Arylstibonic acids are potent and isoform-selective inhibitors of Cdc25a and Cdc25b phosphatases.
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.
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Base de dados:
MEDLINE
Assunto principal:
Compostos Organometálicos
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Propionatos
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Fosfatases cdc25
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Inibidores Enzimáticos
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Antimônio
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article