Any feedback?
Please rate this page
(enzyme.php)
(0/150)

BRENDA support

BRENDA Home
show all | hide all No of entries

Information on EC 2.7.11.16 - G-protein-coupled receptor kinase and Organism(s) Homo sapiens and UniProt Accession P32298

for references in articles please use BRENDA:EC2.7.11.16
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
IUBMB Comments
Requires G-protein for activation and therefore belongs to the family of G-protein-dependent receptor kinases (GRKs). All members of this enzyme subfamily possess a highly conserved binding site for 1-phosphatidylinositol 4,5-bisphosphate. (cf. EC 2.7.11.14, rhodopsin kinase and EC 2.7.11.15, beta-adrenergic-receptor kinase).
Specify your search results
Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: P32298
Show additional data
Do not include text mining results
Include (text mining) results
Include results (AMENDA + additional results, but less precise)
Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
g-protein-coupled receptor kinase, g protein-coupled receptor kinase 5, g protein-coupled receptor kinase 4, g protein-coupled receptor kinase 6, grk4gamma, g-protein-coupled receptor kinase 5, g-protein-coupled receptor kinase 6, g-protein coupled receptor kinase 5, grk-6, g protein-coupled receptor kinase grk6, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
G protein-coupled receptor kinase 4
-
G protein-coupled receptor kinase 4gamma
-
G protein-coupled receptor kinase GRK4
-
GPCR kinase 4
-
GRK4gamma
-
G protein-coupled receptor kinase
-
-
G protein-coupled receptor kinase 2
-
-
G protein-coupled receptor kinase 4
-
-
G protein-coupled receptor kinase 5
G protein-coupled receptor kinase 6
G protein-coupled receptor kinase GRK5
-
G protein-coupled receptor kinase GRK6
-
G protein-coupled receptor kinase-6
-
-
G-protein coupled receptor kinase
-
-
G-protein-coupled receptor kinase 5
GPCR kinase
-
-
GPCR kinase 2
-
-
GRK-6
-
-
GRK3
-
-
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + [G protein-coupled receptor] = ADP + [G protein-coupled receptor]phosphate
show the reaction diagram
regulation mechanism
-
SYSTEMATIC NAME
IUBMB Comments
ATP:[G-protein-coupled receptor] phosphotransferase
Requires G-protein for activation and therefore belongs to the family of G-protein-dependent receptor kinases (GRKs). All members of this enzyme subfamily possess a highly conserved binding site for 1-phosphatidylinositol 4,5-bisphosphate. (cf. EC 2.7.11.14, rhodopsin kinase and EC 2.7.11.15, beta-adrenergic-receptor kinase).
CAS REGISTRY NUMBER
COMMENTARY hide
127407-08-3
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + activated form of G protein-coupled receptors
ADP + phosphorylated G protein-coupled receptors
show the reaction diagram
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
reaction only with GRK4alpha isoform, no reaction with GRK4beta, GRK4gamma, GRK4delta
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
show the reaction diagram
-
-
-
?
ATP + a G protein-coupled receptor
ADP + a phosphorylated G protein-coupled receptor
show the reaction diagram
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
show the reaction diagram
ATP + ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
show the reaction diagram
-
-
-
-
?
ATP + beta 2-adrenergic receptor
ADP + phosphorylated beta 2-adrenergic receptor
show the reaction diagram
-
-
-
?
ATP + BLT1 receptor
ADP + phosphorylated BLT1 receptor
show the reaction diagram
ATP + CXCR4 receptor
ADP + phosphorylated CXCR4 receptor
show the reaction diagram
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
show the reaction diagram
-
GRK4
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
show the reaction diagram
ATP + G-protein-coupled receptor
ADP + phosphorylated G-protein-coupled receptor
show the reaction diagram
ATP + histone deacetylase 6
ADP + phosphorylated histone deacetylase 6
show the reaction diagram
the enzyme phosphorylates histone deacetylase 6 at Ser21 to promote its deacetylase activity
-
-
?
ATP + moesin
ADP + phosphorylated moesin
show the reaction diagram
phosphorylation at Thr66
-
-
?
ATP + porcine brain tubulin
ADP + phosphorylated porcine brain tubulin
show the reaction diagram
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
ATP + rhodopsin
ADP + rhodopsin phosphate
show the reaction diagram
cf. EC 2.7.11.14, rhodopsin is also a substrate of GRK5
-
-
?
