Allosteric regulation of histone lysine methyltransferases: from context-specific regulation to selective drugs.

Authors :: Davidovich C
Zhang Q
Source :: Biochemical Society transactions [Biochem Soc Trans] 2021 Apr 30; Vol. 49 (2), pp. 591-607.
Publication Year :: 2021
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.<br /> (© 2021 The Author(s).)

Subjects :: Drug Development methods
Histone-Lysine N-Methyltransferase chemistry
Histone-Lysine N-Methyltransferase genetics
Histones chemistry
Humans
Lysine chemistry
Methylation drug effects
Protein Binding drug effects
Protein Conformation drug effects
Protein Subunits chemistry
Protein Subunits genetics
Protein Subunits metabolism
Allosteric Regulation drug effects
Histone-Lysine N-Methyltransferase metabolism
Histones metabolism
Lysine metabolism
Pharmaceutical Preparations administration & dosage

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