Epigenetic approaches to cancer therapy

Epigenetic abnormalities are common in human cancer and play a key role in tumor progression through dysregulation of gene expression and chromatin function. The recent identification of the enzymes regulating epigenetic modifications and their altered function in cancer supports the possibility that these abnormalities can be reversed by inhibiting these enzymes. Indeed, drugs targeting such enzymes including DNA methyltransferases (DNMTs) and histone deacetylases (HDACs) have demonstrated antitumor activity in the clinic and inhibitors of DNMTs and HDACs are now approved as anticancer agents. As our understanding of cancer epigenetics grows, members of additional enzyme classes such as histone methyltransferases and demethylases are emerging as targets for future epigenetic cancer therapies.

Section editor:Robert Copeland – Epizyme Inc., Cambridge, MA 02139, USA