4.7 Article

Understanding the Complexity of Epigenetic Target Space

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JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 4, 页码 1299-1307

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AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01507

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The purpose of this review is to provide an overview of the complexity of the epigenetic target space. Chemical modifications of histones and nucleic acids constitute a key epigenetic mechanism. 'Whereas modifications such as methylation and acetylation are well-known, there are many additional, less explored modifications described here. The writers, readers and erasers of such diverse modifications, which constitute a major portion of the potential epigenetic target space, are discussed, in addition to the various other protein families that do not fall under these three categories. Finally, disease relevance and druggability of epigenetic targets are discussed with concluding remarks about the richness and diversity they will provide for future targeted therapies.

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