Demethylating agent

Demethylating agents are chemical substances that can inhibit methylation, resulting in the expression of the previously hypermethylated silenced genes (see Methylation#Cancer for more detail). Cytidine analogs such as 5-azacytidine (azacitidine) and 5-azadeoxycytidine (decitabine) are the most commonly used demethylating agents. They work by inhibiting DNA methyltransferases.[1] Both compounds have been approved in the treatment of myelodysplastic syndrome (MDS) by Food and Drug Administration (FDA) in United States. Azacitidine and decitabine are marketed as Vidaza and Dacogen respectively. Azacitidine is the first drug to be approved by FDA for treating MDS and has been given orphan drug status.[2][3] Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells.[4]

References

  1. ↑ Holliday, R.; Ho, T. (2002). "DNA methylation and epigenetic inheritance". Methods. 27 (2): 179–83. doi:10.1016/S1046-2023(02)00072-5. PMID 12095278.
  2. ↑ Issa, J. P., Kantarjian, H. M. and Kirkpatrick, P. (2005). "Azacitidine". Nat Rev Drug Discov. 4 (4): 275–6. doi:10.1038/nrd1698. PMID 15861567.
  3. ↑ Gore, S. D., Jones, C. and Kirkpatrick, P. (2006). "Decitabine". Nat Rev Drug Discov. 5 (11): 891–2. doi:10.1038/nrd2180. PMID 17117522.
  4. ↑ Villar-Garea A, Fraga MF, Espada J, Esteller M (2003). "Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells" (PDF). Cancer Research. 63 (16): 4984–9. PMID 12941824.
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