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Updated: Nov 1, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
Methylation Landscape: Targeting Writer or Eraser to Discover Anti-Cancer Drug
Wen-Min Zhou1, Bin Liu2, Amin Shavandi3
1Key Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou, China.
Abstract:
Cancer is a major global health challenge for our health system, despite the important pharmacological and therapeutic discoveries we have seen since past 5 decades. The increasing prevalence and mortality of cancer may be closely related to smoking, exposure to environmental pollution, dietary and genetic factors. Despite significant promising discoveries and developments such as cell and biotechnological therapies a new breakthrough in the medical field is needed to develop specific and effective drugs for cancer treatment. On the development of cell therapies, anti-tumor vaccines, and new biotechnological drugs that have already shown promising effects in preclinical studies. With the continuous enrichment and development of chromatin immunoprecipitation sequencing (ChIP-seq) and its derivative technologies, epigenetic modification has gradually become a research hotspot. As key ingredients of epigenetic modification, Writers, Readers, Erasers have been gradually unveiled. Cancer has been associated with epigenetic modification especially methylation and therefore different epigenetic drugs have been developed and some of those are already undergoing clinical phase I or phase II trials, and it is believed that these drugs will certainly assist the treatment in the near future. With respect to this, an overview of anti-tumor drugs targeting modified enzymes and de-modified enzymes will be performed in order to contribute to future research.
Insights
Cancer treatment needs new breakthroughs. Epigenetic drugs targeting cancer
Area of Science:
- Oncology
- Epigenetics
Background:
- Cancer remains a significant global health challenge despite decades of research.
- Increasing cancer prevalence is linked to lifestyle and genetic factors.
- Current therapies like cell and biotechnological treatments show promise but a breakthrough is needed.
Purpose of the Study:
- To review anti-tumor drugs targeting epigenetic modification enzymes.
- To contribute to future research in developing specific and effective cancer drugs.
Main Methods:
- Review of epigenetic modification mechanisms, including Writers, Readers, and Erasers.
- Focus on chromatin immunoprecipitation sequencing (ChIP-seq) and related technologies.
- Analysis of epigenetic drugs targeting methylation.
Main Results:
- Epigenetic modifications, particularly methylation, are associated with cancer.
- Various epigenetic drugs are in clinical trials (Phase I/II).
- These drugs are expected to aid future cancer treatment.
Conclusions:
- Epigenetic drugs represent a promising avenue for cancer therapy.
- Targeting epigenetic enzymes offers a strategy for developing novel anti-cancer drugs.
- Further research into epigenetic modifications is crucial for advancing cancer treatment.
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