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 ?
In a set of experiments, three days after the mice were injected with cancer cells, the researchers put the mice on one of four treatment regimens: injections of saline (as a 'control' treatment); an epigenetic drug known as 5-azacytidine (AZA); a polyamine-blocking drug known as 2-difluoromethylornithine (DFMO); or a combination of AZA and DFMO.
In the COZMOS study, the drug 5-azacytidine is used to change the cells stuck in the on position, so that a second chemotherapy drug, carboplatin, can be more active in destroying the cancer.
Persons with an ICD-0-3 subtype consistent with acute promyelocytic leukemia have been excluded as this disease group is typically NOT treated with cytarabine (standard protocol is 5-azacytidine + arsenic).
Abnormal DNA methylation levels via targeted disruption of these genes results in dysmorphologies and even embryonic lethality.[12],[13] Specifically, DNMT3b mutation is involved in the occurrence of instability-facial anomalies.[14],[15] In addition, the inhibition of DNA methylation by 5-azacytidine exposure in utero leads to CP in fetuses.[16] It has been reported that epigenetic control by imprinting could contribute to oral and craniofacial diseases.[17] Even with the active investigation of genetic associations in NSCL and NSCL/P, direct evidence of epigenetic control in candidate regions and at the genome-wide level remains unreported.
Nevertheless, although a recently completed clinical trial demonstrated promising results in the combination of an HDAC inhibitor, Entinostat, and DNA-demethylating agent, 5-azacytidine, in advanced chemorefractory NSCLC, there is not a HDAC inhibitor that is approved for lung cancer treatment.
Variants in body morphs, such as Daphnia exhibiting a helmet or a neck tooth formation, are induced in response to the presence of predators, whereas variants in body length (e.g., growth) and reproduction (e.g., number of progeny) have been shown to be sensitive to chemical inhibitors of DNA methylation such as 5-azacytidine (5-aza) and the pesticide vinclozolin (Vandegehuchte et al.
It has been shown that cisplatin as well as 5-azacytidine touch off cytotoxic and growth inhibitory effects in vitro by demethylating the promoters of ESR1, BRCA1, RASSF1A, MLH1, MYOD1, hTERT, and DAPK1 to reexpress these tumor-associated genes [94].
Ratajczak, "5-Azacytidine inhibits human rhabdomyosarcoma cell growth by downregulating insulin-like growth factor 2 expression and reactivating the H19 gene product miR-675, which negatively affects insulin-like growth factors and insulin signaling," International Journal of Oncology, vol.
Vesely, "5-Azacytidine, a new, highly effective cancerostatic," Experientia, vol.
For example, the DNA demethylating agent 5-azacytidine was extensively described to enhance the differentiation of SCs into cardiac-like cells in vitro [121-124].
Repression of DNMT by 5-azacytidine reactivates miR-296-5p.
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