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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 ...
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 ...
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, ...
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. ...
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 ...
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 ...
Synergistic Allostery in Multiligand-Protein Interactions
(Cell Press, 2020-11)
Amide hydrogen-deuterium exchange mass spectrometry is powerful for describing combinatorial coupling effects of a cooperative ligand pair binding at noncontiguous sites: adenosine at the ATP-pocket and a docking peptide ...
The activation loop of PKA catalytic isoforms is differentially phosphorylated by Pkh protein kinases in Saccharomyces cerevisiae
(Portland Press, 2012-09)
PDK1 (phosphoinositide-dependent protein kinase 1) phosphorylates and activates PKA (cAMP-dependent protein kinase) in vitro. Docking of the HM (hydrophobic motif) in the C-terminal tail of the PKA catalytic subunits on ...
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 ...