Protein Lysine Methyltransferases Inhibitors

Abstract: Protein lysine methylation is a significant protein post-translational modification (PTMs), and has a key function in epigenetic regulation. Protein lysine methyltransferase (PKMTs) mainly catalyze the lysine methylation of various core histones, but also catalyze a few non-histone proteins. It has been observed that aberrant activity of PKMTs has been found in many cancers and other diseases, and some PKMTs inhibitors have been discovered and progressed to clinical trials. This field developed rapidly and has aroused great interest. In this paper, we reviewed the biochemical and biological activities of PKMTs and their association with various cancers. Selective small-molecule inhibitors including their chemical structure, structure-activity relationship, and in vitro/vivo studies are also be described with the aim of providing ideas for the discovery highly potent, selective PKMTs inhibitors.