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Updated: Jul 17, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
Epigenetic inhibitors and their role in cancer therapy
Nouha Abdelaziz1, Lubna Therachiyil2, Hana Q Sadida3
1Translational Research Institute, Academic Health System, Hamad Medical Corporation, Doha, Qatar.
Abstract:
Epigenetic modifications to DNA are crucial for normal cellular and biological functioning. DNA methylation, histone modifications, and chromatin remodeling are the most common epigenetic mechanisms. These changes are heritable but still reversible. The aberrant epigenetic alterations, such as DNA methylation, histone modification, and non-coding RNA (ncRNA)-mediated gene regulation, play an essential role in developing various human diseases, including cancer. Recent studies show that synthetic and dietary epigenetic inhibitors attenuate the abnormal epigenetic modifications in cancer cells and therefore have strong potential for cancer treatment. In this chapter, we have highlighted various types of epigenetic modifications, their mechanism, and as drug targets for epigenetic therapy.
Insights
Epigenetic modifications regulate gene function and are vital for health. Aberrant epigenetic changes drive diseases like cancer, but epigenetic inhibitors offer promising therapeutic potential.
Area of Science:
- Molecular Biology
- Genetics
- Biochemistry
Background:
- Epigenetic modifications, including DNA methylation and histone alterations, are fundamental to cellular processes.
- These modifications are heritable yet reversible, influencing gene expression without altering DNA sequence.
- Dysregulation of epigenetic mechanisms is implicated in the pathogenesis of various human diseases, notably cancer.
Purpose of the Study:
- To review the diverse landscape of epigenetic modifications.
- To elucidate the mechanisms underlying epigenetic regulation.
- To identify epigenetic modifications as targets for novel therapeutic strategies.
Main Methods:
- Review of current scientific literature on epigenetic mechanisms.
- Analysis of the role of epigenetic alterations in disease development.
- Examination of epigenetic inhibitors as potential therapeutic agents.
Main Results:
- Epigenetic modifications encompass DNA methylation, histone modifications, and non-coding RNA-mediated gene regulation.
- Aberrant epigenetic alterations are key drivers in human diseases, particularly cancer.
- Synthetic and dietary epigenetic inhibitors demonstrate efficacy in targeting abnormal epigenetic modifications in cancer cells.
Conclusions:
- Epigenetic mechanisms are critical for normal biological function and disease development.
- Targeting epigenetic modifications presents a promising avenue for innovative cancer therapies.
- Further research into epigenetic inhibitors could revolutionize disease treatment.
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