Related Experiment Video
Updated: May 30, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
DNA demethylating antineoplastic strategies: a comparative point of view
Stefano Amatori1, Irene Bagaloni, Benedetta Donati
1Molecular Pathology and Oncology Lab. "PaoLa," Department of Biomolecular Sciences, University of Urbino "Carlo Bo," Fano, Italy.
Abstract:
Despite the involvement of genetic alterations in neoplastic cell transformation, it is increasingly evident that abnormal epigenetic patterns, such as those affecting DNA methylation and histone posttranslational modifications (PTMs), play an essential role in the early stages of tumor development. This finding, together with the evidence that epigenetic changes are reversible, enabled the development of new antineoplastic therapeutic approaches known as epigenetic therapies. Epigenetic modifications are involved in the control of gene expression, and their aberrant distribution is thought to participate in neoplastic transformation by causing the deregulation of crucial cellular pathways. Epigenetic drugs are able to revert the defective gene expression profile of cancer cells and, consequently, reestablish normal molecular pathways. Considering the emerging interest in epigenetic therapeutics, this review focuses on the approaches affecting DNA methylation, evaluates novel strategies and those already approved for clinical use, and compares their therapeutic potential.
Insights
Epigenetic alterations, like DNA methylation changes, are crucial in early cancer development. Reversible epigenetic therapies offer new ways to treat cancer by correcting abnormal gene expression in cancer cells.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Genetic alterations are known drivers of cancer, but epigenetic dysregulation, including DNA methylation and histone posttranslational modifications (PTMs), is increasingly recognized in early tumor development.
- Epigenetic changes are reversible, paving the way for novel therapeutic strategies.
- Aberrant epigenetic patterns can deregulate critical cellular pathways essential for neoplastic transformation.
Purpose of the Study:
- To review epigenetic therapies, focusing on DNA methylation.
- To evaluate novel and clinically approved strategies targeting epigenetic modifications.
- To compare the therapeutic potential of different epigenetic approaches.
Main Methods:
- Literature review of epigenetic modifications and therapies.
- Analysis of DNA methylation-targeting strategies.
- Evaluation of approved and emerging epigenetic drugs.
Main Results:
- Epigenetic drugs can reverse aberrant gene expression in cancer cells.
- These drugs have the potential to reestablish normal molecular pathways.
- Several therapeutic strategies affecting DNA methylation are under investigation and in clinical use.
Conclusions:
- Epigenetic therapies represent a promising avenue for cancer treatment.
- Targeting DNA methylation is a key strategy in developing these therapies.
- Further research and clinical evaluation are essential to optimize their therapeutic potential.
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists
Phenothiazines, such as prochlorperazine...
Treatment Resistant Cancers
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

