Database
ISI
SICI code
0960-894X(19991018)9:20<2963:SABCOS>2.0.ZU;2-M
Abstract
SQBAzide, a biotinylated, azido derivative of the TXA(2) receptor antagonis t, SQ31,491, was synthesized and characterized. The compound specifically i nhibited human platelet aggregation mediated by TXA(2) receptor activation and irreversibly labeled platelet TXA(2) receptors upon exposure to ultravi olet light. This probe should prove to be of significant value for the stud y of the receptor-ligand binding domain. (C) 1999 Elsevier Science Ltd. All rights reserved.