NOVEL INHIBITORS OF ALPHA-4-BETA-1 INTEGRIN RECEPTOR INTERACTIONS THROUGH LIBRARY SYNTHESIS AND SCREENING

Authors
SOUERS AJ VIRGILIO AA SCHURER SS ELLMAN JA KOGAN TP WEST HE ANKENER W VANDERSLICE P
Citation
Aj. Souers et al., NOVEL INHIBITORS OF ALPHA-4-BETA-1 INTEGRIN RECEPTOR INTERACTIONS THROUGH LIBRARY SYNTHESIS AND SCREENING, Bioorganic & medicinal chemistry letters, 8(17), 1998, pp. 2297-2302
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
17
Year of publication
1998
Pages
2297 - 2302
Database
ISI
SICI code
0960-894X(1998)8:17<2297:NIOAIR>2.0.ZU;2-W
Abstract
A library of 2302 small molecule beta-turn mimetics was screened for i nhibition of the alpha 4 beta 1 integrin-CS1 splice variant binding in teraction. Preliminary data revealed several active ligands, and valid ation with purified material culminated in the identification of some of the first small molecule ligands (1, IC50 = 5 mu M, and 2, IC50 = 8 mu M) to be reported for this class of integrins. (C) 1998 Elsevier S cience Ltd. All rights reserved.