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. Including inflammation, stroke and variety of cancers. Celgene has been actively involved in the kinase drug discovery programs using structure based drug design (SBDD) approach. One of our discovery programs uses low molecular weight compounds (MW ~300) which are fragments of the typical drug-like molecules. The fragments are selected using biological screening at high concentration, followed by protein crystallography to identify the binding mode. Using this structural information, the compounds can be rapidly optimized for potency by modifying the core to fit the shape of the active site. This approach is expected to yield potent, selective compounds that have favorable drug-like characteristics such as low molecular weight and low logP. We would like to secure SSRL beam time since we do not have an in-house x-ray source and rely solely on synchrotron time for all our crystallography needs.
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