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Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
Exploiting the Epigenome to Control Cancer-Promoting Gene-Expression Programs
Gerard L Brien1, Daria G Valerio1, Scott A Armstrong2
1The Center for Epigenetics Research, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA; Cancer Biology and Genetics Program, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA.
Abstract:
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.
Insights
The cancer epigenome influences gene activity and drives cancer development. Reversible epigenetic changes offer promising therapeutic targets for new cancer drugs currently in clinical trials.
Area of Science:
- Molecular Biology
- Genetics
- Cancer Research
Background:
- The epigenome regulates gene expression and is crucial for cellular function.
- Epigenetic alterations are hallmarks of cancer development and progression.
- The reversibility of epigenetic changes presents therapeutic opportunities.
Purpose of the Study:
- To discuss the role of the cancer epigenome in disease pathogenesis.
- To highlight the impact of epigenetic understanding on cancer drug development.
- To identify future therapeutic potential within the cancer epigenome.
Main Methods:
- This perspective synthesizes current research on the cancer epigenome.
- It reviews insights from epigenetic studies into cancer mechanisms.
- It discusses the development of epigenetic-targeting therapeutics.
Main Results:
- Epigenetic dysregulation is fundamental to cancer pathogenesis.
- Understanding the cancer epigenome informs novel drug discovery strategies.
- Targeting epigenetic mechanisms is a rapidly advancing area in oncology.
Conclusions:
- The cancer epigenome is a critical area for understanding disease.
- Epigenetic therapies hold significant promise for cancer treatment.
- Further research can unlock greater therapeutic potential from the epigenome.
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