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] There are many other demethylating agents that can be used to inhibit the growth of other diseases. [5]
^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.
^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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
^Gore, S. D., Jones, C. and Kirkpatrick, P. (2006). "Decitabine". Nat Rev Drug Discov. 5 (11): 891–2. doi:10.1038/nrd2180. PMID 17117522.{{cite journal}}: CS1 maint: multiple names: authors list (link)
^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.
^Cite error: The named reference pmid26317465 was invoked but never defined (see the help page).
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A hypomethylating agent (or demethylatingagent) is a drug that inhibits DNA methylation: the modification of DNA nucleotides by addition of a methyl...
contributes to the atherosclerotic lesion. An ex vivo experiment using the demethylatingagent Decitabine (5-aza-2 -deoxycytidine) was shown to induce MCT3 expression...
levels from cancer cell lines before and after treatment with a demethylatingagent Since bisulfite sequencing is considered the gold standard for measuring...
Fraga, MF; Espada, J; Esteller, M (Aug 15, 2003). "Procaine is a DNA-demethylatingagent with growth-inhibitory effects in human cancer cells". Cancer Research...
Lübbert M, Silverman LR (January 2014). "Clinical development of demethylatingagents in hematology". The Journal of Clinical Investigation. 124 (1): 40–6...
1994. " Expression of the MAGE1 tumor antigen is upregulated by the demethylatingagent 5-aza-2'-deoxycytidine ". Cancer Research. 54(7): 1766-1771. De Smet...
Imazeki F, et al. (2007). "Methylation status of genes upregulated by demethylatingagent 5-aza-2'-deoxycytidine in hepatocellular carcinoma". Oncology. 71...
efficiency of epigenetic regulating molecules. For example, Zebularine, a demethylatingagent, could be used to remove the methyl groups from the CpGs of the dlc1...
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silencing with synergistic combination of HDAC inhibitors or HDI and DNA-demethylatingagents. HDIs are primarily used as adjunct therapy in several cancer types...
shown that halomon and a related halogenated monoterpene may act as demethylatingagents, suggesting a possible mechanism of action for the pharmacological...
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recruits TET1 to the 8-OHdG lesion (see Figure). This allows TET1 to demethylate an adjacent methylated cytosine. Demethylation of cytosine is an epigenetic...
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in the thesis of Dr. D. L. Romanowsky in the 1890s), it gets serially demethylated and forms all the tri-, di-, mono- and non-methyl intermediates, which...
methylation of the MCPs will increase (because CheB-P is not present to demethylate). The MCPs no longer respond to the attractant when they are fully methylated;...
5(10)-testosterone Prostanozol – 17β-tetrahydropyran ether of the 17α-demethylated analogue of stanozolol List of androgens/anabolic steroids List of estrogen...
recruits the demethylating enzyme TET1 to an association, and brings TET1 to about 600 locations on the genome where TET1 can then demethylate and activate...
[62099-12-1] Whittington RM (May 1963). "Mephentermine Sulphate as a Hypertensive Agent in General Practice". The Journal of the College of General Practitioners...
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based on a combination of eosin plus (chemically reduced eosin) and demethylated methylene blue (containing its oxidation products azure A and azure B)...
the cytochrome P450 isozyme CYP2B6, CYP2D6, and CYP3A4, being O- and N-demethylated to five different metabolites. Of these, desmetramadol (O-desmethyltramadol)...
monoamine oxidase (MAO). It is used as an antidepressant and anxiolytic agent in the clinical treatment of mood and anxiety disorders, respectively. Tranylcypromine...