5-azacytidine


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5-azacytidine

A chemical analogue of the nucleoside cytidine which cells incorporate into DNA during replication and RNA during transcription; it inhibits methyltransferase resulting in demethylation of the sequence, affecting the binding of cell regulatory proteins to the DNA/RNA substrate. It is used to manage myelodysplastic syndromes.
 
Adverse effects
Anaemia, nausea, vomiting, diarrhoea, decreased blood pressure, liver defects, pulmonary oedema.
References in periodicals archive ?
Several of these newly discovered mutations raise the possibility of targeting subpopulations of JMML cases with existing drugs: Janus kinase (JAK) inhibitors, currently used to treat certain other bone marrow and blood cancers such as polycythemia vera, might inhibit signaling through a hyperactive JAK-STAT pathway identified in some patients, while other agents such as 5-azacytidine, most commonly used as a treatment for a blood disorder known as myelodysplastic syndrome, could be used to reduce excessive epigenetic DNA methylation seen in others.
The impact of 5-azacytidine on placental weight, glycoprotein pattern and proliferating cell nuclear antigen expression in rat placenta.
Myogenic cells derived from rat bone marrow mesenchymal stem cells exposed to 5-azacytidine.
Delivery of 5-azacytidine to human cancer cells by elaidic acid esterification increases therapeutic drug efficacy.
As additional support for the correlation between histone acetylation and DNA methylation, it was reported that treatment of round spermatid injection (ROSI) zygotes with TSA rather than with 5-azacytidine, a DNA methyltransferase inhibitor, results in significantly reduced DNA methylation level (Kishigami et al.
The comparative effects of 5-azacytidine and dihydro-5-azacytidine on polysomal RNA in Ehrlich ascites cells in vitro.
They chose 5-azacytidine, which is approved to treat a pre-leukemia condition called myelodysplastic syndrome and is being tested on lung and other cancers at Johns Hopkins and elsewhere.
Treatment of T-cell lines with an agent called 5-azacytidine, which inhibits DNA methylation, leads to the production of cytokines not normally produced by these cells, including IL-2 and IFN[gamma] (Ballas 1984; Young et al.
Remethylation is critical for zygotic genome activation and normal somatic development; exposure of zebrafish embryos to 5-azacytidine (5-azaC; a potent inhibitor of DNA methylation) only during cleavage results in gDNA hypomethylation and developmental abnormalities, including shortened tail or loss of tail, block-shaped somites, and enlarged pericardial cavity (Martin et al.
When combined with various nucleoside analogues clinically used in AML therapy such as Ara-C, clofarabine, and demethylating agents decitabine and 5-azacytidine, TL32711 synergistically enhanced apoptotic cell death in AML cells and AML stem/progenitor cells.
As an independent assay of DNA methylation, Histoplasma capsulatum (Downs strain) was grown in the presence of the cytosine analogue, 5-Azacytidine.

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