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Updated: Jan 28, 2026

ATAC-Seq Optimization for Cancer Epigenetics Research
Published on: June 30, 2022
Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer
Helai P Mohammad1, Olena Barbash1, Caretha L Creasy2
1Epigenetics Department, Oncology, GlaxoSmithKline, Collegeville, PA, USA.
Abstract:
Epigenetic dysregulation is a common feature of most cancers, often occurring directly through alteration of epigenetic machinery. Over the last several years, a new generation of drugs directed at epigenetic modulators have entered clinical development, and results from these trials are now being disclosed. Unlike first-generation epigenetic therapies, these new agents are selective, and many are targeted to proteins which are mutated or translocated in cancer. This review will provide a summary of the epigenetic modulatory agents currently in clinical development and discuss the opportunities and challenges in their development. As these drugs advance in the clinic, drug discovery has continued with a focus on both novel and existing epigenetic targets. We will provide an overview of these efforts and the strategies being employed.
Insights
New epigenetic drugs targeting cancer are advancing in clinical trials. These selective agents target mutated proteins, offering new therapeutic opportunities and challenges in cancer treatment.
Area of Science:
- Oncology
- Epigenetics
- Pharmacology
Background:
- Epigenetic dysregulation is a hallmark of many cancers, often involving alterations in epigenetic machinery.
- First-generation epigenetic therapies have paved the way for newer, more selective agents.
- Targeting mutated or translocated proteins involved in cancer epigenetics is a key focus.
Purpose of the Study:
- To review epigenetic modulatory agents in current clinical development.
- To discuss the opportunities and challenges associated with their clinical advancement.
- To provide an overview of ongoing drug discovery efforts for novel and existing epigenetic targets.
Main Methods:
- Literature review of epigenetic modulatory agents in clinical development.
- Analysis of clinical trial data and outcomes for epigenetic therapies.
- Examination of drug discovery strategies for epigenetic targets in cancer.
Main Results:
- A new generation of selective epigenetic drugs targeting cancer-specific protein alterations are in clinical development.
- Clinical trial results for these agents are beginning to emerge, demonstrating their potential.
- Drug discovery continues to identify novel and existing epigenetic targets for therapeutic intervention.
Conclusions:
- Selective epigenetic therapies targeting mutated proteins represent a promising advancement in cancer treatment.
- Further research and development are crucial to overcome challenges and maximize the potential of these agents.
- Ongoing drug discovery efforts are expanding the landscape of epigenetic targets for cancer therapy.
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