Profiling in Kinase and Methyl Transferase Panel Services

The National Center for Advancing Translational Sciences (NCATS) is a part of the National Institutes of Health (NIH), with a mission to catalyze the generation of innovative methods and technologies that will enhance the development, testing, and implementation of diagnostics and therapeutics across a wide range of human diseases and conditions. The Early Translational Branch (ETB) is tasked with identifying and developing novel small molecule leads against a wide spectrum of human disease targets, which it accomplishes by screening thousands of small molecules in collaboration with both intra-and extramural researchers. NCATS ETB is optimizing small molecules against specific methyl transferases and kinases in four different projects. Since these compounds occupy the binding site occupied by the cofactor ATP and SAM that is common in kinases and methyltransferases it is imperative that selectivity across the same family of enzymes is determined. This will be critical to understand if the intended biological mode of action is driven by the activity against the protein targeted by the small molecules being optimized. It is also important to unearth off target activities that may influence advantageous or disadvantageous phenotypes.