Gold(I)-mediated inhibition of protein tyrosine phosphatases: A detailed in vitro and cellular study

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Liste des auteurs: Krishnamurthy D, Karver MR, Fiorillo E, Orru V, Stanford SM, Bottini N, Barrios AM
Editeur: American Chemical Society
Année de publication: 2008
Numéro du volume: 51
Numéro de publication: 15
Page d'accueil: 4790
Dernière page: 4795
Nombre de pages: 6
ISSN: 0022-2623
Languages: Anglais-Royaume-Uni (EN-GB)


Gold(I) complexes containing N-heterocyclic carbene ligands were synthesized, characterized, and along with the antiarthritic drug, auranofin, tested as inhibitors of the cysteine-dependent protein tyrosine phosphatases, which are implicated in several disease states. These compounds exhibit potencies in the low micromolar range against the enzymes in vitro. At therapeutically relevant concentrations, all compounds inhibit PTP activity in Jurkat T leukemia cells with some selectivity. In addition, the gold-carbene compounds inhibit phosphatase activity in primary mouse thymocytes.


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