Activating Compound | Comment | Organism | Structure |
---|---|---|---|
platelet-derived growth factor receptor-beta | activates the enzyme by tyrosine phosphorylation at Y13, Y86, and Y92, required, the wild-type PDGFRbeta is 60fold more active with GRK2 than PDGFRbeta mutant Y857F, GRK2 activation also increases GRK2 degradation and downregulation, independent of Gbetagamma subunits and phosphoinositide 3-kinase | Bos taurus |
Cloned (Comment) | Organism |
---|---|
expression of HA-tagged GRK2 wild-type and mutants and of FLAG-tagged platelet-derived growth factor receptor-beta wild-type and mutants in HEK-293 cells | Bos taurus |
Protein Variants | Comment | Organism |
---|---|---|
Y13F | site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is reduced with the mutant GRK2, reduced activity compared to the wild-type | Bos taurus |
Y13F/Y86F/Y92F | site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is eliminated with the mutant GRK2, reduced activity compared to the wild-type | Bos taurus |
Y86F | site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is reduced with the mutant GRK2, reduced activity compared to the wild-type | Bos taurus |
Y86F/Y92F | site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is highly reduced with the mutant GRK2, reduced activity compared to the wild-type | Bos taurus |
Y92F | site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is reduced with the mutant GRK2, reduced activity compared to the wild-type | Bos taurus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | platelet-derived growth factor receptor-beta activates the enzyme by tyrosine phosphorylation, the wild-type PDGFRbeta is 60fold more active with GRK2 than PDGFRbeta mutant Y857F, GRK2 activation also increases GRK2 degradation and downregulation | Bos taurus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + platelet-derived growth factor receptor-beta | Bos taurus | feedback inhibition mechanism, overview | ADP + phosphorylated platelet-derived growth factor receptor-beta | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Bos taurus | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | - |
Bos taurus |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + platelet-derived growth factor receptor-beta | feedback inhibition mechanism, overview | Bos taurus | ADP + phosphorylated platelet-derived growth factor receptor-beta | - |
? | |
ATP + platelet-derived growth factor receptor-beta | active with the wild-type and mutant Y740F/Y751F PDGFRbeta, GRK2 phosphorylation desensitizes the PDGF receptor-beta, feedback inhibition mechanism, overview | Bos taurus | ADP + phosphorylated platelet-derived growth factor receptor-beta | - |
? |
Synonyms | Comment | Organism |
---|---|---|
G protein-coupled receptor kinase-2 | - |
Bos taurus |
GRK2 | - |
Bos taurus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Bos taurus |