Journal
DRUG DISCOVERY TODAY
Volume 24, Issue 12, Pages 2323-2331Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2019.08.006
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Funding
- National Science & Technology Major Project of China 'Key New Drug Creation and Manufacturing Program' [2018ZX09711002-007]
- National Natural Science Foundation of China [21603189, 21575128, 81773632]
- Zhejiang Provincial Natural Science Foundation of China [LZ19H300001]
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DNA methyltransferases (DNMTs) are a conserved family of cytosine methylases with crucial roles in epigenetic regulation. They have been considered as promising therapeutic targets for the epigenetic treatment of cancer. Therefore, DNMT inhibitors (DNMTis) have attracted considerable interest in recent years for the modulation of the aberrant DNA methylation pattern in a reversible way. In this review, we provide a structure-based overview of the therapeutic importance of DNMTs against different cancer types, and then summarize recently investigated DNMTis as well as their inhibitory mechanisms, focusing on recent advances in the development of DNMTis with specificity and/or selectivity using computational approaches.
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