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Updated: May 28, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
Recent Advances in Searching for DNMT Inhibitors and Their Potential Application in Treating Human Diseases
Anatoliy A Bulygin1, Anastasiia T Davletgildeeva1, Nikita A Kuznetsov1,2
1Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
Abstract:
DNA methylation is one of the most important epigenetic mechanisms regulating gene expression. DNA methyltransferases (DNMTs) are key players in these processes, regulating dynamic DNA methylation patterns in embryonic and adult cells. Therefore, dysfunction of DNMTs can lead to serious diseases and cancer due to distortions in gene methylation, including that of tumor suppressor genes. Due to the reversibility of DNA methylation, DNMTs are considered an important epigenetic target for drug development. This narrative review summarizes knowledge about DNMTs, including structural features and biological functions, and describes the development of DNMT inhibitors as therapeutics, from the earliest developments to the most modern and promising ones.
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