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PDPK1 (3 Phosphoinositide Dependent Protein Kinase 1) phosphorylates AGC kinases. PDPK1 activates conventional PKC and PKC zeta through phosphorylation of critical threonine residues in the activation loop. PDPK1 also phosphorylates Protein Kinase B (PKB) at threonine 308 in the presence of phosphatidylinositol-3,4,5-trisphosphate. Active Akt inactivates Glycogen Synthase Kinase 3 (GSK3), eventually leading to the dephosphorylation and activation of glycogen synthase, and the stimulation of glycogen synthesis. Because of the role that PDPK1 plays in insulin-induced glycogen synthesis and PKC activation, it is a potentially important target for metabolic drug research.
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