G protein-coupled receptor kinase
| G protein-coupled receptor kinase | |||||||||
|---|---|---|---|---|---|---|---|---|---|
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| Identifiers | |||||||||
| EC number | 2.7.11.16 | ||||||||
| Databases | |||||||||
| IntEnz | IntEnz view | ||||||||
| BRENDA | BRENDA entry | ||||||||
| ExPASy | NiceZyme view | ||||||||
| KEGG | KEGG entry | ||||||||
| MetaCyc | metabolic pathway | ||||||||
| PRIAM | profile | ||||||||
| PDB structures | RCSB PDB PDBe PDBsum | ||||||||
| Gene Ontology | AmiGO / EGO | ||||||||
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G protein-coupled receptor kinases (GRKs, GPCRKs) are a family of protein kinases that regulate the activity of G protein-coupled receptors (GPCRs) by phosphorylating their intracellular domains after their associated G proteins have been released and activated.
The phosphorylated serine and threonine residues act as binding sites for arrestin proteins that prevent the reassociation of the G proteins with their receptors, thereby preventing reactivation of the signaling pathway.
GRKs regulate also cellular responses independent of their kinase activity. In particular, G protein-coupled receptor kinase 2 interacts with a diverse repertoire of non-GPCR substrates.[2]
GRK1 is involved with Rhodopsin phosphorlylation and deactivation. Defects in GRK1 result in Oguchi disease 2.[3]
Types of GRKs
| Name | Notes | Gene | OMIM |
| G protein-coupled receptor kinase 1 | Rhodopsin kinase | GRK1 | 180381 |
| G protein-coupled receptor kinase 2 | β-Adrenergic receptor kinase 1 (BARK1) | ADRBK1 (GRK2) | 109635 |
| G protein-coupled receptor kinase 3 | β-Adrenergic receptor kinase 2 (BARK2) | ADRBK2 (GRK3) | 109636 |
| G protein-coupled receptor kinase 4 | Has been associated with regulation of kidney tubule function | GRK4 | 137026 |
| G protein-coupled receptor kinase 5 | Knockout mice have altered core body temperature | GRK5 | 600870 |
| G protein-coupled receptor kinase 6 | Knockout mice are supersensitive to dopaminergics[4] | GRK6 | 600869 |
| G protein-coupled receptor kinase 7 | Cone opsin kinase | GRK7 | 606987 |
See also
References
Further reading
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