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Article

Exploring a non-ATP pocket for potential allosteric modulation of PI3Kα.

The journal of physical chemistry. B - 22 Jan 2015

Gkeka Paraskevi, Papafotika Alexandra, Christoforidis Savvas, Cournia Zoe

Abstract excerpt

Allosteric modulators offer a novel approach for kinase inhibition because they target less conserved binding sites compared to the active site; thus, higher selectivity may be obtained. PIK-108, a known pan phosphoinositide 3-kinase (PI3K) inhibitor, was recently detected to occupy a non-ATP binding site in the PI3Kα C-lobe. This newly identified pocket is located close to residue 1047, which is frequently...

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PMID: 25299356
DOI: 10.1021/jp506423e

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