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Updated: Jun 22, 2025

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
Pharmacological targeting of the cancer epigenome
Nathaniel W Mabe1,2, Jennifer A Perry1, Clare F Malone1,2
1Department of Pediatric Oncology, Dana-Farber Cancer Institute, Boston, MA, USA.
Abstract:
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including disease initiation, maintenance and therapy resistance. As a result, there have been advances in the development and evaluation of epigenetic therapies for cancer, revealing substantial promise but also challenges. Three epigenetic inhibitor classes are approved in the USA, and many more are currently undergoing clinical investigation. In this Review, we discuss recent developments for each epigenetic drug class and their implications for therapy, as well as highlight new insights into the role of epigenetics in cancer.
Insights
Epigenetic dysregulation drives cancer initiation, progression, and treatment resistance. Recent advances in epigenetic therapies show promise, with approved drugs and ongoing clinical trials offering new cancer treatment strategies.
Area of Science:
- Oncology
- Epigenetics
- Cancer Biology
Background:
- Epigenetic alterations are fundamental to cancer development and progression.
- Understanding epigenetic dysregulation is crucial for effective cancer treatment.
- Therapeutic strategies targeting epigenetic mechanisms are emerging as a significant area of research.
Purpose of the Study:
- To review recent advancements in epigenetic therapies for cancer.
- To discuss the role of epigenetics in cancer initiation, maintenance, and therapy resistance.
- To highlight new insights into epigenetic mechanisms in oncology.
Main Methods:
- Comprehensive literature review of epigenetic drug classes.
- Analysis of clinical trial data for epigenetic therapies.
- Synthesis of current understanding of epigenetics in cancer.
Main Results:
- Several classes of epigenetic inhibitors are approved or in clinical trials.
- Epigenetic therapies demonstrate substantial promise in treating various cancers.
- Challenges remain in the development and application of these therapies.
Conclusions:
- Epigenetic dysregulation is a key driver of cancer.
- Epigenetic therapies offer a promising avenue for cancer treatment.
- Continued research is vital to overcome challenges and optimize epigenetic drug efficacy.
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