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

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Author list: Krishnamurthy D, Karver MR, Fiorillo E, Orru V, Stanford SM, Bottini N, Barrios AM
Publisher: American Chemical Society
Publication year: 2008
Volume number: 51
Issue number: 15
Start page: 4790
End page: 4795
Number of pages: 6
ISSN: 0022-2623
Languages: English-Great Britain (EN-GB)


Abstract

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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Last updated on 2019-23-08 at 11:15