Exploring Methods of Targeting Histone Methyltransferases and Their Applications in Cancer Therapeutics.

ABSTRACT: Histone methyltransferases (HMTs) are enzymes that catalyze the methylation of lysine or arginine residues of histone proteins, a key post-translational modification (PTM). Aberrant expression or activity of these enzymes can lead to abnormal histone methylation of cancer-related genes and thus promote tumorigenesis. Histone methyltransferases have been implicated in chemotherapeutic resistance and immune stimulation, making these enzymes potential therapeutic targets of interest, and chemically targeting these proteins provides an avenue for novel drug development in cancer therapy. This Review aims to discuss the evolution of chemical approaches that have emerged in the past five years to design probes targeting these enzymes, including inhibition through noncovalent inhibitors, covalent

SUBMITTER: Wang MY 

PROVIDER: S-EPMC9336197 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature