Protein methyltransferase inhibitors as personalized cancer therapeutics

The protein methyltransferases (PMTs) have emerged as a novel target class, especially for oncology indications where specific genetic alterations, affecting PMT activity, drive cancer tumorigenesis. This target class has proved quite druggable; small molecule inhibitors (PMTis) of several PMT enzymes have been reported, that display a diversity of chemical structures and target binding modalities. Here we review recent progress in identifying, characterizing and optimizing PMTis for eventual use as personally targeted cancer therapeutics.