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Arylstibonic acids are potent and isoform-selective inhibitors of Cdc25a and Cdc25b phosphatases.
Mak, Lok Hang; Knott, Jessica; Scott, Katherine A; Scott, Claire; Whyte, Gillian F; Ye, Yu; Mann, David J; Ces, Oscar; Stivers, James; Woscholski, Rudiger.
Afiliação
  • Mak LH; Department of Chemistry, Imperial College London, Exhibition Road, London SW7 2AZ, UK.
Bioorg Med Chem ; 20(14): 4371-6, 2012 Jul 15.
Article em En | MEDLINE | ID: mdl-22705189
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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos Organometálicos / Propionatos / Fosfatases cdc25 / Inibidores Enzimáticos / Antimônio Idioma: En Ano de publicação: 2012 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos Organometálicos / Propionatos / Fosfatases cdc25 / Inibidores Enzimáticos / Antimônio Idioma: En Ano de publicação: 2012 Tipo de documento: Article