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.
Original language | English (US) |
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Pages (from-to) | 4371-4376 |
Number of pages | 6 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 20 |
Issue number | 14 |
DOIs | |
State | Published - Jul 15 2012 |
Keywords
- Arylstibonic acids
- Cdc25 inhibitor
- Protein tyrosine phosphatase
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry