What is Azacitidine?

Azacitidine is believed to apply its antineoplastic furnishings by causing hypomethylation of DNA and absolute cytotoxicity on aberrant hematopoietic beef in the cartilage marrow. The absorption of azacitidine appropriate for best inhibition of DNA methylation in vitro does not could could cause above abolishment of DNA synthesis. Hypomethylation may restore accustomed action to genes that are analytical for adverse and proliferation. The cytotoxic furnishings of azacitidine could could cause the afterlife of rapidly adding cells, including blight beef that are no best acknowledging to accustomed advance ascendancy mechanisms. Non-proliferating beef are almost aloof to azacitidine. Upon uptake into cells, azacitidine is phosphorylated to 5-azacytidine monophosphate by uridine-cytidine kinase, again to diphosphate by pyrimidine monophosphate kinases and triphosphate by diphosphate kinases. 5-Azacitidine triphosphate is congenital into RNA, arch to the disruption of nuclear and cytoplasmic RNA metabolism and inhibition of protein synthesis. 5-Azacytidine diphosphate is bargain to 5-aza-deoxycytidine diphosphate by ribonucleotide reductase. The resultant metabolite is phosphorylated to 5-azadeoxycitidine triphosphate by nucleoside diphosphate kinases. 5-azadeoxycitidine triphosphate is again incoporated into DNA, arch to inhibition of DNA synthesis. Azacitidine is a lot of baneful during the S-phase of the corpuscle cycle.

Azacitidine is a actinic alternation of the cytosine nucleoside used in DNA and RNA. Azacitidine is anticipation to abet antineoplastic action via two mechanisms; inhibition of DNA methyltransferase at low doses, causing hypomethylation of DNA, and absolute cytotoxicity in aberrant hematopoietic beef in the cartilage bottom through its assimilation into DNA and RNA at top doses, consistent in corpuscle death. As azacitidine is a ribonucleoside, it incoporates into RNA to a beyond admeasurement than into DNA. The assimilation into RNA leads to the dissembly of polyribosomes, abnormal methylation and acceptor action of alteration RNA, and inhibition of the assembly of protein. Its assimilation into DNA leads to a covalent bounden with DNA methyltransferases, which prevents DNA amalgam and consecutive cytotoxicity.