Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases.

@article{Brckner2005EpigeneticRO,
  title={Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases.},
  author={B. Br{\"u}ckner and Regine Garc{\'i}a Boy and Pawel Siedlecki and Tanja Musch and H Christian Kliem and Piotr Zielenkiewicz and S{\'a}ndor Suhai and Manfred Wiessler and Frank Lyko},
  journal={Cancer research},
  year={2005},
  volume={65 14},
  pages={6305-11}
}
DNA methylation regulates gene expression in normal and malignant cells. The possibility to reactivate epigenetically silenced genes has generated considerable interest in the development of DNA methyltransferase inhibitors. Here, we provide a detailed characterization of RG108, a novel small molecule that effectively blocked DNA methyltransferases in vitro and did not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of the compound… CONTINUE READING
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