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- Title
Allosteric regulation of histone lysine methyltransferases: from context-specific regulation to selective drugs.
- Authors
Davidovich, Chen; Qi Zhang
- Abstract
Histone lysine methyltransferases (HKMTs) are key regulators of many cellular processes. By definition, HKMTs catalyse the methylation of lysine residues in histone proteins. The enzymatic activities of HKMTs are under precise control, with their allosteric regulation emerging as a prevalent paradigm. We review the molecular mechanisms of allosteric regulation of HKMTs using well-studied histone H3 (K4, K9, K27 and K36) methyltransferases as examples. We discuss the current advances and future potential in targeting allosteric sites of HKMTs for drug development.
- Subjects
HISTONE methyltransferases; DRUG laws; ALLOSTERIC regulation; METHYLTRANSFERASES; DRUG development; HISTONES; LYSINE
- Publication
Biochemical Society Transactions, 2021, Vol 49, Issue 2, p591
- ISSN
0300-5127
- Publication type
Article
- DOI
10.1042/BST20200238