This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. The purpose of this visit to BNL/NSLS is to collect a better quality X-diffraction data for the cMet kinase-inhibitor complex. cMET and its ligand, hepatocyte growth factor/scatter factor have become one of the leading molecular targets in cancer. The success of targeting tyrosine kinase receptors in human cancer has triggered an entirely new therapeutic strategy for treating the disease. The project involves the development of drugs that might be of use in treating cancers. ArQule has several drugs in development that bind to specific protein receptors believed to be involved in cancers. This proposal is to examine the crystals structures of receptors-drug complexes in order to guide the stereo-synthesis of the drugs. In order to design a better inhibitor for cMet it is crucial to obtain the 3D-dimensional structure of its complex. We have generated crystals for complex of a small molecule inhibitors and cMet kinase. These crystals weakly diffract in our in-house X-ray source and difficult to determine the structure with a poor diffraction data. However, this problem could be solved by collecting diffraction data using an intense X-ray beam at BNL. A temporary access to BNL is crucial for us to conduct diffraction experiment on cMet-inhibitor complex.
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