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 Citations (Scopus)

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

Fingerprint

Integrins
Disulfides
Cysteine
Tyrosine
Molecular Weight
Molecular weight
Communication
thiazolidine-4-carboxylic acid

ASJC Scopus subject areas

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

Cite this

Archibald, S. C., Head, J. C., Gozzard, N., Howat, D. W., Parton, T. A. H., Porter, J. R., ... 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

Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists. / Archibald, Sarah C.; Head, John C.; Gozzard, Neil; Howat, David W.; Parton, Ted A H; Porter, John R.; Robinson, Martyn K.; Shock, Anthony; Warrellow, Graham J.; Abraham, William M.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 10, No. 9, 01.05.2000, p. 997-999.

Research output: Contribution to journalArticle

Archibald, SC, Head, JC, Gozzard, N, Howat, DW, Parton, TAH, Porter, JR, Robinson, MK, Shock, A, Warrellow, GJ & Abraham, WM 2000, 'Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 10, no. 9, pp. 997-999. https://doi.org/10.1016/S0960-894X(00)00147-5
Archibald, Sarah C. ; Head, John C. ; Gozzard, Neil ; Howat, David W. ; Parton, Ted A H ; Porter, John R. ; Robinson, Martyn K. ; Shock, Anthony ; Warrellow, Graham J. ; Abraham, William M. / Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists. In: Bioorganic and Medicinal Chemistry Letters. 2000 ; Vol. 10, No. 9. pp. 997-999.
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