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Issue 2, 2012
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Development of second generation epigenetic agents

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DNA in the nucleus of eukaryote cells is packaged in the nucleosomes around histone proteins, and this is highly organized and tightly regulated to control gene transcription. This packaging is not static and the histone tails undergo a wide variety of post-translational modifications that regulate gene transcription, and these patterns have been shown to be aberrantly regulated in multiple disease states. The biology behind these histone modifications is being elucidated, and it is now known that multiple proteins control the writing, reading and removal of these covalent histone modifications. The first agents, vorinostat and romidepsin, which inhibit histone deacetylase enzymes responsible for removing one of these marks have been approved for use in humans. This review focuses on the progress in the development of the second generation of epigenetic modifiers able to modulate histone marks, and restore normal gene transcription.

Graphical abstract: Development of second generation epigenetic agents

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Article information

01 Aug 2011
17 Sep 2011
First published
26 Oct 2011

Med. Chem. Commun., 2012,3, 135-161
Article type
Review Article

Development of second generation epigenetic agents

P. Jones, Med. Chem. Commun., 2012, 3, 135
DOI: 10.1039/C1MD00199J

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