Format

Send to

Choose Destination
J Med Chem. 2008 Aug 14;51(15):4790-5. doi: 10.1021/jm800101w. Epub 2008 Jul 8.

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

Author information

1
Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, USA.

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.

PMID:
18605719
DOI:
10.1021/jm800101w
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for American Chemical Society
Loading ...
Support Center