Protein Lysine Methyltransferases Inhibitors

Protein lysine methylation is a significant protein post-translational modification (PTMs) and has a key function in epigenetic regulation. Protein lysine methyltransferase (PKMTs) mainly catalyzes the lysine methylation of various core histones and 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 PKMT 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 described to provide ideas for the discovery of highly potent, selective PKMT inhibitors.

Automated summary

Protein lysine methylation is an important protein post-translational modification involved in epigenetic regulation. Aberrant activity of protein lysine methyltransferase (PKMTs) has been found in various cancers and diseases, and PKMT inhibitors have been discovered and progressed to clinical trials. This field has developed rapidly and attracted significant interest.