Journal
NATURE REVIEWS DRUG DISCOVERY
Volume 20, Issue 4, Pages 265-286Publisher
NATURE PORTFOLIO
DOI: 10.1038/s41573-020-00108-x
Keywords
-
Funding
- NIH [K00CA212435, R01 CA236118, R01CA218600, R01CA230854, R01GM122749, R01HD088626]
Ask authors/readers for more resources
Protein lysine methylation is a crucial post-translational modification that plays a role in various diseases. Drugs targeting specific KMTs have been developed, with some already approved for clinical use and others under evaluation. These KMTs are emerging as promising new targets for drug development to treat diverse diseases.
Protein lysine methylation is a crucial post-translational modification that regulates the functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' of protein lysine methylation, lysine methyltransferases (KMTs), is implicated in the cause of many diseases, including cancer, mental health disorders and developmental disorders. Over the past decade, significant advances have been made in developing drugs to target KMTs that are involved in histone methylation and epigenetic regulation. The first of these inhibitors, tazemetostat, was recently approved for the treatment of epithelioid sarcoma and follicular lymphoma, and several more are in clinical and preclinical evaluation. Beyond chromatin, the many KMTs that regulate protein synthesis and other fundamental biological processes are emerging as promising new targets for drug development to treat diverse diseases.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available