Article
Identification of allosteric binding sites for PI3Kα oncogenic mutant specific inhibitor design.
Bioorganic & medicinal chemistry - 15 Feb 2017
Miller Michelle S, Maheshwari Sweta, McRobb Fiona M, Kinzler Kenneth W, Amzel L Mario, Vogelstein Bert, Gabelli Sandra B
Abstract excerpt
PIK3CA, the gene that encodes the catalytic subunit of phosphatidylinositol 3-kinase α (PI3Kα), is frequently mutated in breast and other types of cancer. A specific inhibitor that targets the mutant forms of PI3Kα could maximize treatment efficiency while minimizing side-effects. Herein we describe the identification of novel binding pockets that may provide an opportunity for the design of mutant selective...
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