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AGC kinases, mechanisms of regulation and innovative drug development
(Academic Press Ltd - Elsevier Science Ltd, 2018-02)
The group of AGC kinases consists of 63 evolutionarily related serine/threonine protein kinases comprising PDK1, PKB/Akt, SGK, PKC, PRK/PKN, MSK, RSK, S6K, PKA, PKG, DMPK, MRCK, ROCK, NDR, LATS, CRIK, MAST, GRK, Sgk494, ...
Allosteric Regulation of Protein Kinases Downstream of PI3-Kinase Signalling
(Springer, 2019)
Allostery is a basic principle that enables proteins to process and transmit cellular information. Protein kinases evolved allosteric mechanisms to transduce cellular signals to downstream signalling components or effector ...
Bidirectional Allosteric Communication between the ATP-Binding Site and the Regulatory PIF Pocket in PDK1 Protein Kinase
(Cell Press, 2016-10)
Allostery is a phenomenon observed in many proteins where binding of a macromolecular partner or a small-molecule ligand at one location leads to specific perturbations at a site not in direct contact with the region where ...
An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms
(American Chemical Society, 2017-02)
There is a current and pressing need for improved cancer therapies. The use of small molecule kinase inhibitors and their application in combinatorial regimens represent an approach to personalized targeted cancer therapy. ...
STAT3 enhances the constitutive activity of AGC kinases in melanoma by transactivating PDK1
(BioMed Central, 2019-01)
Background: The PI3K/Akt and the STAT3 pathways are functionally associated in many tumor types. Both in vitro and in vivo studies have revealed that either biochemical or genetic manipulation of the STAT3 pathway activity ...
Akt/PKB: one kinase, many modifications
(Portland Press, 2015-06)
Akt/PKB, a serine/threonine kinase member of the AGC family of proteins, is involved in the regulation of a plethora of cellular processes triggered by a wide diversity of extracellular signals and is thus considered a key ...
A Chemical Biology Approach to Understand The Regulation Of Full-Length Phosphoinositide-Dependent Protein Kinase 1 (Pdk1)
(Biocell, 2019)
Phosphoinositide-dependent protein kinase 1 (PDK1) is a master AGC kinase that phosphorylates at least other 23 AGC kinases, being PKB/Aktthe most relevant substrate downstream of PI3-kinase, important for growth and cell ...
Alternative AKT2 splicing produces protein lacking the hydrophobic motif regulatory region
(Public Library of Science, 2020-11)
Three AKT serine/threonine kinase isoforms (AKT1/AKT2/AKT3) mediate proliferation, metabolism, differentiation and anti-apoptotic signals. AKT isoforms are activated downstream of PI3-kinase and also by PI3-kinase independent ...
AKT
(Springer, 2018)
AKT is a serine/threonine kinase member of the AGC family of protein kinases. The three isoforms of AKT (AKT1/2/3) play a central role in growth, proliferation, glucose uptake, metabolism, protein translation and cell ...
PIF-Pocket as a Target for C. albicans Pkh Selective Inhibitors
(American Chemical Society, 2013-08-02)
The phosphoinositide-dependent protein kinase 1, PDK1, is a master kinase that phosphorylates the activation loop of up to 23 AGC kinases. S. cerevisiae has three PDK1 orthologues, Pkh1 −3, which also phosphorylate AGC ...