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Literature summary 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

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.1 additional information insulin stimulates GSK3 phosphorylation at Ser21 and Ser9 by PKB protein kinase Homo sapiens
2.7.11.1 PDK1 interacting fragment PIF required for activity of PDK1 Homo sapiens
2.7.11.1 phosphatidylinositol 3,4,5-trisphosphate required by PDK1 for phosphorylation and activation of PKB Homo sapiens
2.7.11.24 additional information interaction motifs, i.e. docking sites or recognition sequences, of substrates are crucial for MAPK activity, i.e. motif Leu-Xaa-Leu preceded by 3-5 basic residues, overview Homo sapiens

Application

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

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.11.24 crystal structure of p38alpha, show docking grooves for binding of substrate D-domains, i.e. of MEF2A, and of activating kinases, e.g. of MKK3b, Ile116 and Gln120 play important roles Homo sapiens

Protein Variants

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

General Stability

EC Number General Stability Organism
2.7.11.11 N-terminal and C-terminal extensions stabilize the catalytic core Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.1 additional information GSK3 phosphorylation and inhibition by PKB protein kinase at S21 and S9 Homo sapiens
2.7.11.11 PKI pseudo-substrate inhibitor Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.24 cytosol
-
 Homo sapiens 5829
-
2.7.11.24 nucleus
-
 Homo sapiens 5634
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.1 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.1 ATP + axin Homo sapiens glycogen synthase kinase 3 ADP + phosphorylated axin
-
 ?
2.7.11.1 ATP + beta-catenin Homo sapiens glycogen synthase kinase 3 ADP + phosphorylated beta-catenin
-
 ?
2.7.11.1 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
-
 ?
2.7.11.1 ATP + glycogen synthase kinase 3 Homo sapiens PKB protein kinase ADP + phosphorylated glycogen synthase kinase 3
-
 ?
2.7.11.1 ATP + PKB protein kinase Homo sapiens PDK1 kinase, phosphorylates Thr308 and Ser473, which is required for activation of PKB ADP + phosphorylated PKB protein kinase
-
 ?
2.7.11.24 ATP + a protein Homo sapiens MAPK activate mitogen-activated proteins in several signal transduction pathways, overview ADP + a phosphoprotein
-
 ?
2.7.11.24 ATP + c-Jun Homo sapiens substrate of JNK ADP + phosphorylated c-Jun
-
 ?
2.7.11.24 ATP + Lin-1 Homo sapiens substrate of ERK2, negative regulation of Lin-1 ADP + phosphorylated Lin-1
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.1 Homo sapiens Q13153
-
-
2.7.11.11 Homo sapiens
-
-
-
2.7.11.24 Homo sapiens P53778
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.1 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)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.1 ATP + axin glycogen synthase kinase 3 Homo sapiens ADP + phosphorylated axin
-
 ?
2.7.11.1 ATP + beta-catenin glycogen synthase kinase 3 Homo sapiens ADP + phosphorylated beta-catenin
-
 ?
2.7.11.1 ATP + glycogen synthase glycogen synthase kinase 3 Homo sapiens ADP + phosphorylated glycogen synthase
-
 ?
2.7.11.1 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
-
 ?
2.7.11.1 ATP + glycogen synthase kinase 3 PKB protein kinase Homo sapiens ADP + phosphorylated glycogen synthase kinase 3
-
 ?
2.7.11.1 ATP + glycogen synthase kinase 3 PKB protein kinase, phosphorylation at S21 and S9 Homo sapiens ADP + phosphorylated glycogen synthase kinase 3
-
 ?
2.7.11.1 ATP + PKB protein kinase PDK1 kinase, phosphorylates Thr308 and Ser473, which is required for activation of PKB Homo sapiens ADP + phosphorylated PKB protein kinase
-
 ?
2.7.11.1 ATP + PKB protein kinase PDK1 kinase Homo sapiens ADP + phosphorylated PKB protein kinase
-
 ?
2.7.11.1 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 ?
-
 ?
2.7.11.11 additional information recognition motif and phosphorylation sequences, substrate binding structure, peptide binding in an extended conformation, N-terminal and C-terminal extensions bind pseudosubstrates Homo sapiens ?
-
 ?
2.7.11.24 ATP + a protein
-
 Homo sapiens ADP + a phosphoprotein
-
 ?
2.7.11.24 ATP + a protein MAPK activate mitogen-activated proteins in several signal transduction pathways, overview Homo sapiens ADP + a phosphoprotein
-
 ?
2.7.11.24 ATP + c-Jun substrate of JNK Homo sapiens ADP + phosphorylated c-Jun
-
 ?
2.7.11.24 ATP + c-Jun substrate of JNK, binding via delta domain of c-Jun substrate Homo sapiens ADP + phosphorylated c-Jun
-
 ?
2.7.11.24 ATP + Lin-1 substrate of ERK2, negative regulation of Lin-1 Homo sapiens ADP + phosphorylated Lin-1
-
 ?
2.7.11.24 ATP + Lin-1 Lin-1 is an ETS transcription factor, substrate of ERK2, binding via the docking sequence of the substrate Homo sapiens ADP + phosphorylated Lin-1
-
 ?
2.7.11.24 additional information interaction motifs of substrates are crucial for MAPK activity, motif Leu-Xaa-Leu preceded by 3-5 basic residues is abundant, docking mechanism in MAPK signalling, the recognition modules can function synergistically or competitively, MAPK determinants recognizing docking motifs, overview Homo sapiens ?
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.1 More enzyme docking sequences and targeting, overview Homo sapiens
2.7.11.11 More the enzyme consists of an N-terminal small lobe and a C-terminal large lobe giving the catalytic core a bean-like structure and stabilizing the enzyme Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.11.1 glycogen synthase kinase 3
-
 Homo sapiens
2.7.11.1 GSK3
-
 Homo sapiens
2.7.11.1 PDK1
-
 Homo sapiens
2.7.11.1 PKB
-
 Homo sapiens
2.7.11.11 cAMP-dependent protein kinase
-
 Homo sapiens
2.7.11.11 PKA
-
 Homo sapiens
2.7.11.24 ERK
-
 Homo sapiens
2.7.11.24 JNK
-
 Homo sapiens
2.7.11.24 MAPK
-
 Homo sapiens
2.7.11.24 p38
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.1 ATP
-
 Homo sapiens
2.7.11.11 ATP binds between two lobes, directing the gamma-phosphate outwards while the adenine ring lies deep in the cleft between the lobes Homo sapiens
2.7.11.24 ATP
-
 Homo sapiens