TY - JOUR
T1 - Gold(I)-mediated inhibition of protein tyrosine phosphatases
T2 - A detailed in vitro and cellular study
AU - Krishnamurthy, Divya
AU - Karver, Mark R.
AU - Fiorillo, Edoardo
AU - Orrú, Valeria
AU - Stanford, Stephanie M.
AU - Bottini, Nunzio
AU - Barrios, Amy M.
PY - 2008/8/14
Y1 - 2008/8/14
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=49449099348&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=49449099348&partnerID=8YFLogxK
U2 - 10.1021/jm800101w
DO - 10.1021/jm800101w
M3 - Article
C2 - 18605719
AN - SCOPUS:49449099348
SN - 0022-2623
VL - 51
SP - 4790
EP - 4795
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 15
ER -