Literature DB >> 22705189

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

Lok Hang Mak1, Jessica Knott, Katherine A Scott, Claire Scott, Gillian F Whyte, Yu Ye, David J Mann, Oscar Ces, James Stivers, Rudiger Woscholski.   

Abstract

Arylstibonates structurally resemble n class="Chemical">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.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22705189      PMCID: PMC3389297          DOI: 10.1016/j.bmc.2012.05.040

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  20 in total

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6.  Mechanism of inhibition of protein-tyrosine phosphatases by vanadate and pervanadate.

Authors:  G Huyer; S Liu; J Kelly; J Moffat; P Payette; B Kennedy; G Tsaprailis; M J Gresser; C Ramachandran
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Authors:  Annette C Schmid; Richard D Byrne; Ramón Vilar; Rüdiger Woscholski
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9.  Potent inhibition of human apurinic/apyrimidinic endonuclease 1 by arylstibonic acids.

Authors:  Lauren A Seiple; John H Cardellina; Rhone Akee; James T Stivers
Journal:  Mol Pharmacol       Date:  2007-11-27       Impact factor: 4.436

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  1 in total

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  1 in total

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