Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha.

@article{Zunder2008DiscoveryOD,
  title={Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha.},
  author={Eli R. Zunder and Zachary A Knight and Benjamin T. Houseman and Beth Apsel and Kevan M. Shokat},
  journal={Cancer cell},
  year={2008},
  volume={14 2},
  pages={180-92}
}
p110 alpha (PIK3CA) is the most frequently mutated kinase in human cancer, and numerous drugs targeting this kinase are currently in preclinical development or early-stage clinical trials. Clinical resistance to protein kinase inhibitors frequently results from point mutations that block drug binding; similar mutations in p110 alpha are likely, but currently none have been reported. Using a S. cerevisiae screen against a structurally diverse panel of PI3K inhibitors, we have identified a… CONTINUE READING

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