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Updated: Aug 13, 2025

An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues
Published on: April 5, 2018
Recent advances in epigenetic anticancer therapeutics and future perspectives
Liwen Ren1,2, Yihui Yang1,2, Wan Li1,2
1The State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing, China.
Abstract:
Tumor development is frequently accompanied by abnormal expression of multiple genomic genes, which can be broadly viewed as decreased expression of tumor suppressor genes and upregulated expression of oncogenes. In this process, epigenetic regulation plays an essential role in the regulation of gene expression without alteration of DNA or RNA sequence, including DNA methylation, RNA methylation, histone modifications and non-coding RNAs. Therefore, drugs developed for the above epigenetic modulation have entered clinical use or preclinical and clinical research stages, contributing to the development of antitumor drugs greatly. Despite the efficacy of epigenetic drugs in hematologic caners, their therapeutic effects in solid tumors have been less favorable. A growing body of research suggests that epigenetic drugs can be applied in combination with other therapies to increase efficacy and overcome tumor resistance. In this review, the progress of epigenetics in tumor progression and oncology drug development is systematically summarized, as well as its synergy with other oncology therapies. The future directions of epigenetic drug development are described in detail.
Insights
Epigenetic drugs show promise in cancer treatment by regulating gene expression. Combining epigenetic therapies with other treatments may improve efficacy against solid tumors.
Area of Science:
- Oncology
- Epigenetics
- Drug Development
Background:
- Tumorigenesis involves altered gene expression, including oncogene upregulation and tumor suppressor gene downregulation.
- Epigenetic mechanisms like DNA methylation, histone modifications, and non-coding RNAs regulate gene expression without changing DNA sequence.
- Epigenetic drugs are emerging as a significant area in oncology drug development.
Purpose of the Study:
- To systematically review the role of epigenetics in tumor progression.
- To summarize the progress of epigenetic drugs in oncology.
- To explore the synergy of epigenetic therapies with other cancer treatments.
Main Methods:
- Literature review of epigenetic mechanisms in cancer.
- Analysis of current epigenetic drug development status.
- Examination of combination therapy strategies involving epigenetic drugs.
Main Results:
- Epigenetic drugs have shown efficacy in hematologic cancers but less so in solid tumors.
- Epigenetic modulation is crucial for regulating gene expression during tumor development.
- Combination therapies involving epigenetic drugs are a promising strategy to enhance efficacy and overcome resistance.
Conclusions:
- Epigenetic drugs represent a vital class of anticancer agents.
- Further research into epigenetic drug development and combination therapies is warranted for solid tumors.
- Epigenetic strategies hold significant potential for future cancer treatment paradigms.
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