A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation.

@article{Datta2009ANC,
  title={A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation.},
  author={Jharna Datta and Kalpana Ghoshal and William A. Denny and Swarna A. Gamage and Darby G. Brooke and Pasit Phiasivongsa and Sanjeev Redkar and S. T. Jacob},
  journal={Cancer research},
  year={2009},
  volume={69 10},
  pages={4277-85}
}
Reactivation of silenced tumor suppressor genes by 5-azacytidine (Vidaza) and its congener 5-aza-2'-deoxycytidine (decitabine) has provided an alternate approach to cancer therapy. We have shown previously that these drugs selectively and rapidly induce degradation of the maintenance DNA methyltransferase (DNMT) 1 by a proteasomal pathway. Because the toxicity of these compounds is largely due to their incorporation into DNA, it is critical to explore novel, nonnucleoside compounds that can… CONTINUE READING
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