Azacitidine are DNA Methyltransferase Inhibitors

641 Words Feb 19th, 2018 3 Pages
Azacitidine being an analog for cytidine gets integrated into the DNA sequence of the DNMT gene, the gene turns dysfunctional, inhibiting the DNA methyltransferase enzymes which normally methylate DNA.
Azacitidine is used primarily for the treatment of myelodysplastic syndromes or MDS- a blood disorder which affects the bone marrow leading to a low or ineffective production of blood cells. The cancerous overgrowth of a number of immature cells or blasts and the abnormally developed or dysplastic cells increase, thereby reducing the cell count of normal red blood cells, white blood cells, and platelets.
Azacitidine as a chemotherapeutic drug (in low doses) prevents the body from making nucleic acids required for cell growth of the cancerous cells. This stops the growth of cancer cells and leads to cell death. Azacitidine also appears to help restore normal growth and differentiation (cell specialization) in the cells of the bone marrow. This betters the bone marrow production of normal blood cells.

Discovery:
Azacitidine was first synthesized by Piskala and Sorm in 1964 [Piskala A, Sorm F. (1964). Collect Czech Chem. Commun., 29: 2060-2076]. It was developed as a nucleoside antimetabolite specifically used for the treatment of acute myelogenous leukemia (Cihak, 1974;Sorm et al., 1964).

But studies later revealed that this drug inhibited cell mitosis with high…

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