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Updated: Feb 28, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
Human DNA (cytosine-5)-methyltransferases: a functional and structural perspective for epigenetic cancer therapy
Grégoire Rondelet1, Johan Wouters1
1Department of Chemistry, NAmur MEdicine & Drug Innovation Center (NAMEDIC-NARILIS), University of Namur, 61 rue de Bruxelles, B-5000 Namur, Belgium.
Abstract:
Epigenetic modifications modulate chromatin states to regulate gene expression. Among them, DNA methylation and histone modifications play a crucial role in the establishment of the epigenome. In cancer, these epigenetic events may act in concert to repress tumor suppressor genes or promote oncogenic pathways. In the context of cancer initiation and progression, recruitment of DNA (cytosine-5)-methyltransferases to specific genomic regions is mainly mediated by histone epigenetic marks, transcription factors and co-regulators as part of a dynamic process. Herein, we will review these mechanisms and present state-of-the-art of DNA methylation, treatment and development of epigenetic cancer therapies targeting this epigenetic modification.
Insights
Epigenetic modifications like DNA methylation are crucial in cancer. Understanding these mechanisms informs the development of novel epigenetic cancer therapies targeting DNA methylation for improved treatment outcomes.
Area of Science:
- Molecular Biology
- Genetics
- Cancer Research
Background:
- Epigenetic modifications, including DNA methylation and histone modifications, regulate gene expression by altering chromatin states.
- These epigenetic events are critical in cancer initiation and progression, often repressing tumor suppressor genes or activating oncogenic pathways.
- The recruitment of DNA methyltransferases to specific genomic regions is dynamically regulated by histone marks, transcription factors, and co-regulators.
Purpose of the Study:
- To review the mechanisms by which epigenetic modifications, particularly DNA methylation, are involved in cancer.
- To present the current state-of-the-art in DNA methylation research within the context of cancer.
- To discuss the development of epigenetic cancer therapies targeting DNA methylation.
Main Methods:
- Review of existing literature on epigenetic modifications in cancer.
- Analysis of mechanisms involving DNA methylation and its regulators.
- Examination of current and developing therapeutic strategies targeting DNA methylation.
Main Results:
- Epigenetic modifications play a significant role in cancer development and progression.
- DNA methylation is a key epigenetic mechanism implicated in oncogenesis.
- Targeting DNA methylation represents a promising avenue for novel cancer therapies.
Conclusions:
- Epigenetic modifications are fundamental to cancer biology.
- Understanding the interplay of DNA methylation and other epigenetic marks is crucial for cancer treatment.
- Epigenetic therapies targeting DNA methylation hold significant potential for future cancer treatment strategies.
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