Induced protein degradation: an emerging drug discovery paradigm

@article{Lai2017InducedPD,
  title={Induced protein degradation: an emerging drug discovery paradigm},
  author={Ashton C. Lai and Craig M Crews},
  journal={Nature Reviews Drug Discovery},
  year={2017},
  volume={16},
  pages={101-114}
}
Small-molecule drug discovery has traditionally focused on occupancy of a binding site that directly affects protein function, and this approach typically precludes targeting proteins that lack such amenable sites. Furthermore, high systemic drug exposures may be needed to maintain sufficient target inhibition in vivo, increasing the risk of undesirable off-target effects. Induced protein degradation is an alternative approach that is event-driven: upon drug binding, the target protein is… CONTINUE READING
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Small-Molecule Kinase Downregulators.

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  • 2017
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Bivalent Ligands for Protein Degradation in Drug Discovery

  • Computational and structural biotechnology journal
  • 2019
VIEW 1 EXCERPT
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References

Publications referenced by this paper.
SHOWING 1-10 OF 217 REFERENCES

Degradation of Akt using protein-catalyzed capture agents.

  • Journal of peptide science : an official publication of the European Peptide Society
  • 2016

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