Exploiting the Epigenome to Control Cancer-Promoting Gene-Expression Programs

Publication date: 11 April 2016
Source:Cancer Cell, Volume 29, Issue 4
Author(s): Gerard L. Brien, Daria G. Valerio, Scott A. Armstrong
The epigenome is a key determinant of transcriptional output. Perturbations within the epigenome are thought to be a key feature of many, perhaps all cancers, and it is now clear that epigenetic changes are instrumental in cancer development. The inherent reversibility of these changes makes them attractive targets for therapeutic manipulation, and a number of small molecules targeting chromatin-based mechanisms are currently in clinical trials. In this perspective we discuss how understanding the cancer epigenome is providing insights into disease pathogenesis and informing drug development. We also highlight additional opportunities to further unlock the therapeutic potential within the cancer epigenome.

Teaser

In this perspective article Brien et al. discuss how our burgeoning understanding of the epigenetic changes in cancer is providing significant insights into the mechanistic role of the epigenome in oncogenesis. Moreover, the authors highlight how this understanding is being exploited therapeutically with the development of novel epigenetic therapies, several of which are in ongoing clinical trials. Finally, the authors discuss possibilities to further unlock the therapeutic potential within the cancer epigenome, through efforts to broaden our understanding of the epigenetic changes underlying cancer development.


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