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Updated: Jun 13, 2026

An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues
Published on: April 5, 2018
Epigenetic tools in potential anticancer therapy
Katarina Sebova1, Ivana Fridrichova
1Laboratory of Cancer Genetics, Cancer Research Institute of Slovak Academy of Sciences, Bratislava, Slovakia.
Abstract:
Human cancer represents a heterogeneous group of diseases that are driven by progressive genetic and epigenetic abnormalities. The latter alterations involve hypermethylation and hypomethylation of DNA, and changed patterns of histone modification, with resultant remodeling of the chromatin structure that cause deregulation of the transcription activity of many genes. Unlike the remarkable progress in understanding the processes by which DNA methyltransferases can regulate gene expression and histone deacetylases can induce alteration of chromatin structure, the roles of epigenetic events in tumors remain insufficiently explained. In contrast to genetic changes, the epigenetic alterations in cancer cells can be reversed by the inhibition of DNA methylation and histone deacetylation. Therefore, many inhibition agents for re-expression, predominantly of tumor-suppressor genes, have been identified and tested in laboratory models and numerous clinical trials. Despite in-vitro evidence that a single drug can lead to reactivation of methylated genes, inhibitors of DNA methyltransferases and histone deacetylases have been investigated in combination, or together with cytotoxic chemotherapy, radiotherapy, immunotherapy, or hormonal therapy to improve the therapeutic effect. Ongoing trials are recognizing that the identification of a target group of patients who are more likely to respond to the epigenetic therapy, defining of an optimal dose and schedule of treatment, and the development of more specific inhibitors with minimal unwanted side effects are necessary. Thus, new combinations of anticancer agents, including epigenetic modulators, may lead to a more effective control of cancer.
Insights
Epigenetic alterations drive cancer progression but can be reversed. Investigating epigenetic drugs, alone or in combination, offers a promising strategy for more effective cancer control.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Human cancers arise from genetic and epigenetic changes, including DNA methylation and histone modifications.
- Epigenetic alterations can remodel chromatin, deregulating gene transcription, and their roles in tumors are still being elucidated.
- Unlike genetic mutations, epigenetic changes are potentially reversible.
Purpose of the Study:
- To review the current understanding of epigenetic events in cancer.
- To discuss the therapeutic potential of epigenetic drugs targeting DNA methylation and histone deacetylation.
- To highlight ongoing research and future directions for epigenetic cancer therapy.
Main Methods:
- Review of scientific literature on epigenetic modifications in cancer.
- Analysis of preclinical and clinical studies involving epigenetic inhibitors.
- Discussion of combination therapies involving epigenetic modulators.
Main Results:
- Epigenetic drugs, such as DNA methyltransferase and histone deacetylase inhibitors, can reverse gene silencing, particularly of tumor-suppressor genes.
- Combination therapies (epigenetic drugs with chemotherapy, radiotherapy, immunotherapy, or hormonal therapy) show potential for enhanced therapeutic effects.
- Ongoing clinical trials are focused on identifying patient subgroups, optimizing dosage, and developing more specific inhibitors.
Conclusions:
- Epigenetic therapy represents a promising avenue for cancer treatment due to the reversible nature of epigenetic alterations.
- Further research is needed to refine epigenetic drug development and combination strategies for improved cancer control.
- Personalized approaches and novel drug combinations are key to maximizing the efficacy of epigenetic therapies in cancer.
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