Journal
NATURE REVIEWS DRUG DISCOVERY
Volume 11, Issue 5, Pages 384-400Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/nrd3674
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Funding
- Canadian Institutes of Health Research
- Eli Lilly
- Genome Canada through the Ontario Genomics Institute
- GlaxoSmithKline
- Ontario Ministry for Research and Innovation
- Novartis Research Foundation
- Pfizer
- Wellcome Trust
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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.
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