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Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening
A J Souers1, A A Virgilio, S S Schürer
1Department of Chemistry, University of California, Berkeley 94720, USA.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
Abstract:
A library of 2302 small molecule beta-turn mimetics was screened for inhibition of the alpha 4 beta 1 integrin-CS1 splice variant binding interaction. Preliminary data revealed several active ligands, and validation with purified material culminated in the identification of some of the first small molecule ligands (1, IC50 = 5 microM, and 2, IC50 = 8 microM) to be reported for this class of integrins.