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Structural comparisons of class I phosphoinositide 3-kinases.


ABSTRACT: Class I phosphoinositide 3-kinases (PI3Ks) are lipid kinases that regulate cell growth. One of these kinases, PI3Kalpha, is frequently mutated in diverse tumour types. The recently determined structure of PI3Kalpha reveals features that distinguish this enzyme from related lipid kinases. In addition, wild-type PI3Kgamma differs from PI3Kalpha by a substitution identical to a PI3Kalpha oncogenic mutant (His1047Arg) that might explain the differences in the enzymatic activities of the normal and mutant PI3Kalpha. Comparison of the PI3K structures also identified structural features that could potentially be exploited for the design of isoform-specific inhibitors.

SUBMITTER: Amzel LM 

PROVIDER: S-EPMC2847604 | biostudies-literature | 2008 Sep

REPOSITORIES: biostudies-literature

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Structural comparisons of class I phosphoinositide 3-kinases.

Amzel L Mario LM   Huang Chuan-Hsiang CH   Mandelker Diana D   Lengauer Christoph C   Gabelli Sandra B SB   Vogelstein Bert B  

Nature reviews. Cancer 20080901 9


Class I phosphoinositide 3-kinases (PI3Ks) are lipid kinases that regulate cell growth. One of these kinases, PI3Kalpha, is frequently mutated in diverse tumour types. The recently determined structure of PI3Kalpha reveals features that distinguish this enzyme from related lipid kinases. In addition, wild-type PI3Kgamma differs from PI3Kalpha by a substitution identical to a PI3Kalpha oncogenic mutant (His1047Arg) that might explain the differences in the enzymatic activities of the normal and m  ...[more]

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