A targeting modality for destruction of RNA polymerase I that possesses anticancer activity.

@article{Peltonen2014ATM,
  title={A targeting modality for destruction of RNA polymerase I that possesses anticancer activity.},
  author={K Peltonen and Laureen Colis and Hester Liu and Rishi Trivedi and Michael S Moubarek and Henna M. Moore and Baoyan Bai and Michelle A. Rudek and Charles J. Bieberich and Marikki Laiho},
  journal={Cancer cell},
  year={2014},
  volume={25 1},
  pages={77-90}
}
We define the activity and mechanisms of action of a small molecule lead compound for cancer targeting. We show that the compound, BMH-21, has wide and potent antitumorigenic activity across NCI60 cancer cell lines and represses tumor growth in vivo. BMH-21 binds GC-rich sequences, which are present at a high frequency in ribosomal DNA genes, and potently and rapidly represses RNA polymerase I (Pol I) transcription. Strikingly, we find that BMH-21 causes proteasome-dependent destruction of… CONTINUE READING
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