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Literature summary for 2.7.11.1 extracted from

  • Biondi, R.M.; Nebreda, A.R.
    Signalling specificity of Ser/Thr protein kinases through docking-site-mediated interactions (2003), Biochem. J., 372, 1-13.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.11.1

Activating Compound

Activating Compound Comment Organism Structure
additional information insulin stimulates GSK3 phosphorylation at Ser21 and Ser9 by PKB protein kinase Homo sapiens
PDK1 interacting fragment PIF required for activity of PDK1 Homo sapiens
phosphatidylinositol 3,4,5-trisphosphate required by PDK1 for phosphorylation and activation of PKB Homo sapiens

Application

Application Comment Organism
drug development protein kinases are major targets for drug development and design in the pharmaceutical industry Homo sapiens

Protein Variants

Protein Variants Comment Organism
I119A site-directed mutagenesis of a PIF pocket residue of PDK1, mutant shows reduced activity compared to the wild-type enzyme Homo sapiens
additional information mutation of Leu155 and Lys115, residues of the PIF pocket of PDK1, results in 4fold higher PDK1 activity Homo sapiens
Q150A site-directed mutagenesis of a PIF pocket residue of PDK1, mutant shows reduced activity compared to the wild-type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information GSK3 phosphorylation and inhibition by PKB protein kinase at S21 and S9 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + axin Homo sapiens glycogen synthase kinase 3 ADP + phosphorylated axin
-
 ?
ATP + beta-catenin Homo sapiens glycogen synthase kinase 3 ADP + phosphorylated beta-catenin
-
 ?
ATP + glycogen synthase Homo sapiens glycogen synthase kinase 3 is involved in the insulin signaling pathway regulating glycogen synthesis via glycogen synthase antagonizing insulin ADP + phosphorylated glycogen synthase
-
 ?
ATP + glycogen synthase kinase 3 Homo sapiens PKB protein kinase ADP + phosphorylated glycogen synthase kinase 3
-
 ?
ATP + PKB protein kinase Homo sapiens PDK1 kinase, phosphorylates Thr308 and Ser473, which is required for activation of PKB ADP + phosphorylated PKB protein kinase
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q13153
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein insulin-induced GSK3 phosphorylation and inhibition by PKB protein kinase at S21 and S9, phosphorylation at Thr308 and Ser473 of PKB leading to activation of PKB by PDK1 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + axin glycogen synthase kinase 3 Homo sapiens ADP + phosphorylated axin
-
 ?
ATP + beta-catenin glycogen synthase kinase 3 Homo sapiens ADP + phosphorylated beta-catenin
-
 ?
ATP + glycogen synthase glycogen synthase kinase 3 Homo sapiens ADP + phosphorylated glycogen synthase
-
 ?
ATP + glycogen synthase glycogen synthase kinase 3 is involved in the insulin signaling pathway regulating glycogen synthesis via glycogen synthase antagonizing insulin Homo sapiens ADP + phosphorylated glycogen synthase
-
 ?
ATP + glycogen synthase kinase 3 PKB protein kinase Homo sapiens ADP + phosphorylated glycogen synthase kinase 3
-
 ?
ATP + glycogen synthase kinase 3 PKB protein kinase, phosphorylation at S21 and S9 Homo sapiens ADP + phosphorylated glycogen synthase kinase 3
-
 ?
ATP + PKB protein kinase PDK1 kinase, phosphorylates Thr308 and Ser473, which is required for activation of PKB Homo sapiens ADP + phosphorylated PKB protein kinase
-
 ?
ATP + PKB protein kinase PDK1 kinase Homo sapiens ADP + phosphorylated PKB protein kinase
-
 ?
additional information substrate specificity of PDK1, PDK1 binds the hydrophobic motif of substrates via its PIF pocket, GSK3 substrates need to bind tightly to the enzyme for phosphorylation Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
More enzyme docking sequences and targeting, overview Homo sapiens

Synonyms

Synonyms Comment Organism
glycogen synthase kinase 3
-
 Homo sapiens
GSK3
-
 Homo sapiens
PDK1
-
 Homo sapiens
PKB
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens