Activating Compound | Comment | Organism | Structure |
---|---|---|---|
arrestins | arrestins modulate the enzyme activity having a regulatory role, regulation of arrestins, overview | Mus musculus | |
additional information | autophosphorylation of GRK5 is stimulated by phospholipids, such as phosphatidylinositol-4,5-bisphosphate | Mus musculus |
Protein Variants | Comment | Organism |
---|---|---|
additional information | phenotypes of several GRK and arrestin knockout mice mutants and of transgenic mice overexpressing GRK4 or GRK5, overview | Mus musculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Ca2+/calmodulin | inhibit GRK5 with an IC50 of 40-50 nM, inhibition mechanism via inducing inhibitory autophosphorylation and blocking of membrane association | Mus musculus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
plasma membrane | constitutive association, location of GRK4-6 near the activated receptors, covalent attachment by fatty acids to the C-terminus, e.g. palmitoylated GRK4 and GRK6, or by electrostatic interactions with phospholipids, e.g. for GRK5 | Mus musculus | 5886 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Mus musculus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + beta-adrenergic receptor | Mus musculus | desensitization of the receptor by GRK4, GRK5, and GRK6 | ADP + phosphorylated beta-adrenergic receptor | - |
? | |
ATP + G protein-coupled receptor | Mus musculus | phosphorylation has a regulatory role | ADP + phosphorylated G protein-coupled receptor | - |
? | |
additional information | Mus musculus | G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mus musculus | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
lipoprotein | GRK4-6 are permanently modulated by fatty acids and/or phospholipids | Mus musculus |
phosphoprotein | regulation of GRK5 by phosphorylation through PKC, GRK5 is activated by autophosphorylation, autophosphorylation is stimulated by phospholipids, such as phosphatidylinositol-4,5-bisphosphate, overview | Mus musculus |
Purification (Comment) | Organism |
---|---|
GRK2 by gel filtration from Sf9 cells | Mus musculus |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + beta-adrenergic receptor | desensitization of the receptor by GRK4, GRK5, and GRK6 | Mus musculus | ADP + phosphorylated beta-adrenergic receptor | - |
? | |
ATP + G protein-coupled receptor | phosphorylation has a regulatory role | Mus musculus | ADP + phosphorylated G protein-coupled receptor | - |
? | |
ATP + G protein-coupled receptor | the GPCRs possess multiple phosphorylation sites for serine/threonine kinases | Mus musculus | ADP + phosphorylated G protein-coupled receptor | - |
? | |
additional information | G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview | Mus musculus | ? | - |
? | |
additional information | the GRKs are specific for GPCRs and arrestins, overview | Mus musculus | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
G protein-coupled receptor kinase 4 | - |
Mus musculus |
G protein-coupled receptor kinase 5 | - |
Mus musculus |
GRK4 | - |
Mus musculus |
GRK5 | - |
Mus musculus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Mus musculus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00004 | 0.00005 | inhibit GRK5 with an IC50 of 40-50 nM, inhibition mechanism via inducing inhibitory autophosphorylation and blocking of membrane association | Mus musculus | Ca2+/calmodulin |