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Updated: Aug 11, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
The development of small molecules targeting methyltransferase-like 3
Hongyu Li1, Qiong Zhang1, Qinglan Feng1
1Jiang Su Key Laboratory of Drug Design and Optimization and Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Small molecules targeting Methyltransferase-like 3 (METTL3) show therapeutic potential for various diseases, particularly cancer. This review covers METTL3 small molecule discovery and future development for researchers.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- N-methyladenosine (m6A) is the most prevalent mRNA modification in mammals.
- Methyltransferase-like 3 (METTL3) is the key enzyme regulating m6A.
- METTL3 dysregulation is linked to diverse diseases, including cancer initiation and progression.
Approach:
- Systematic review of small molecules targeting METTL3.
- Analysis of current discovery and development strategies.
- Identification of future research directions.
Key Points:
- METTL3 is a critical regulator of mRNA methylation.
- Targeting METTL3 with small molecules offers therapeutic opportunities.
- The review consolidates information on METTL3 inhibitors for researchers.
Conclusions:
- Small molecule inhibitors of METTL3 are promising therapeutic agents.
- Further development is needed to optimize METTL3-targeting drugs.
- This review provides a comprehensive resource for METTL3 research.
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