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Epigenetic regulation of gene expression is a dynamic and reversible process that establishes normal cellular phenotypes but also contributes to human diseases. At the molecular level, epigenetic regulation involves hierarchical covalent modification of DNA and the proteins that package DNA, such as histones. Here, we review the key protein families that mediate epigenetic signalling through the acetylation and methylation of histones, including histone deacetylases, protein methyltransferases, lysine demethylases, bromodomain-containing proteins and proteins that bind to methylated histones. These protein families are emerging as druggable classes of enzymes and druggable classes of protein-protein interaction domains. In this article, we discuss the known links with disease, basic molecular mechanisms of action and recent progress in the pharmacological modulation of each class of proteins.

Original publication

DOI

10.1038/nrd3674

Type

Journal article

Journal

Nat Rev Drug Discov

Publication Date

13/04/2012

Volume

11

Pages

384 - 400

Keywords

Acetylation, Animals, Drug Discovery, Epigenesis, Genetic, Gene Expression Regulation, Histones, Humans, Methylation, Protein Binding, Proteins, Signal Transduction