Sorm and Vesely first described the pyrimidine analogs 5-aza-2′-deoxycytidine and 5-azacytidine in the mid-1960. They were generally considered to be in the antimetabolite class of anticancer agents; however, unique actions of 5-aza-2′-deoxycytidine clearly extend these molecules beyond the realm of most other antimetabolites. 5-Aza-2′-deoxycytidine and 5-azacytidine may be better considered as the prototypical agents of an emergent class of therapeutic agents, epigenetic modifiers (epigenetics, epigenetic therapy). The most notable epigenetic effect of these 5-aza-pyrimidines is their ability to demethylate the DNA of proliferating cells, and these drugs are now classified as DNA demethylating agents (methylation). To attain therapeutic efficacy, enzymatic activation of...
KeywordsEpigenetic Landscape Transcriptional Reprogram Pyrimidine Analog Epigenetic Gene Silence Epigenetic Switch
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