Rapid Histone Methyltransferase Profiling with Luminescent Reporters

DESCRIPTION (provided by applicant): Human cells contain three billion base pairs of DNA, our genome, compacted into chromatin. Expression levels of proteins are controlled by chromatin structure through chemical modifications that provide a second layer of control beyond the DNA blueprint, collectively termed the epigenome. Alterations to the epigenome by methylation of histones and DNA are tightly coupled to many diseases, particularly cancer. At present, our ability to control the methylation state of histones as well as other proteins in the human genome is severely limited by the paucity of selective drugs that target histone methyl transferases (hMTases). An ever increasing body of knowledge suggests that hMTases are a druggable target class with considerable interest from both industry and academia. The ability to provide a comprehensive panel of direct assays for profiling inhibitors against the gt50 hMTases will accelerate the development of new drug leads and new opportunities to dissect the rol