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

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

Research output: Contribution to journalArticle

54 Citations (Scopus)

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

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Integrins
Inhibitory Concentration 50
Screening
Small Molecule Libraries
Ligands
Molecules

ASJC Scopus subject areas

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

Cite this

Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening. / Souers, Andrew J.; Virgilio, Alex A.; Schuerer, Stephan C; Ellman, Jonathan A.; Kogan, Timothy P.; West, Henry E.; Ankener, Wendy; Vanderslice, Peter.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 8, No. 17, 08.09.1998, p. 2297-2302.

Research output: Contribution to journalArticle

Souers, Andrew J. ; Virgilio, Alex A. ; Schuerer, Stephan C ; Ellman, Jonathan A. ; Kogan, Timothy P. ; West, Henry E. ; Ankener, Wendy ; Vanderslice, Peter. / Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening. In: Bioorganic and Medicinal Chemistry Letters. 1998 ; Vol. 8, No. 17. pp. 2297-2302.
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