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epigenetic drugs

Monday 19 April 2010

Epigenetics is central to our understanding of the dynamic and adaptive nature of cancer cell phenotypes that cannot be explained by the constraints of genetic alterations.

DNA methylation and histone modifications are the best characterized of the different layers of epigenetic dysregulation of human tumors.

Both sets of epigenetic marks may also affect DNA sequences that give rise to
microRNAs. The first epigenetic drugs, such as DNA demethylating agents and histone deacetylase inhibitors, are used for the treatment of leukemias and lymphomas.

A new generation of epigenetic drugs targeting histone methyltransferases, histone demethylases, sirtuins, and the microRNA machinery is rapidly emerging.


- zebularine
- 3-deazaneplanocin
- sirtuins

See also

- miRNA drugs