[DNA methylation and cancer--DNA methylation as a target of cancer chemotherapy]
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Updated: Aug 29, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
Kazuaki Miyamoto1, Toshikazu Ushijima
1Carcinogenesis Division, National Cancer Center Research Institute, 1-1 Tsukiji 5-chome, Chuo-ku, Tokyo 104-0045, Japan.
Abstract:
Aberrant epigenetic information, represented by aberrant DNA methylation, plays a large role in carcinogenesis. Hypermethylation of CpG islands in promoter regions can lead to silencing of tumor-suppressor genes, and hypomethylation of the genome could lead to its instability. Epigenetic information is inherited from a cell to its daughter cells without any decay in somatic cells, but shows dynamic changes during embryonic development. Based on the possibility that epigenetic information can be theoretically reversed, attempts are being made to use the aberrant epigenetic information as therapeutic targets. A demethylating agent, 5-aza-2'-deoxycytidine, has been reported to be effective for some hematological malignancies, and its derivatives are being developed. Finally, reports are coming out on methods that can induce sequence-specific methylation changes. Rapid progress in this field is expected.
Insights
Aberrant DNA methylation is crucial in cancer development. Reversing these epigenetic changes, using agents like 5-aza-2'-deoxycytidine, shows promise for cancer therapy and future research.
Area of Science:
- Epigenetics
- Cancer Biology
- Genomic Instability
Background:
- Aberrant DNA methylation, including hypermethylation and hypomethylation, is a key factor in cancer development.
- Hypermethylation can silence tumor-suppressor genes, while hypomethylation contributes to genomic instability.
- Epigenetic information is stably inherited in somatic cells but dynamically altered during embryonic development.
Purpose of the Study:
- To explore the therapeutic potential of reversing aberrant epigenetic information in cancer.
- To highlight the role of DNA methylation in carcinogenesis and its potential as a therapeutic target.
Main Methods:
- Review of existing literature on DNA methylation in cancer.
- Discussion of therapeutic strategies targeting epigenetic modifications, including demethylating agents.
- Exploration of emerging methods for sequence-specific methylation changes.
Main Results:
- The demethylating agent 5-aza-2 -deoxycytidine has shown efficacy in certain hematological malignancies.
- Development of derivatives of 5-aza-2 -deoxycytidine is ongoing.
- Methods for inducing sequence-specific methylation changes are emerging.
Conclusions:
- Aberrant epigenetic information, particularly DNA methylation, represents a viable therapeutic target in oncology.
- Targeting epigenetic alterations holds significant promise for cancer treatment, with ongoing advancements in the field.
- Further research into reversing epigenetic dysregulation is expected to yield rapid progress in cancer therapy.
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