Article
Structural effects of oncogenic PI3Kα mutations.
Current topics in microbiology and immunology - 1 Jan 2010
Gabelli Sandra B, Huang Chuan-Hsiang, Mandelker Diana, Schmidt-Kittler Oleg, Vogelstein Bert, Amzel L Mario
Abstract excerpt
Physiological activation of PI3Kα is brought about by the release of the inhibition by p85 when the nSH2 binds the phosphorylated tyrosine of activated receptors or their substrates. Oncogenic mutations of PI3Kα result in a constitutively activated enzyme that triggers downstream pathways that increase tumor aggressiveness and survival. Structural information suggests that some mutations also activate the enzyme...
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