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Abstract
Grant Number: 1R21NS061758-01 Project Title: Development of a High-Throughput Assay for Human Desumoylating Enzymes [SENPs]
PI Information: Name Title SALVESEN, GUY S. gsalvesen@burnham.org PROFESSOR AND DIRECTOR Abstract: DESCRIPTION (provided by applicant): The human peptidase clan CE is defined by seven proteases with a common fold and catalytic mechanism, commonly known as SENPs (sentrin specific proteases - sentrin being an alternative name for SUMO). Current information suggests that most SENPs are specific for processing of SUMO precursors and removing SUMO conjugated to protein substrates. Small-molecule compounds that target SENPs in a selective manner will provide an important toolset to study the biology of these enzymes, to aid in the discovery of their role in disease etiology and progression, and to facilitate the subsequent development of therapeutics against disease-relevant targets. The availability of simple kinetic assays that are applicable the SENPs would significantly enhance the discovery of chemical probes for members of the family, and for .orphan. SENPs with lesser known natural substrate specificity. Our application squarely addresses this important unmet need for a development of high-throughput substrate-based assays. We propose to develop small peptide based substrates with broad specificity for all seven human members of the SENP family, and generate simple assay procedures. The assays are expected to provide a tool for the rapid development of chemical probes for members of the family.
Public Health Relevance:
This Public Health Relevance is not available.Thesaurus Terms:
endopeptidase, enzyme substrate, high throughput technology, small molecule, technology /technique development
NIH Roadmap Initiative tag
Institution: BURNHAM INSTITUTE FOR MEDICAL RESEARCH LA JOLLA, CA 92037 Fiscal Year: 2007 Department: Project Start: 30-SEP-2007 Project End: 31-AUG-2010 ICD: NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE IRG: ZMH1