| Gene Symbol |
GRK5
|
| Entrez Gene |
2869
|
| Alt Symbol |
GPRK5
|
| Species |
Human
|
| Gene Type |
protein-coding
|
| Description |
G protein-coupled receptor kinase 5
|
| Other Description |
FP2025|g protein-coupled receptor kinase GRK5
|
| Swissprots |
Q5T059 D3DRD0 P34947
|
| Accessions |
CBX53840 EAW49393 EAW49394 EAW49395 P34947 AF370369 AAQ15205 AK097099 AK298261 BAG60525 AK301450 BAG62974 AK309761 AK313012 BAG35847 BC018116 BC064506 AAH64506 BC114448 AAI14449 BQ184611 CN290123 L15388 AAA58620 XM_005269707 XP_005269764 XM_005269708 XP_005269765 XM_011539699 XP_011538001 NM_005308 NP_005299
|
| Function |
Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein- coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70- interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2- mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of
|
| Subcellular Location |
Cytoplasm. Nucleus. Cell membrane; Peripheral membrane protein. Note=Predominantly localized at the plasma membrane; targeted to the cell surface through the interaction with phospholipids. Nucleus localization is regulated in a GPCR and Ca(2+)/calmodulin-dependent fashion.
|
| Tissue Specificity |
Highest levels in heart, placenta, lung > skeletal muscle > brain, liver, pancreas > kidney. {ECO:0000269|PubMed:7685906}.
|
| Top Pathways |
Endocytosis, Chemokine signaling pathway, Morphine addiction
|