CATALYTIC DOMAINS OF THE HUMAN HEPATOCYTE GROWTH FACTOR RECEPTOR TYROSINE KINASE, AND MATERIALS AND METHODS FOR IDENTIFICATION OF INHIBITORS THEREOF

• Main Authors: ZHU, JEFF, SARUP, JAY, PARGE, HANS, MCTIGUE, MICHELE ANN, HICKEY, MICHAEL, MURRAY, BRION WILLIAM, MROCZKOWSKI, BARBARA
• Format: Patent
• Language: English; French
• Published: 23.09.2002
• Edition: 7
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS OR TEST PAPERS THEREFOR; COMPOSITIONS THEREOF; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES; CULTURE MEDIA; ENZYMOLOGY; FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIREDCHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERSFROM A RACEMIC MIXTURE; MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PEPTIDES; PROCESSES OF PREPARING SUCH COMPOSITIONS; PROCESSES USING MICROORGANISMS; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPIRITS; VINEGAR; WINE

The identification, isolation, purification, and characterization of the catalytic domain of the human hepatocyte growth factor receptor kinase (hHGFR) are described. A crystal structure of the hHGFR kinase domain is reported herein. This structure provides a thr ee- dimensional description of the binding site of the hHGFR for structure-based design of small molecule inhibitors thereof as therapeutic agents. The kinase domain of human HGFR an d its associated crystal structure is described for use in the discovery, identification and characeterization of modulators of human HGFR.