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

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Abstract

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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Article information


Submitted
29 Apr 2010
Accepted
18 Jun 2010
First published
09 Jul 2010

Med. Chem. Commun., 2010,1, 114-124
Article type
Review Article

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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