Ontology highlight
ABSTRACT:
SUBMITTER: Kulkarni RA
PROVIDER: S-EPMC3863632 | biostudies-literature | 2013 Sep
REPOSITORIES: biostudies-literature
Kulkarni Rhushikesh A RA Stanford Stephanie M SM Vellore Nadeem A NA Krishnamurthy Divya D Bliss Matthew R MR Baron Riccardo R Bottini Nunzio N Barrios Amy M AM
ChemMedChem 20130719 9
We screened a small library of thiuram disulfides for inhibition of lymphoid tyrosine phosphatase (LYP) activity. The parent thiuram disulfide, disulfiram, inhibited LYP activity in vitro and in Jurkat T cells, whereas diethyldithiocarbamate failed to inhibit LYP at the concentrations tested. Compound 13, an N-(2-thioxothiazolidin-4-one) analogue, was found to be the most potent LYP inhibitor in this series, with an IC50 value of 3 μM. Compound 13 inhibits LYP pseudo-irreversibly, as evidenced b ...[more]