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azacitidine : ウィキペディア英語版
azacitidine

Azacitidine (INN; trade name Vidaza) is a chemical analogue of cytidine, a nucleoside present in DNA and RNA. Azacitidine and its deoxy derivative, decitabine (also known as 5-aza-2′deoxycytidine), are used in the treatment of myelodysplastic syndrome. Both drugs were first synthesized in Czechoslovakia as potential chemotherapeutic agents for cancer.
==Uses==
Azacitidine is mainly used in the treatment of myelodysplastic syndrome (MDS), for which it received approval by the U.S. Food and Drug Administration on May 19, 2004; it is marketed as Vidaza.〔(Vidaza web site ).〕 In a randomized controlled trial comparing azacitidine to supportive treatment of MDS, around 16% of people receiving the drug had a complete or partial response—blood cell counts and bone marrow morphology returning to normal—and 2/3 patients who required blood transfusions before the study no longer needed them after receiving azacitidine.
It can also be used ''in vitro'' to remove methyl groups from DNA. This may weaken the effects of gene silencing mechanisms that occurred prior to the methylation. Methylation events are therefore believed to secure the DNA in a silenced state. Demethylation may reduce the stability of silencing signals and thus confer relative gene activation.〔Whitelaw E and Garrick D (2005), ''The Epigenome, ''Chapter 7'','' ''In'': ''Mammalian Genomics'', Ed: Ruvinsky A & Marshall Graves JA, CABI Publishing, Wallingford, UK, ISBN 0-85199-910-7.〕
Azacitidine induces tumor regression on IDH1 mutant glioma xenografts in mice.〔Borodovsky, A, et al., "5-azacytidine reduces methylation, promotes differentiation and induces tumor regression in a patient-derived IDH1 mutant glioma xenograft", Oncotarget Advance Publications (2013)〕
In research, 5-azacytidine is commonly used for promoting cardiomyocyte differentiation of adult stem cells, however it is suggested that this drug has a compromised efficacy as a cardiac differentiation factor as it promotes the transdifferentiation of cardiac cells to skeletal myocytes.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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