Demethylating agent

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Demethylating agents are compounds that can inhibit methylation, resulting in the expression of the previously hypermethylated silenced genes (see methylation: methylation and cancer for more detail). Cytidine analogs such as 5-azacytidine (azacitidine) and 5-azadeoxycytidine (decitabine) are the most commonly used demethylating agents . These compounds work by binding to the enzymes that catalyse the methylation reaction, DNA methyltransferases; and titrate out these enzymes [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].


[edit] References

  1. ^ Holliday, R. and Ho, T. (2002). "DNA methylation and epigenetic inheritance". Methods 27 (2): 179-83. PMID 12095278. 
  2. ^ Issa, J. P., Kantarjian, H. M. and Kirkpatrick, P. (2005). "Azacitidine". Nat Rev Drug Discov 4 (4): 275-6. PMID 15861567. 
  3. ^ Gore, S. D., Jones, C. and Kirkpatrick, P. (2006). "Decitabine". Nat Rev Drug Discov 5 (11): 891-2. PMID 17117522.