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Mini-Reviews in Medicinal Chemistry

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ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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Mini-Review Article

DNA Methyltransferase 3A: A Significant Target for the Discovery of Inhibitors as Potent Anticancer Drugs

Author(s): Qixun Feng, Honggao Duan, Xinglong Zhou, Yuning Wang, Jinda Zhang, Haoge Zhang, Guoliang Chen* and Xuefei Bao*

Volume 24, Issue 5, 2024

Published on: 21 September, 2023

Page: [507 - 520] Pages: 14

DOI: 10.2174/1389557523666230825100246

Price: $65

Abstract

DNA methyltransferase (DNMT) is a conserved family of Cytosine methylases, which plays a crucial role in the regulation of Epigenetics. They have been considered promising therapeutic targets for cancer. Among the DNMT family, mutations in the DNMT3A subtype are particularly important in hematologic malignancies. The development of specific DNMT3A subtype inhibitors to validate the therapeutic potential of DNMT3A in certain diseases is a significant task. In this review, we summarized the small molecule inhibitors of DNMT3A discovered in recent years and their inhibitory activities, and classified them based on their inhibitory mechanisms.

Keywords: DNMT, DNMT3A, SAM, DNMT inhibitors, epigenetic modification, cancer.

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Graphical Abstract

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