The drug diazaborine blocks ribosome biogenesis by inhibiting the AAA-ATPase Drg1.

@article{Loibl2014TheDD,
  title={The drug diazaborine blocks ribosome biogenesis by inhibiting the AAA-ATPase Drg1.},
  author={Mathias Loibl and Isabella Klein and Michael Prattes and Claudia Schmidt and Lisa Kappel and Gertrude Zisser and Anna Gungl and Elmar Krieger and Brigitte Pertschy and Helmut Bergler},
  journal={The Journal of biological chemistry},
  year={2014},
  volume={289 7},
  pages={3913-22}
}
The drug diazaborine is the only known inhibitor of ribosome biogenesis and specifically blocks large subunit formation in eukaryotic cells. However, the target of this drug and the mechanism of inhibition were unknown. Here we identify the AAA-ATPase Drg1 as a target of diazaborine. Inhibitor binding into the second AAA domain of Drg1 requires ATP loading and results in inhibition of ATP hydrolysis in this site. As a consequence the physiological activity of Drg1, i.e. the release of Rlp24… CONTINUE READING

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