Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | phosphorylation activates the enzyme | Homo sapiens | |
additional information | GRK2 is activated by phosphorylation through kinases c-SRC, PKA and PKC, and it is activated by phospholipids | Mammalia |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
actin | - |
Homo sapiens | |
actinin | - |
Mammalia | |
alpha-actinin | - |
Homo sapiens | |
Ca2+/calmodulin | - |
Mammalia | |
Calmodulin | - |
Homo sapiens | |
caveolin | - |
Homo sapiens | |
caveolin | - |
Mammalia | |
Raf kinase inhibitor protein | RKIP | Mammalia | |
RKIP | - |
Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
80000 | - |
x * 80000, GRK2, SDS-PAGE | Homo sapiens |
80000 | - |
x * 80000, GRK2 catalytic domain, domain structure, overview | Mammalia |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview | ? | - |
? | |
additional information | Mammalia | G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP. Different mechanisms of signalling pathways modulation by GRK2, and regulation of GRK2, overview | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Mammalia | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | phosphorylation, e.g. by PKA, PKC, ERK1/2 or c-SRC, activates the enzyme | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
additional information | GRK2 and GRK3 are ubiquitously expressed in mammalian tissues | Mammalia | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + ezrin | GRK2 | Homo sapiens | ADP + phosphorylated ezrin | - |
? | |
ATP + phosducin | GRK2 | Homo sapiens | ADP + phosphorylated phosducin | - |
? | |
ATP + R-smad | GRK2 | Homo sapiens | ADP + phosphorylated R-smad | - |
? | |
ATP + ribosomal protein P2 | GRK2 | Homo sapiens | ADP + phosphorylated ribosomal protein P2 | - |
? | |
ATP + synuclein | GRK2 | Homo sapiens | ADP + phosphorylated synuclein | - |
? | |
ATP + tubulin | GRK2 | Homo sapiens | ADP + phosphorylated tubulin | - |
? | |
additional information | GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview | Homo sapiens | ? | - |
? | |
additional information | G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP. Different mechanisms of signalling pathways modulation by GRK2, and regulation of GRK2, overview | Mammalia | ? | - |
? | |
additional information | GRK2 can also phosphorylate non-receptor substrates such as phosducins, synucleins, tubulin, ribosomal protein P2, ezrin, and receptor regulated Smads. The RH domain of GRK2 specifically interacts with Galphaq family members, although it does not stimulate the GTPase activity of Galphaq as efficiently as other classical RGS proteins do, interaction with other oroteins, detailed overview | Mammalia | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
? | x * 80000, GRK2, SDS-PAGE | Homo sapiens |
? | x * 80000, GRK2 catalytic domain, domain structure, overview | Mammalia |
More | domain structure of GRK2, overview | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
G protein-coupled receptor kinase 2 | - |
Homo sapiens |
G protein-coupled receptor kinase 3 | - |
Homo sapiens |
GRK2 | - |
Mammalia |
GRK2 | - |
Homo sapiens |
GRK3 | - |
Homo sapiens |
More | the enzyme belongs to the beta-adrenergic receptor kinase subfamily | Homo sapiens |
More | the enzyme belongs to the beta-adrenergic receptor kinases subfamily | Mammalia |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |