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Demethylating agent information


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]

  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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.
  5. ^ Cite error: The named reference pmid26317465 was invoked but never defined (see the help page).

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Demethylating agent

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approved demethylating agents for the treatment of solid tumors which can be a focus of research in the future. Treatment utilizing demethylating agents can...

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Hypomethylating agent

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A hypomethylating agent (or demethylating agent) is a drug that inhibits DNA methylation: the modification of DNA nucleotides by addition of a methyl...

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TIMP1

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in Human Placenta and Fetal Membranes by lipopolysaccharide and demethylating agent 5-aza-2'-deoxycytidine". Reproductive Biology and Endocrinology....

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DNA methylation

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contributes to the atherosclerotic lesion. An ex vivo experiment using the demethylating agent Decitabine (5-aza-2 -deoxycytidine) was shown to induce MCT3 expression...

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Cancer epigenetics

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levels from cancer cell lines before and after treatment with a demethylating agent Since bisulfite sequencing is considered the gold standard for measuring...

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Peter DeMarco

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Fraga, MF; Espada, J; Esteller, M (Aug 15, 2003). "Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells". Cancer Research...

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Azacitidine

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Lübbert M, Silverman LR (January 2014). "Clinical development of demethylating agents in hematology". The Journal of Clinical Investigation. 124 (1): 40–6...

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Tumor antigens recognized by T lymphocytes

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1994. " Expression of the MAGE1 tumor antigen is upregulated by the demethylating agent 5-aza-2'-deoxycytidine ". Cancer Research. 54(7): 1766-1771. De Smet...

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CSRP1

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Imazeki F, et al. (2007). "Methylation status of genes upregulated by demethylating agent 5-aza-2'-deoxycytidine in hepatocellular carcinoma". Oncology. 71...

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DLC1

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efficiency of epigenetic regulating molecules. For example, Zebularine, a demethylating agent, could be used to remove the methyl groups from the CpGs of the dlc1...

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CTAG1B

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The effect of DNA demethylation is evident by the capability of demethylating agents, such as 5-aza-2-deoxycytidine, to induce CTAs re-expression in tumour...

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Chromatin remodeling

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silencing with synergistic combination of HDAC inhibitors or HDI and DNA-demethylating agents. HDIs are primarily used as adjunct therapy in several cancer types...

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Halomon

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shown that halomon and a related halogenated monoterpene may act as demethylating agents, suggesting a possible mechanism of action for the pharmacological...

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Desmetramadol

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opioid analgesic and the main active metabolite of tramadol. Tramadol is demethylated by the liver enzyme CYP2D6 to desmetramadol in the same way as codeine...

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Baeocystin

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psilocybin, norbaeocystin, aeruginascin, and psilocin. Baeocystin is an N-demethylated derivative of psilocybin, and a phosphorylated derivative of 4-HO-NMT...

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DNA repair

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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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Norbaeocystin

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it is a derivative. Norbaeocystin is an N-demethylated derivative of baeocystin (itself an N-demethylated derivative of psilocybin), and a phosphorylated...

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Anabolic steroid

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aromatized. AAS that are 17α-alkylated (and not also 4,5α-reduced or 19-demethylated) are also aromatized but to a lesser extent than is testosterone. However...

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Methylene blue

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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...

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Chemotaxis

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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;...

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List of androgen esters

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5(10)-testosterone Prostanozol – 17β-tetrahydropyran ether of the 17α-demethylated analogue of stanozolol List of androgens/anabolic steroids List of estrogen...

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Epigenetics

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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...

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Mephentermine

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[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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Pethidine

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phenylpiperidine class. Synthesized in 1938 as a potential anticholinergic agent by the German chemist Otto Eisleb, its analgesic properties were first recognized...

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Staining

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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)...

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Tramadol

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the cytochrome P450 isozyme CYP2B6, CYP2D6, and CYP3A4, being O- and N-demethylated to five different metabolites. Of these, desmetramadol (O-desmethyltramadol)...

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Tranylcypromine

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monoamine oxidase (MAO). It is used as an antidepressant and anxiolytic agent in the clinical treatment of mood and anxiety disorders, respectively. Tranylcypromine...

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