Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening

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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.

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Souers, A. J., Virgilio, A. A., Schürer, S. S., Ellman, J. A., Kogan, T. P., West, H. E., … Vanderslice, P. (1998). Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening. Bioorganic and Medicinal Chemistry Letters, 8(17), 2297–2302. https://doi.org/10.1016/S0960-894X(98)00416-8

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