Recent Progress in the Discovery of Epigenetic Inhibitors for the Treatment of Cancer

: Epigenetics investigates heritable changes in gene transcription that do not involve a change in DNA sequence, and an increased understanding in the role of epigenetic misregulation as a key contributor to cancer has triggered the development of epigenetic targeted cancer therapies. Among these include efforts around a class of enzymes known as histone methyltransferases (HMTs). The level of interest in the development of HMT inhibitors as a class of anticancer agents has significantly grown beyond academic settings, and in the last 5 years whole research groups from biotech and big pharma have been dedicated to this area. There are now multiple reports describing small-molecule HMT inhibitors, including chemical probes and drug candidates entering the clinic as first-in-class agents. Recent progress in this emerging area is the topic of this chapter.