Chemical genetic discovery of targets and anti-targets for cancer polypharmacology

@article{Dar2012ChemicalGD,
  title={Chemical genetic discovery of targets and anti-targets for cancer polypharmacology},
  author={Arvin C. Dar and Tirtha Kamal Das and Kevan M. Shokat and Ross L. Cagan},
  journal={Nature},
  year={2012},
  volume={486},
  pages={80-84}
}
The complexity of cancer has led to recent interest in polypharmacological approaches for developing kinase-inhibitor drugs; however, optimal kinase-inhibition profiles remain difficult to predict. Using a Ret-kinase-driven Drosophila model of multiple endocrine neoplasia type 2 and kinome-wide drug profiling, here we identify that AD57 rescues oncogenic Ret-induced lethality, whereas related Ret inhibitors imparted reduced efficacy and enhanced toxicity. Drosophila genetics and compound… CONTINUE READING
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