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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
The role of epigenetic transcription repression and DNA methyltransferases in cancer
Filipe Ivan Daniel1, Karen Cherubini, Liliane Soares Yurgel
1School of Dentistry, Oral Medicine Division, Pontifical Catholic University of Rio Grande do Sul, Brazil. fidaniel@brturbo.com.br
Abstract:
Epigenetic alterations such as DNA methylation have been implicated in the development and progression of various cancers. DNA methylation consists of the reversible addition of a methyl group to the carbon 5 position of cytosine in CpG dinucleotides and is considered essential for normal embryonic development. However, global genomic hypomethylation and aberrant hypermethylation of regulatory regions of tumor suppressor genes have been associated with chromosomal instability and transcription repression, respectively, providing neoplastic cells with a selective advantage. DNA methyltransferases are the enzymes responsible for the addition of methyl groups to CpG dinucleotides, which, together with histone modifiers, initiate the events necessary for transcription repression to occur. It has been demonstrated that increased expression of DNA methyltransferases may contribute to tumor progression through methylation-mediated gene inactivation in various human cancers. Given their importance, this article reviews the main epigenetic mechanisms for regulating transcription and its implications in cancer development.
Insights
Epigenetic alterations, including DNA methylation, are crucial in cancer development. Aberrant DNA methylation patterns can lead to gene inactivation and tumor progression, highlighting epigenetic mechanisms in cancer.
Area of Science:
- Molecular Biology
- Cancer Research
- Epigenetics
Background:
- Epigenetic alterations, particularly DNA methylation, are increasingly recognized for their role in cancer.
- DNA methylation involves adding a methyl group to cytosine in CpG dinucleotides, a process vital for development.
- Dysregulation includes global hypomethylation and hypermethylation of tumor suppressor genes, promoting cancer progression.
Purpose of the Study:
- To review the primary epigenetic mechanisms regulating transcription.
- To explore the implications of these mechanisms in cancer development.
Main Methods:
- Literature review of epigenetic mechanisms in cancer.
- Analysis of DNA methylation and its role in gene regulation.
Main Results:
- DNA methylation is essential for normal development but its aberrant forms drive cancer.
- Increased DNA methyltransferases expression correlates with tumor progression via gene inactivation.
- Epigenetic changes provide neoplastic cells with a selective advantage.
Conclusions:
- Epigenetic regulation, especially DNA methylation, is fundamental to understanding cancer.
- Targeting epigenetic mechanisms may offer novel therapeutic strategies for cancer treatment.
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