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Updated: Jan 26, 2026
Extraction of Histones from Clinical Specimens for Epigenetic Profiling by Mass Spectrometry
Published on: November 21, 2025
Inhibitors of DNA Methylation and Histone Deacetylation as Epigenetically Active Drugs for Anticancer Therapy
Veronika A Myasoedova1, Vasily Sukhorukov1,2, Andrey V Grechko3
1Laboratory of Angiopathology, Institute of General Pathology and Pathophysiology, Moscow 125315, Russian Federation.
Abstract:
Gene expression is regulated and tightly controlled by epigenetic mechanisms. Alterations of these mechanisms are frequently observed in various diseases, particularly, in various types of cancer. Malignant transformation is caused by the impairment of the mechanisms of cell differentiation and cell cycle control associated with epigenetic changes. Altered patterns of epigenetic modification associated with malignancies can potentially be reversed by some agents that act on the key proteins responsible for DNA/histone modification and chromatin remodelling. Examples of such substances include the inhibitors of DNA methyltransferases or histone deacetylase. During the recent years, a number of such substances have been evaluated as potential therapeutic agents against certain types of cancer in preclinical and clinical studies, and some of them have been approved for treatment of hematological cancers. Application of epidrugs for therapy of solid tumors remains, however, more challenging. In this review, we summarize the current knowledge on the most studied mechanisms of epigenetic modification and the available epigenetically active drugs.
Insights
Epigenetic mechanisms regulate gene expression and are crucial in cancer development. Epigenetic drugs targeting DNA methyltransferases and histone deacetylase show promise for cancer therapy, though solid tumors present challenges.
Area of Science:
- Molecular Biology
- Genetics
- Oncology
Background:
- Epigenetic mechanisms tightly control gene expression.
- Alterations in these mechanisms are implicated in various cancers, disrupting cell differentiation and cell cycle control.
- Malignant transformation is linked to impaired epigenetic regulation.
Purpose of the Study:
- To review current knowledge on epigenetic modification mechanisms.
- To summarize available epigenetically active drugs (epidrugs).
- To discuss the therapeutic potential of epidrugs in cancer treatment.
Main Methods:
- Review of preclinical and clinical studies on epigenetic modifications and drugs.
- Focus on inhibitors of DNA methyltransferases and histone deacetylase.
- Analysis of therapeutic applications and challenges of epidrugs.
Main Results:
- Epigenetic modifications are frequently altered in malignancies.
- Certain epidrugs, like DNA methyltransferase and histone deacetylase inhibitors, can potentially reverse aberrant epigenetic patterns.
- Some epidrugs are approved for hematological cancers, but solid tumor treatment remains challenging.
Conclusions:
- Epigenetic modifications play a significant role in cancer.
- Epigenetic drugs offer a promising therapeutic avenue for cancer, particularly hematological malignancies.
- Further research is needed to overcome challenges in applying epidrugs to solid tumors.
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