Definition of the binding mode of a new class of phosphoinositide 3-kinase α-selective inhibitors using in vitro mutagenesis of non-conserved amino acids and kinetic analysis

The binding mechanism of a new class of lipid-competitive, ATP non-competitive, p110α isoform-selective PI3K (phosphoinositide 3-kinase) inhibitors has been elucidated. Using the novel technique of isoform reciprocal mutagenesis of non-conserved amino acids in the p110α and p110β isoforms, we have i...

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Main Authors: Zheng, Zhaohua, Amran, Syazwani I., Zhu, Jiuxiang, Schmidt-Kittler, Oleg, Kinzler, Kenneth W., Vogelstein, Bert, Shepherd, Peter R., Thompson, Philip E., Jennings, Ian G.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3474370/
https://ncbi.nlm.nih.gov/pubmed/22502592
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1042/BJ20120499
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