Figure. 7.5. Current drugs targeting various epigenetic machinery.
Histone acetyltransferase inhibitors (HATi) may be effective treatments since HAT proteins are sometimes considered to be tumor promoters. Histone deacetylase inhibitors (HDACi) such as vorinostat (SAHA) and romidepsin have been FDA approved for treatments of certain hematological cancers. SIRT inhibitors (SIRTi) specifically target the SIRT family of histone deacetylases. Histone demethyltransferase inhibitors (HDMi) and histone methylasetransferase (HMTi) have importantly become more selective towards specific marks, since methylation can act as both a repressive and an activating mark. DNA methyltransferase inhibitors (DNMTi) may serve as promising drugs for re-sensitizing certain cancer cells to chemotherapy, and two (vidaza and decitabine) are FDA approved for cancer treatment. (Rodríguez-Paredes et al., 2011)