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Abstract
Grant Number: 1R03MH076407-01 Project Title: Chemical Complementation Assay for MKP-1 (RMI)
PI Information: Name Title LAZO, JOHN S. lazo@pitt.edu PROFESSOR AND PROGRAM LEADER, MOLECULAR Abstract: DESCRIPTION (provided by applicant): Mitogen activated protein kinase phosphatase-1 (MKP-1) is a dual specificity phosphatase that has a central role regulating intracellular signal transduction by controlling the phosphorylation status of mitogen activated protein kinases. There is considerable evidence indicating MKP-1 could be a potential molecular target for several human diseases. Nonetheless, no potent or selective small molecule inhibitors of this protein phosphatase have been identified. Cell-based chemical complementation assays provide a novel platform technology to screen for cell-active inhibitors of this protein phosphatase. This proposal will provide sufficient reagents, including cells and DMA transfection vectors, to permit the high throughput screening of 100,000 compounds.
Public Health Relevance:
This Public Health Relevance is not available.Thesaurus Terms:
antineoplastic, drug discovery /isolation, drug screening /evaluation, enzyme inhibitor, high throughput technology, mitogen activated protein kinase
biological signal transduction, small molecule
tissue /cell culture, transfection /expression vector
Institution: UNIVERSITY OF PITTSBURGH AT PITTSBURGH 350 THACKERAY HALL PITTSBURGH, PA 15260 Fiscal Year: 2005 Department: PHARMACOLOGY AND CHEMICAL BIOLOGY Project Start: 15-SEP-2005 Project End: 14-SEP-2006 ICD: NATIONAL INSTITUTE OF MENTAL HEALTH IRG: ZMH1