Prospects & Overviews
Epigenetic cancer therapy: Proof of concept and remaining challenges
Article first published online: 1 SEP 2010
Copyright © 2010 WILEY Periodicals, Inc.
Volume 32, Issue 11, pages 949–957, November 2010
How to Cite
Mund, C. and Lyko, F. (2010), Epigenetic cancer therapy: Proof of concept and remaining challenges. Bioessays, 32: 949–957. doi: 10.1002/bies.201000061
- Issue published online: 14 OCT 2010
- Article first published online: 1 SEP 2010
- DNA methylation;
- histone modifications
Over the past few years several drugs that target epigenetic modifications have shown clinical benefits, thus seemingly validating epigenetic cancer therapy. More recently, however, it has become clear that these drugs are either characterized by low specificity or that their target enzymes have low substrate specificity. As such, clinical proof-of-concept for epigenetic cancer therapies remains to be established. Human cancers are characterized by widespread changes in their genomic DNA methylation and histone modification patterns. Epigenetic cancer therapy aims to restore normal epigenetic modification patterns through the inhibition of epigenetic modifier enzymes. In this review, we provide an overview about the known functional roles of DNA methyltransferases, histone deacetylases, histone methyltransferases, and demethylases in cancer development. The available data identify several examples that warrant further consideration as drug targets. Future research should be directed toward targeted enzyme inhibition and toward exploring interactions between epigenetic pathways to maximize cancer specificity.