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

نویسندگان

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

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.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry

دوره 20 14  شماره 

صفحات  -

تاریخ انتشار 2012