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Updated: Jan 13, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
The Role of DNA and RNA Methylation in Cancer: Mechanisms and Therapeutic Potential of Epigenetic and
Julia Pisarek1, Marta Koblowska2
1Wydział Biologii, Uniwersytet Warszawski.
Abstract:
Chemical modifications of DNA and RNA play a pivotal role in the regulation of gene expression, enabling precise control of cellular functions and adaptation to changing environmental conditions. The most common modification in human DNA is cytosine methylation at the 5th position (5mC), while in RNA it is adenosine methylation at the N6 position (m⁶A), recognized as the predominant epitranscriptomic modification. Regulation of these modifications relies on the coordinated action of three groups of proteins: methyltransferases, demethylases, and reader proteins, which recognize modified nucleobases and recruit effector protein complexes, thereby translating the pattern of nucleic acid modifications into a specific biological response. Dysfunction of these protein groups leads to aberrant 5mC and m⁶A patterns, which play a crucial role in the pathogenesis and progression of many human diseases, including cancer. Deregulation of DNA and RNA methylation affects, among others, the control of genes involved in proliferation, apoptosis, and genome stability, which may promote tumor progression; moreover, the dynamic and reversible nature of these modifications makes them attractive diagnostic and therapeutic targets in cancer treatment.
Insights
Chemical modifications like DNA and RNA methylation are crucial for gene regulation and cellular function. Aberrant patterns, particularly in cancer, highlight their role in disease and potential as therapeutic targets.
Area of Science:
- Molecular Biology
- Epigenetics
- Cancer Biology
Background:
- Chemical modifications of DNA and RNA, such as 5-methylcytosine (5mC) and N6-methyladenosine (m⁶A), are key regulators of gene expression.
- These modifications control cellular functions and adaptation, with m⁶A being the primary epitranscriptomic mark.
- Proteins including methyltransferases, demethylases, and reader proteins orchestrate these modifications, translating them into biological responses.
Purpose of the Study:
- To explore the role of DNA and RNA methylation in gene expression regulation.
- To investigate the involvement of aberrant 5mC and m⁶A patterns in human diseases, particularly cancer.
- To highlight the potential of these dynamic modifications as diagnostic and therapeutic targets in oncology.
Main Methods:
- Review of existing literature on DNA and RNA methylation.
- Analysis of the regulatory mechanisms involving methyltransferases, demethylases, and reader proteins.
- Examination of the link between aberrant methylation patterns and disease pathogenesis.
Main Results:
- DNA and RNA methylation are critical for precise control of cellular functions and adaptation.
- Dysregulation of 5mC and m⁶A patterns is implicated in the pathogenesis of numerous diseases, including cancer.
- Aberrant methylation affects genes controlling proliferation, apoptosis, and genome stability, potentially driving tumor progression.
Conclusions:
- The coordinated action of specific proteins regulates DNA and RNA methylation patterns.
- Aberrant methylation patterns are significant contributors to cancer development and progression.
- The reversible nature of DNA and RNA methylation offers promising avenues for cancer diagnostics and therapeutics.
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