The chemical diversity and structure-based discovery of allosteric modulators for the PIF-pocket of protein kinase PDK1

The chemical diversity and structure-based discovery of allosteric modulators for the PIF-pocket of protein kinase PDK1

Phosphoinositide-dependent protein kinase-1 (PDK1) is an important protein in mediating the PI3K-AKT pathway and is thus identified as a promising target. The catalytic activity of PDK1 is tightly regulated by allosteric modulators, which bind to the PDK1 Interacting Fragment (PIF) pocket of the kin...

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Bibliographic Details
Main Authors: Xinyuan Xu, Yingyi Chen, Qiang Fu, Duan Ni, Jian Zhang, Xiaolong Li, Shaoyong Lu
Format: Article
Language:English
Published: Taylor & Francis Group 2019-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
pi3k
pdk1
allosteric modulators
allostery
orthosteric ligands
atp binding site
Online Access:http://dx.doi.org/10.1080/14756366.2018.1553167

Internet

http://dx.doi.org/10.1080/14756366.2018.1553167

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