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Details on Person UniProt:P25098 GRK2

Class:IdReferenceGeneProduct:50271
_chainChangeLogchain:1-689 added on Fri February 6 2015
_displayNameUniProt:P25098 GRK2
_timestamp2026-02-20 21:46:52
chainchain:1-689
checksum4DB68F62841AFA7D
commentFUNCTION Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them (PubMed:19715378). Phosphorylates catecholamine-activated ADRB2 to regulate physiological cardiomyocyte contraction rate responses (By similarity). Also phosphorylates ligand-bound C3a and C5a anaphylatoxin receptors (C3AR1 and C5AR1, respectively), leading to receptor desensitization (PubMed:21799898, PubMed:23077507). Key regulator of LPAR1 signaling (PubMed:19306925). Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor (PubMed:19306925). Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner (PubMed:19306925). Positively regulates ciliary smoothened (SMO)-dependent Hedgehog (Hh) signaling pathway by facilitating the trafficking of SMO into the cilium and the stimulation of SMO activity (By similarity). Inhibits relaxation of airway smooth muscle in response to blue light (PubMed:30284927).CATALYTIC ACTIVITY [beta-adrenergic receptor] + ATP = [beta-adrenergic receptor]-phosphate + ADP + H(+)ACTIVITY REGULATION In contrast to other AGC family kinases, the catalytic activity is solely regulated by the binding of substrates and ligands, not by phosphorylation of the kinase domain.SUBUNIT Interacts with the heterodimer formed by GNB1 and GNG2 (By similarity). Interacts with GIT1 (By similarity). Interacts with, and phosphorylates chemokine-stimulated CCR5 (PubMed:10085131). Interacts with ARRB1 (PubMed:9501202). Interacts with LPAR1 and LPAR2 (PubMed:19306925). Interacts with RALA in response to LPAR1 activation (PubMed:19306925). ADRBK1 and RALA mutually inhibit each other's binding to LPAR1 (PubMed:19306925). Interacts with ADRB2 (PubMed:19715378).INTERACTION Expressed in peripheral blood leukocytes.DOMAIN The PH domain binds anionic phospholipids and helps recruiting ADRBK1 from the cytoplasm to plasma membrane close to activated receptors. It mediates binding to G protein beta and gamma subunits, competing with G-alpha subunits and other G-betagamma effectors.SIMILARITY Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily.ONLINE INFORMATION Beta adrenergic receptor kinase entry
descriptionrecommendedName: Beta-adrenergic receptor kinase 1 shortName: Beta-ARK-1 ecNumber evidence="12"2.7.11.15 alternativeName: fullName evidence="18"G-protein coupled receptor kinase 2
geneNameGRK2
ADRBK1
BARK
BARK1
identifierP25098
isSequenceChangedFALSE
keyword3D-structure
ATP-binding
Cell membrane
Cell projection
Cytoplasm
Kinase
Membrane
Nucleotide-binding
Phosphoprotein
Proteomics identification
Reference proteome
Serine/threonine-protein kinase
Synapse
Transferase
modified[InstanceEdit:9836292] Weiser, Joel, 2023-05-25
[InstanceEdit:9852000] Weiser, Joel, 2023-11-03
[InstanceEdit:9926675] Weiser, Joel, 2024-11-03
[InstanceEdit:9983091] Weiser, Joel, 2026-02-20
nameGRK2
referenceDatabase[ReferenceDatabase:2] UniProt
referenceGene[ReferenceDNASequence:8998168] ENSEMBL:ENSG00000173020 GRK2 [Homo sapiens]
secondaryIdentifierARBK1_HUMAN
B0ZBE1
Q13837
Q6GTT3
sequenceLength689
species[Species:48887] Homo sapiens
(referenceEntity)[EntityWithAccessionedSequence:50270] GRK2 [plasma membrane] [Homo sapiens]
[EntityWithAccessionedSequence:111969] p-S29-ADRBK1 [plasma membrane] [Homo sapiens]
[EntityWithAccessionedSequence:5632504] ADRBK1 [cilium] [Homo sapiens]
[EntityWithAccessionedSequence:9645318] p-S29-ADRBK1 [cytosol] [Homo sapiens]
(referenceSequence)[ModifiedResidue:111968] O-phospho-L-serine at 29
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No pathways have been reviewed or authored by UniProt:P25098 GRK2 (50271)