Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

5-aza-2′ Deoxycytidine

  • Bernard W. FutscherEmail author
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_503-2



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...


Epigenetic Landscape Transcriptional Reprogram Pyrimidine Analog Epigenetic Gene Silence Epigenetic Switch 
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  1. Christman JK (2002) 5-Azacytidine and 5-aza-2′-deoxycytidine as inhibitors of DNA methylation: mechanistic studies and their implications for cancer therapy. Oncogene 21:5483–5495CrossRefPubMedGoogle Scholar
  2. Jones PA (1985) Altering gene expression with 5-azacytidine. Cell 40(3):485–486CrossRefPubMedGoogle Scholar
  3. Jones PA, Bay SB (2007) The epigenomics of cancer. Cell 128:683–912CrossRefPubMedPubMedCentralGoogle Scholar
  4. Jones PA, Baylin SB (2002) The fundamental role of epigenetic events in cancer. Nat Rev Genet 3:415–428CrossRefPubMedGoogle Scholar
  5. Silverman LR, Mufti GJ (2005) Methylation inhibitor therapy in the treatment of myelodysplastic syndrome. Nat Clin Pract Oncol 2(Suppl 1):S12–S23CrossRefPubMedGoogle Scholar

See Also

  1. (2012) Hypomethylation. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 1791. doi: 10.1007/978-3-642-16483-5_2922Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  1. 1.Department of Pharmacology and Toxicology, Arizona Cancer Center and College of PharmacyUniversity of ArizonaTucsonUSA