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Issue 2, 2010
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Targeting epigenetic modifiers: Inhibitors of histone methyltransferases

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The term epigenetics is defined as inheritable changes that influence the outcome of a phenotype without changes in the genome. Epigenetics is based upon DNA methylation and posttranslational histone modifications. While there is much known about reversible acetylation as a posttranslational modification, research on histone methylation is still emerging, especially with regard to drug discovery. As aberrant epigenetic modifications have been linked to many diseases, inhibitors of histone methylation are very much in demand. This article gives an outline on the different histone methyltransferases, their involvement in disease, the available inhibitors and their potential as drugs.

Graphical abstract: Targeting epigenetic modifiers: Inhibitors of histone methyltransferases

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Publication details

The article was received on 29 Apr 2010, accepted on 18 Jun 2010 and first published on 09 Jul 2010

Article type: Review Article
DOI: 10.1039/C0MD00062K
Citation: Med. Chem. Commun., 2010,1, 114-124
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    Targeting epigenetic modifiers: Inhibitors of histone methyltransferases

    E. Bissinger, R. Heinke, W. Sippl and M. Jung, Med. Chem. Commun., 2010, 1, 114
    DOI: 10.1039/C0MD00062K

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