Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists

Sarah C. Archibald, John C. Head, Neil Gozzard, David W. Howat, Ted A.H. Parton, John R. Porter, Martyn K. Robinson, Anthony Shock, Graham J. Warrellow, William M. Abraham

Research output: Contribution to journalArticle

25 Scopus citations

Abstract

Using disulphide cysteine-based inhibitors as lead structures, this communication describes our strategy for identifying more stable, potent antagonists of the α4β1 integrin. These studies ultimately discovered potent, low molecular weight inhibitors based on D-thioproline-L-tyrosine. (C) 2000 Elsevier Science Ltd. All rights reserved.

Original languageEnglish (US)
Pages (from-to)997-999
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume10
Issue number9
DOIs
StatePublished - May 1 2000

ASJC Scopus subject areas

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

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    Archibald, S. C., Head, J. C., Gozzard, N., Howat, D. W., Parton, T. A. H., Porter, J. R., Robinson, M. K., Shock, A., Warrellow, G. J., & Abraham, W. M. (2000). Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists. Bioorganic and Medicinal Chemistry Letters, 10(9), 997-999. https://doi.org/10.1016/S0960-894X(00)00147-5