5-Aza-cytidine is a potent inhibitor of DNA methyltransferase 3a and induces apoptosis in HCT-116 colon cancer cells via Gadd45- and p53-dependent mechanisms.

@article{SchneiderStock20045AzacytidineIA,
  title={5-Aza-cytidine is a potent inhibitor of DNA methyltransferase 3a and induces apoptosis in HCT-116 colon cancer cells via Gadd45- and p53-dependent mechanisms.},
  author={Regine Schneider-Stock and Mona Diab-Assef and Astrid Rohrbeck and Charlotte Foltzer-Jourdainne and Carsten Boltze and Roland Hartig and Peter Sch{\"o}nfeld and Albert Roessner and Hala Gali-Muhtasib},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2004},
  volume={312 2},
  pages={
          525-36
        }
}
Methyltransferase inhibitors commonly used in clinical trials promote tumor cell death, but their detailed cytotoxic action is not yet fully understood. A deeper knowledge about their apotosis-inducing mechanisms and their interaction with DNA methyltransferases (DNMTs) DNMT1, DNMT3a, and DNMT3b might allow the design of more effective drugs with lower cytotoxicity. 5-aza-cytidine (5-aza-CR), a potent inhibitor of DNMT1, is known to induce demethylation and reactivation of silenced genes. In… CONTINUE READING
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