Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase

Yuli Xie, Yidong Liu, Gangli Gong, Alison Rinderspacher, Shi Xian Deng, Deborah H. Smith, Udo Toebben, Effie Tzilianos, Lars Branden, Dušica Vidović, Caty Chung, Stephan Schürer, Lutz Tautz, Donald W. Landry

Research output: Contribution to journalArticle

32 Scopus citations

Abstract

We report here a class of thiazolidine-2,4-diones and 2-thioxothiazolidin-4-ones as potent inhibitors of the lymphoid specific tyrosine phosphatase (Lyp) identified from high throughput screens. Chemical modification by incorporating the known phosphotyrosine (pTyr) mimics led to the discovery of a salicylate-based inhibitor with submicromolar potency.

Original languageEnglish (US)
Pages (from-to)2840-2844
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number9
DOIs
StatePublished - May 1 2008

Keywords

  • Lyp
  • Salicylate
  • Thiazolidine
  • pTyr mimics

ASJC Scopus subject areas

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

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  • Cite this

    Xie, Y., Liu, Y., Gong, G., Rinderspacher, A., Deng, S. X., Smith, D. H., Toebben, U., Tzilianos, E., Branden, L., Vidović, D., Chung, C., Schürer, S., Tautz, L., & Landry, D. W. (2008). Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase. Bioorganic and Medicinal Chemistry Letters, 18(9), 2840-2844. https://doi.org/10.1016/j.bmcl.2008.03.079