Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 18, Issue 28, Pages 2448-2457Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026619666181120150122
Keywords
Epigenetic; DNA methylation; Inhibitor; Selectivity; Nucleoside; Cancer
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Funding
- Natural Science Foundation of the Jiangsu Higher Education Institutions of China [18KJA350001]
- National Natural Science Foundation of China [21302134]
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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 overex-pressed 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.
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