Article
Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha.
Cancer cell - 12 Aug 2008
Zunder Eli R, Knight Zachary A, Houseman Benjamin T, Apsel Beth, Shokat Kevan M
Abstract excerpt
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...
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