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

Divya Krishnamurthy, Mark R. Karver, Edoardo Fiorillo, Valeria Orrú, Stephanie M. Stanford, Nunzio Bottini, Amy M. Barrios

Research output: Contribution to journalArticlepeer-review

114 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)4790-4795
Number of pages6
JournalJournal of Medicinal Chemistry
Volume51
Issue number15
DOIs
StatePublished - Aug 14 2008

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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