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 |
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 |
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 |
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 |
EC Number | General Stability | Organism |
---|---|---|
2.7.11.11 | N-terminal and C-terminal extensions stabilize the catalytic core | Homo sapiens |
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 |
EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|---|
2.7.11.24 | cytosol | - |
Homo sapiens | 5829 | - |
2.7.11.24 | nucleus | - |
Homo sapiens | 5634 | - |
EC Number | Metals/Ions | Comment | Organism | Structure |
---|---|---|---|---|
2.7.11.1 | Mg2+ | - |
Homo sapiens |
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 | - |
? |
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 | - |
- |
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 |
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 | ? | - |
? |
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 |
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 |
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 |