Decitabine: development of a DNA methyltransferase inhibitor for hematological malignancies.
Decitabine (DAC) is a small molecule nucleotide analog that is incorporated into DNA and traps human DNA methyltransferases. Although initially developed as a cytotoxic agent, low-dose DAC is enjoying a revival as a specific inhibitor of hypermethylation in cancer. DAC has activity in several hematological diseases, especially myelodysplastic syndrome, chronic myelogenous leukemia and acute myeloid leukemia. Clinical and preclinical advances are presented in this review.
Lyons
John
J
jlyons1@ireland.com
Bayar
Emel
E
Fine
Gil
G
McCullar
Michael
M
Rolens
Randee
R
Rubinfeld
Joseph
J
Rosenfeld
Craig
C
D000818:Animals; D001374:Azacitidine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use*; D002986:Clinical Trials as Topic / Q000706:statistics & numerical data; D015254:DNA Modification Methylases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000077209:Decitabine; D004791:Enzyme Inhibitors / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use*; D019337:Hematologic Neoplasms / Q000188:drug therapy* / Q000201:enzymology; D006801:Humans
D004791:Enzyme Inhibitors; D000077209:Decitabine; D015254:DNA Modification Methylases; D001374:Azacitidine