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

Andrew J. Souers, Alex A. Virgilio, Stephan S. Schürer, Jonathan A. Ellman, Timothy P. Kogan, Henry E. West, Wendy Ankener, Peter Vanderslice

Research output: Contribution to journalArticle

54 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)2297-2302
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number17
DOIs
StatePublished - Sep 8 1998
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    Souers, A. J., Virgilio, A. A., Schürer, S. S., Ellman, J. A., Kogan, T. P., West, H. E., Ankener, W., & 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