Arylstibonic acids are potent and isoform-selective inhibitors of Cdc25a and Cdc25b phosphatases

Lok Hang Mak, Jessica Knott, Katherine A. Scott, Claire Scott, Gillian F. Whyte, Yu Ye, David J. Mann, Oscar Ces, James Stivers, Rudiger Woscholski

Research output: Contribution to journalArticlepeer-review

Abstract

Arylstibonates structurally resemble phosphotyrosine side chains in proteins and here we addressed the ability of such compounds to act as inhibitors of a panel of mammalian tyrosine and dual-specificity phosphatases. Two arylstibonates both possessing a carboxylate side chain were identified as potent inhibitors of the protein tyrosine phosphatase PTP-ß. In addition, they inhibited the dual-specificity, cell cycle regulatory phosphatases Cdc25a and Cdc25b with sub-micromolar potency. However, the Cdc25c phosphatase was not affected demonstrating that arylstibonates may be viable leads from which to develop isoform specific Cdc25 inhibitors.

Original languageEnglish (US)
Pages (from-to)4371-4376
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume20
Issue number14
DOIs
StatePublished - Jul 15 2012

Keywords

  • Arylstibonic acids
  • Cdc25 inhibitor
  • Protein tyrosine phosphatase

ASJC Scopus subject areas

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

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