DNA Methyltransferase Inhibitors and their Therapeutic Potential

Author(s): Zehao Zhou, Huan-Qiu Li*, Feng Liu*

Journal Name: Current Topics in Medicinal Chemistry

Volume 18 , Issue 28 , 2018

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Graphical Abstract:


Aberrant DNA methylation at the 5-position of cytosine, catalyzed by DNA methyltransferases (DNMTs), is associated with not only various cancers by silencing of tumor suppressor genes but also other diseases. The DNMTs, especially the DNMT1, DNMT3A and DNMT3B, are often overexpressed in various cancer tissues and cell lines. DNMTs are important epigenetic targets for drug development since the DNA methylation is reversible. This review summarizes an array of nucleoside and non-nucleoside inhibitors of DNMTs, as well as their biological activities. Among these inhibitors, the nucleoside analogue azacytidine and its deoxy derivative decitabine are both irreversible DNMT inhibitors and approved for the treatment of myelodysplastic syndrome.

Keywords: Epigenetic, DNA methylation, Inhibitor, Selectivity, Nucleoside, Cancer.

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Article Details

Year: 2018
Published on: 12 February, 2019
Page: [2448 - 2457]
Pages: 10
DOI: 10.2174/1568026619666181120150122
Price: $65

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