Targeting the histone methylome as a therapeutic strategy continues to capture the interest of developers due to the genetic and expression abnormalities displayed in a variety of human cancers, as well as the chemically tractable nature of modifying enzymes. Over the past few years, developers have intensely pursued these targets, resulting in the rapid entry of histone methyltransferase (HMT) and histone demethylases (HDM) inhibitors into the clinical. Recently, interest in developing inhibitors against arginine methyltransferase enzymes, targeting of protein-protein interactions of enzyme complexes, and designing HMT and HDM inhibitors for combination cancer immunotherapy has provided new avenues for continued development.
Cambridge Healthtech Institute’s 6th Annual Targeting Histone Methyltransferases and Demethylases conference will once again gather an interdisciplinary collection of leaders working to advance epigenetic drug discovery.