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Drug Discov Today. 2011 Aug;16(15-16):683-90. doi: 10.1016/j.drudis.2011.05.004. Epub 2011 May 13.

DNA demethylases: a new epigenetic frontier in drug discovery.

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  • 1CellCentric Ltd., Chesterford Research Park, Little Chesterford, CB10 1XL, UK.


DNA methylation is one of the most extensively studied, and one of the most stable, of all epigenetic modifications. Two drugs that target DNA methyltransferase enzymes are licensed for clinical use in oncology but relatively little attention has focused on the enzymatic pathways by which DNA methylation can be reversed. Recent breakthroughs have identified at least two classes of enzymes that can achieve functional reversal. This review discusses the significance of DNA demethylation in a range of human diseases, the candidate proteins that mediate the demethylation and the opportunities and challenges in targeting these candidates to develop new therapeutics.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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