Identifying Potent, Selective Protein Tyrosine Phosphatase Inhibitors from a Library of Au(I) Complexes
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Liste des auteurs: Karver MR, Krishnamurthy D, Kulkarni RA, Bottini N, Barrios AM
Editeur: American Chemical Society
Année de publication: 2009
Numéro du volume: 52
Numéro de publication: 21
Page d'accueil: 6912
Dernière page: 6918
Nombre de pages: 7
ISSN: 0022-2623
Languages: Anglais-Royaume-Uni (EN-GB)
Résumé
Therapeutic inhibition of protein tyrosine phosphatase activity is a compelling yet challenging approach to the treatment of human disease. Toward this end, a library of 40 gold complexes with the general formula R(3)P-Au-Cl was screened to identify novel inhibitors of PTP activity. The most promising inhibitor obtained for the lymphoid tyrosine phosphatase LYP, (2-pyridine)(Ph(2))P-Au-Cl, is one of the most potent and selective LYP inhibitors identified to date with an IC(50) of 1.5 +/- 0.3 mu M, 10-fold selectivity for LYP over PTP-PEST, HePTP, and CD45 in vitro, and activity in cellular studies as well.
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