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Updated: May 18, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
DNA methylation inhibitors in cancer: recent and future approaches
Christina Gros1, Jacques Fahy, Ludovic Halby
1USR CNRS-Pierre Fabre n° 3388-ETaC Epigenetic Targeting of Cancer, CRDPF 3 avenue Hubert Curien, 31035 Toulouse Cedex 01, France.
Abstract:
This review presents the different human DNA methyltransferases (DNMTs), their biological roles, their mechanisms of action and their role in cancer. The description of assays for detecting DNMT inhibitors (DNMTi) follows. The different known DNMTi are reported along with their advantages, drawbacks and clinical trials. A discussion on the features of the future DNMT inhibitors will conclude this review.
Insights
This review covers human DNA methyltransferases (DNMTs) and their role in cancer. It details DNMT inhibitors (DNMTi), their clinical trials, and future directions for cancer therapy.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- DNA methyltransferases (DNMTs) are crucial enzymes involved in epigenetic regulation.
- Aberrant DNA methylation is a hallmark of various cancers.
- Understanding DNMTs is key to developing targeted cancer therapies.
Purpose of the Study:
- To review human DNA methyltransferases (DNMTs), their functions, and their involvement in cancer.
- To describe assays for identifying DNMT inhibitors (DNMTi).
- To summarize current DNMTi, their clinical applications, and future prospects.
Main Methods:
- Literature review of DNMTs, their roles in cancer, and DNMT inhibitors.
- Analysis of existing assays for DNMT inhibitor screening.
- Compilation of data on DNMTi clinical trials and their outcomes.
Main Results:
- Detailed overview of human DNMTs, including their biological functions and mechanisms.
- Description of various assays used to detect DNMT inhibitors.
- Summary of known DNMT inhibitors, highlighting their pros, cons, and clinical trial status.
Conclusions:
- DNMTs play a significant role in cancer development and progression.
- DNMT inhibitors represent a promising therapeutic strategy for cancer treatment.
- Further research into novel DNMT inhibitors is warranted for improved cancer therapies.
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