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Updated: Jun 8, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
DNA demethylating agents and epigenetic therapy of cancer
1International Agency for Research on Cancer, Lyon, France.
Abstract:
Epigenetic events have been associated with virtually every step of tumor development and progression, and epigenetic alterations are believed to occur early in tumor development and may precede the malignant process. In contrast to genetic changes, epigenetic alterations arise in a gradual manner, leading to a progressive silencing of specific genes. An important distinction between epigenetic and genetic alterations is intrinsic reversibility of the former, making cancer-associated changes in DNA methylation, histone modifications, and expression of noncoding RNAs attractive targets for therapeutic intervention. This realization has triggered an impressive quest for the development of "epigenetic drugs" and epigenetic therapies. A number of agents have been subjected to an intensive investigation, many of which have been found capable of altering epigenetic states, including DNA methylation patterns and histone modification states. Many of these agents are currently being tested in clinical trials, while several of them are already used in clinics. This review will focus on the recent advances in the development of epigenetic drugs based on the inhibition of DNA methylation. Combinatorial therapies that couple DNA demethylating agents with histone deacetylase inhibitors will also be discussed.
Insights
Epigenetic drugs targeting DNA methylation and histone modifications offer reversible cancer therapies. Recent advances focus on these agents, including combination therapies, for clinical application in cancer treatment.
Area of Science:
- Oncology
- Epigenetics
- Pharmacology
Background:
- Epigenetic alterations, including DNA methylation and histone modifications, are crucial in tumor development and progression.
- These changes are gradual and potentially reversible, distinguishing them from genetic mutations.
- The reversibility of epigenetic changes makes them promising therapeutic targets for cancer.
Purpose of the Study:
- To review recent advancements in the development of epigenetic drugs.
- To focus specifically on agents that inhibit DNA methylation.
- To discuss combinatorial therapies involving DNA demethylating agents and histone deacetylase inhibitors.
Main Methods:
- Review of recent scientific literature on epigenetic drugs.
- Analysis of agents targeting DNA methylation patterns.
- Evaluation of clinical trial data for epigenetic therapies.
Main Results:
- Numerous epigenetic agents capable of altering DNA methylation and histone modifications have been identified.
- Many of these agents are in clinical trials, with some already in clinical use.
- Combinatorial approaches, such as pairing demethylating agents with histone deacetylase inhibitors, show therapeutic promise.
Conclusions:
- Epigenetic drugs, particularly those inhibiting DNA methylation, represent a significant therapeutic strategy for cancer.
- The reversibility of epigenetic modifications offers a unique advantage over traditional genetic therapies.
- Combination epigenetic therapies are advancing cancer treatment paradigms.
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