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 | Comment | Organism |
---|---|---|
drug development | protein kinases are major targets for drug development and design in the pharmaceutical industry | Homo sapiens |
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 | Comment | Organism | Structure |
---|---|---|---|
additional information | GSK3 phosphorylation and inhibition by PKB protein kinase at S21 and S9 | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q13153 | - |
- |
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 | 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 | Comment | Organism |
---|---|---|
More | enzyme docking sequences and targeting, overview | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
glycogen synthase kinase 3 | - |
Homo sapiens |
GSK3 | - |
Homo sapiens |
PDK1 | - |
Homo sapiens |
PKB | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |