Arylstibonic acids are potent and isoform-selective inhibitors of Cdc25a and Cdc25b phosphatases |
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Authors: | Mak Lok Hang Knott Jessica Scott Katherine A Scott Claire Whyte Gillian F Ye Yu Mann David J Ces Oscar Stivers James Woscholski Rudiger |
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Institution: | Department of Chemistry, Imperial College London, Exhibition Road, London SW7 2AZ, UK. |
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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. |
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