Author/Authors :
Andrew J. Souers، نويسنده , , Alex A. Virgilio، نويسنده , , Stephan S. Schürer، نويسنده , , Jonathan A. Ellman، نويسنده , , Timothy P. Kogan، نويسنده , , Henry E. West، نويسنده , , Wendy Ankener and، نويسنده , , Peter Vanderslice، نويسنده ,
Abstract :
A library of 2302 small molecule β-turn mimetics was screened for inhibition of the α4β1 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 μM, and 2, IC50 = 8 μM) to be reported for this class of integrins.