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Updated: May 29, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
[Histone methyltransferases: a new class of therapeutic targets in cancer treatment?]
Hassiba Chaib1, Thomas Prébet, Norbert Vey
1Centre de recherche en cancérologie de Marseille, Marseille, France.
Abstract:
Epigenetic gene regulation contributes, together with genetic alterations, to cancer development and progression. In contrast to genetic disorders, the possibility of reversing epigenetic alterations has provided original targets for therapeutic application. In the last years, work has been focused on the pharmacological restoration of epigenetic regulation balance using epidrugs which yield hopes for novel strategy in cancer therapy. Histone acetylation and DNA methylation are epigenetic modifications which have been closely linked to the pathology of human cancers, and inhibitors of both enzyme classes for clinical use are at hands. Novel findings accumulated during the last years both in chemistry and biomedical applications give rise to new targeted treatments against cancer. Since their links with pathogenesis and progression of cancer were recognized, histone methyltransferases emerge as promising therapeutic targets in cancer treatment.
Insights
Epigenetic modifications like DNA methylation and histone acetylation are key in cancer. Reversing these epigenetic changes with drugs offers a promising new cancer therapy strategy.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Epigenetic gene regulation, alongside genetic changes, drives cancer development and progression.
- Unlike genetic disorders, epigenetic alterations are potentially reversible, offering unique therapeutic targets.
- Epidrugs aim to restore epigenetic balance, representing a novel strategy in cancer therapy.
Purpose of the Study:
- To explore the role of epigenetic modifications in cancer.
- To highlight the therapeutic potential of targeting epigenetic regulators in cancer treatment.
- To discuss recent advancements in epidrugs for cancer therapy.
Main Methods:
- Review of current literature on epigenetic modifications in cancer.
- Analysis of pharmacological approaches targeting epigenetic enzymes.
- Examination of novel findings in chemistry and biomedical applications of epidrugs.
Main Results:
- Histone acetylation and DNA methylation are strongly associated with human cancer pathology.
- Inhibitors for enzymes involved in histone acetylation and DNA methylation are available for clinical use.
- Histone methyltransferases are emerging as significant therapeutic targets due to their role in cancer pathogenesis.
Conclusions:
- Targeting epigenetic modifications represents a promising avenue for novel cancer treatments.
- Epidrugs offer a potential strategy to reverse aberrant epigenetic changes in cancer.
- Further research into histone methyltransferases could lead to new targeted cancer therapies.
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