Kinome-wide cell-based assays

DESCRIPTION (provided by applicant): Protein kinases serve as critical mediators of signal transduction in human cells and impact virtually all aspects of cellular physiology, from the coordination of the cell cycle and cell division to apoptosis. The deregulation of kinase mediated signaling is now known to be involved in a variety of human diseases that include, diabetes, inflammation, cardiovascular diseases, tumor cell proliferation and metastasis making them a target for drug development. Structurally,kinases share a very similar architecture at the active-site (ATP-binding domain), making selectivity an issue in drug discovery and development. Thus, the development of rapid and economic methods for profiling drug candidates against a large panel of kinases in whole cells will not only aid in anticipating potential long term toxicit, but also help in understanding kinase targeted polypharmacology and aid in identifying new targets for old compounds. In this Phase I application, we will develop a sp