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Bioorg Med Chem. 2012 Jul 15;20(14):4371-6. doi: 10.1016/j.bmc.2012.05.040. Epub 2012 May 24.

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

Author information

1
Department of Chemistry, Imperial College London, Exhibition Road, London SW7 2AZ, UK.

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.

PMID:
22705189
PMCID:
PMC3389297
DOI:
10.1016/j.bmc.2012.05.040
[Indexed for MEDLINE]
Free PMC Article

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