Implementation of high-content assay for inhibitors of mitogen-activated protein kinase phosphatases.
Small molecule inhibitors of protein tyrosine kinases have become both powerful chemical probes of biological processes and clinically effective therapeutics. In contrast, few small molecule inhibitors of protein tyrosine phosphatases have been identified and none are currently approved for clinical use. New cell-based high-content methods have been developed that should enable investigators to probe for selective inhibitors of diseases-relevant protein phosphatases. Details of these methods are described herein.
Vogt
Andreas
A
Department of Pharmacology, The University of Pittsburgh Drug Discovery Institute, The Pittsburgh Molecular Library Screening Center, Biomedical Science Tower 3, Suite 10040, University of Pittsburgh, Pittsburgh, PA 15260, USA.
Lazo
John S
JS
D004353:Drug Evaluation, Preclinical / Q000379:methods; D054642:Dual Specificity Phosphatase 6; D004791:Enzyme Inhibitors / Q000032:analysis*; D048049:Extracellular Signal-Regulated MAP Kinases / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D020928:Mitogen-Activated Protein Kinases / Q000378:metabolism; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D014162:Transfection
D004791:Enzyme Inhibitors; D048049:Extracellular Signal-Regulated MAP Kinases; D020928:Mitogen-Activated Protein Kinases; C517035:DUSP6 protein, human; D054642:Dual Specificity Phosphatase 6; D017027:Protein Tyrosine Phosphatases