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Methods of using chemical libraries to search for new kinase inhibitors

United States Patent

June 3, 2003
View the Complete Patent at the US Patent & Trademark Office
The generation of selective inhibitors for specific protein kinases would provide new tools for analyzing signal transduction pathways and possibly new therapeutic agents. We have invented an approach to the development of selective protein kinase inhibitors based on the unexpected binding mode of 2,6,9-trisubstituted purines to the ATP binding site of human CDK2. The most potent inhibitor, purvalanol B (IC.sub.50 =6 nM), binds with a 30-fold greater affinity than the known CDK2 inhibitor, flavopiridol. The cellular effects of this class of compounds were examined and compared to those of flavopiridol by monitoring changes in mRNA expression levels for all genes in treated cells of Saccharomyces cerevisiae using high-density oligonucleotide probe arrays.
Gray; Nathanael S. (Berkeley, CA), Schultz; Peter (Oakland, CA), Wodicka; Lisa (Santa Clara, CA), Meijer; Laurent (Roscoff, FR), Lockhart; David J. (Mountain View, CA)
The Regents of the University of California (Oakland, CA), Affymetrix, Inc. (Santa Clara, CA), Centre National de la Recherche Scientifique (Paris, FR)
09/ 221,406
December 22, 1998
FEDERALLY SPONSORED RESEARCH AND DEVELOPMENT This invention was supported by the Director, Office of Health Effects Research of the U.S. Department of Energy and by the National Science Foundation. The Government has certain rights in this invention.