Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | GRK3 bind the Gbetagamma subunit complex, a process that induces activation of the GRKs by phosphorylation | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
co-expression of rat thyrotropin receptor with GRK2 and GRK3 in HEK-293 cells, receptor phosphorylation occurs with both enzymes | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + beta-adrenergic receptor | Homo sapiens | in human heart failure, impaired beta-adrenergic receptor signaling compromises cardiac sensitivity to inotropic stimulation, overview | ADP + phosphorylated beta-adrenergic receptor | - |
? | |
additional information | Homo sapiens | GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling and desensitization, beta-arrestin-mediated receptor internalization, activity of GRKs and subcellular targeting is tightly regulated by interaction with receptor domains, G protein subunits, lipids, anchoring proteins and calcium-sensitive proteins, selective binding of activated Galphaq and Galpha-11 to RH domains of GRK2 and GRK3 selectively inhibits Gq signaling | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | GRKs are regulated by phopshorylation | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
heart | GRK3 expression is not increased in heart failure | Homo sapiens | - |
thyroid gland | increased expression of GRK3 in hyperfunctioning thyroid nodule | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + beta-adrenergic receptor | - |
Homo sapiens | ADP + phosphorylated beta-adrenergic receptor | - |
? | |
ATP + beta-adrenergic receptor | in human heart failure, impaired beta-adrenergic receptor signaling compromises cardiac sensitivity to inotropic stimulation, overview | Homo sapiens | ADP + phosphorylated beta-adrenergic receptor | - |
? | |
additional information | GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling and desensitization, beta-arrestin-mediated receptor internalization, activity of GRKs and subcellular targeting is tightly regulated by interaction with receptor domains, G protein subunits, lipids, anchoring proteins and calcium-sensitive proteins, selective binding of activated Galphaq and Galpha-11 to RH domains of GRK2 and GRK3 selectively inhibits Gq signaling | Homo sapiens | ? | - |
? | |
additional information | GRK2 interacts with a component of the MAPK pathway, as well as with the PI-3K substrate AKT, GRK2 and GRK3 bind the Gbetagamma subunit complex, a process that induces activation of the GRKs | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
G protein-coupled receptor kinase 2 | - |
Homo sapiens |
GRK2 | - |
Homo sapiens |
GRK3 | - |
Homo sapiens |
More | the enzyme belongs to the GRK2 subfamily, consisting of GRK2, beta-ARK1, GRK3, and beta-ARK2 | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |