Recent Advances in Searching for DNMT Inhibitors and Their Potential Application in Treating Human Diseases

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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Publication Details

Journal
International Journal of Molecular Sciences
Published
2026-05-19
DOI
https://doi.org/10.3390/ijms27104560
Primary Topic
Epigenetics and DNA Methylation
Type
article
Field-Weighted Citation Impact
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article

Recent Advances in Searching for DNMT Inhibitors and Their Potential Application in Treating Human Diseases

International Journal of Molecular Sciences
Epigenetics and DNA Methylation
article

Recent Advances in Searching for DNMT Inhibitors and Their Potential Application in Treating Human Diseases

article en

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.

International Journal of Molecular SciencesVol. 27(10)
Novosibirsk State University (RU), Institute of Chemical Biology and Fundamental Medicine (RU), Siberian Branch of the Russian Academy of Sciences (RU)
Good health and well-being
Openalex Percentile: Top 8%
Epigenetics and DNA Methylation
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