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Updated: Mar 6, 2026
An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues
Published on: April 5, 2018
Marked for death: targeting epigenetic changes in cancer
Sophia Xiao Pfister1, Alan Ashworth1
1Helen Diller Family Comprehensive Cancer Center, University of California, San Francisco, California 94158, USA.
Abstract:
In the past few years, it has become clear that mutations in epigenetic regulatory genes are common in human cancers. Therapeutic strategies are now being developed to target cancers with mutations in these genes using specific chemical inhibitors. In addition, a complementary approach based on the concept of synthetic lethality, which allows exploitation of loss-of-function mutations in cancers that are not targetable by conventional methods, has gained traction. Both of these approaches are now being tested in several clinical trials. In this Review, we present recent advances in epigenetic drug discovery and development, and suggest possible future avenues of investigation to drive progress in this area.
Insights
Mutations in cancer epigenetic genes are common. New therapies targeting these genes and synthetic lethality approaches are in clinical trials, offering new cancer treatment strategies.
Area of Science:
- Oncology
- Epigenetics
- Drug Discovery
Background:
- Mutations in epigenetic regulatory genes are frequently observed in human cancers.
- Targeting these mutations with chemical inhibitors is a developing therapeutic strategy.
- Synthetic lethality offers a novel approach for cancers resistant to conventional treatments.
Purpose of the Study:
- To review recent advancements in epigenetic drug discovery and development for cancer treatment.
- To explore future research directions in the field of epigenetic therapies.
Main Methods:
- Review of current literature on epigenetic drug discovery.
- Analysis of clinical trial data for epigenetic therapies.
- Discussion of synthetic lethality principles in cancer treatment.
Main Results:
- Epigenetic drug discovery is rapidly advancing with several promising chemical inhibitors.
- Synthetic lethality approaches are gaining traction and entering clinical trials.
- Clinical trials are actively evaluating the efficacy of these novel cancer therapies.
Conclusions:
- Epigenetic therapies, including chemical inhibitors and synthetic lethality, represent a significant frontier in cancer treatment.
- Continued research and development are crucial for realizing the full potential of epigenetic drugs.
- Future investigations should focus on optimizing drug delivery and identifying new epigenetic targets.
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