ATP + [alpha-synuclein]
ADP + [alpha-synuclein]phosphate
show the reaction diagram
the enzyme phosphorylates alpha-synuclein at Ser129
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
show the reaction diagram
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor]phosphate
show the reaction diagram
-
GRK4-6
-
-
?
ATP + [dopamine D1 receptor]
ADP + [dopamine D1 receptor]phosphate
show the reaction diagram
ATP + [follicle-stimulating hormone receptor]
ADP + [follicle-stimulating hormone receptor]phosphate
show the reaction diagram
-
GRK4-6
-
-
?
ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
show the reaction diagram
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
show the reaction diagram
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
show the reaction diagram
ATP + [luteinizing hormone/chorionic gonadotropin receptor]
ADP + [luteinizing hormone/chorionic gonadotropin receptor]phosphate
show the reaction diagram
-
GRK4-6
-
-
?
ATP + [M2 muscarinic receptor]
ADP + [M2 muscarinic receptor]phosphate
show the reaction diagram
-
GRK4-6
-
-
?
ATP + [M3 muscarinic acetylcholine receptor]
ADP + phospho-[M3 muscarinic acetylcholine receptor]
show the reaction diagram
ATP + [rhodopsin]
ADP + [rhodopsin]phosphate
show the reaction diagram
-
GRK4-6
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
show the reaction diagram
nucleophosmin 1 + ATP
phosphorylated nucleophosmin 1 + ADP
show the reaction diagram
-
-
-
-
?
p53 + ATP
phosphorylated-p53 + ADP
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
show the reaction diagram
-
-
-
?
ATP + a G protein-coupled receptor
ADP + a phosphorylated G protein-coupled receptor
show the reaction diagram
-
the GRKs are important in the cardiovascular system, the major G protein-coupled receptor regulatory pathway involves phosphorylation of activated receptors by GRKs, followed by binding of arrestin proteins, which prevent receptors from activating downstream heterotrimeric G protein pathways while allowing activation of arrestin-dependent signaling pathways, general mechanisms of GRK-arrestin regulation, overview, physiological functions and potential pathophysiological roles of GRKs and arrestins in human disorders, overview
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
show the reaction diagram
-
GRK5 phosphorylates Ser-129 of alpha-synuclein at the plasma membrane and induces translocation of phosphorylated alpha-synuclein to the perikaryal area, GRK5 promotes alpha-linolenic acid-induced oligomerization of alpha-synuclein, alpha-synuclein phosphorylation by GRK5 plays a crucial role in the pathogenesis of sporadic Parkinson's disease, sPD
-
-
?
ATP + ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
show the reaction diagram
-
-
-
-
?
ATP + BLT1 receptor
ADP + phosphorylated BLT1 receptor
show the reaction diagram
-
GRK6, ablation of GRK6 leads to augmented signaling by leukotriene B4 acting through the BLT1 receptor
-
-
?
ATP + CXCR4 receptor
ADP + phosphorylated CXCR4 receptor
show the reaction diagram
-
GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
show the reaction diagram
-
GRK4
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
show the reaction diagram
-
regulation mechanism of GRK5, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview
-
-
?
ATP + G-protein-coupled receptor
ADP + phosphorylated G-protein-coupled receptor
show the reaction diagram
-
leading to receptor endocytosis
-
-
?
ATP + moesin
ADP + phosphorylated moesin
show the reaction diagram
phosphorylation at Thr66
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
-
-
-
-
?
ATP + [alpha-synuclein]
ADP + [alpha-synuclein]phosphate
show the reaction diagram
the enzyme phosphorylates alpha-synuclein at Ser129
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
show the reaction diagram
GRK5 plays a distinctive role in the phosphorylation of the beta2AR
-
-
?
ATP + [dopamine D1 receptor]
ADP + [dopamine D1 receptor]phosphate
show the reaction diagram
-
GRK4 constitutively phosphorylates active and inactive receptor, in the latter case diminishing stimulation of the receptor by dopamine, phosphorylation reduces receptor desensitization and internalization, followed by reduced cAMP accumulation
-
-
?
ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
show the reaction diagram
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
show the reaction diagram
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
show the reaction diagram
ATP + [M3 muscarinic acetylcholine receptor]
ADP + phospho-[M3 muscarinic acetylcholine receptor]
show the reaction diagram
-
GRK6 plays a major role in specific M3 muscarinic acetylcholine receptor regulation
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
show the reaction diagram
-
GRK4-6, receptor activation
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
-
inhibits GRK5
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Calmodulin
reaction of isoenzyme GRK4alpha with rhodopsin, IC50: 80 nM
actin
-
-
actinin
-
inhibits GRK5
-
alpha-actinin
-
-
Calmodulin
caveolin
-
CCG-215022
-
CCG-265328
-
GSK1326255A
-
-
GSK1713088A
-
-
GSK2163632A
-
-
RKIP
-
-
RNA aptamer C13
development and synthesis of a highly specific RNA aptamer C13 that potently inhibits GRK2, EC 2.7.11.15, and GRK5, inhibitor secondary structure, overview
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
isoproterenol
stimulates the phosphorylation activity of GRK5 by10-15fold at 0.001 mM
methacholine
-
stimulation of M3 muscarinic acetylcholine receptor phosphorylation is reversible by atropine
phosphatidylinositol 4,5-bisphosphate
-
activates the receptor phosphorylation activity of GRK5, but not its autophosphorylation or peptide phosphorylation activity
Phospholipids
-
activate GRK5
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.014 - 0.02
ATP
0.0012 - 0.0018
rhodopsin
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4.1 - 8.7
ATP
2.9 - 6.5
rhodopsin
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00008
Calmodulin
Homo sapiens
reaction of isoenzyme GRK4alpha with rhodopsin, IC50: 80 nM
0.0011
CCG-265328
Homo sapiens
at pH 7.5, and temperature not specified in the publication
0.0025
GSK1326255A
Homo sapiens
at pH 7.5, and temperature not specified in the publication
-
0.0032
GSK1713088A, GSK2163632A
Homo sapiens
at pH 7.5, and temperature not specified in the publication
-
0.000079
RNA aptamer C13
Homo sapiens
inhibition of GRK5
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
8
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
assay at room temperature
37
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
spermatogonia cell line GC-1 spg
Manually annotated by BRENDA team
GRK4gamma is the only detectable isoform in human sperm
Manually annotated by BRENDA team
-
GRK4 predominantly
Manually annotated by BRENDA team
-
neuroblastoma cell line, contains no GRK5
Manually annotated by BRENDA team
-
increased expression of GRK4 in hyperfunctioning thyroid nodule
Manually annotated by BRENDA team
-
prepared without lymphocytic infiltrations in the tumor, GRKs expression patterns, moderate expression level of GRK4
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
association of GRK6 with the cell membrane is mediated in part by the palmitoylation of cysteine residues that lie in a C-terminal region
-
Manually annotated by BRENDA team
-
GRK5 co-localizes with gamma-tubulin, centrin, and pericentrin in centrosomes. The centrosomal localization of GRK5 is observed predominantly at interphase and although its localization is not dependent on microtubules, it can mediate microtubule nucleation of centrosome
Manually annotated by BRENDA team
additional information
-
GRK4, GRK5, and GRK6 lack the G protein betagamma-subunit binding domain but use direct PIP2 binding and/or covalent lipid modification with palmitate to reside primarily at the plasma membrane
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
GRK4_HUMAN
578
0
66583
Swiss-Prot
other Location (Reliability: 2)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
66050
-
2 * 66050, recombinant acetylated, full-length, palmitoylation-deficient GRK6, mass spectrometry
69000
-
x * 69000, GRK5, SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
-
2 * 66050, recombinant acetylated, full-length, palmitoylation-deficient GRK6, mass spectrometry
monomer
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
lipoprotein
nitrosylation
S-nitrosylation of isoform GRK6 by nitric oxide enhances the kinase activity towards the phosphorylation of alpha-synuclein
phosphoprotein
additional information
-
mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquitination or protease cleavage, overview
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
mutant enzyme A486V crystallized in the presence of 5'-adenylyl beta,gamma-imidodiphosphate, sitting drop vapor diffusion method, at 4°C in 0.1 M sodium citrate, pH 5.0-6.5, 15-27.5% (w/v) polyethylene glycol 3350
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A142V
the mutation is associated with hypertension
A486V
the mutation is associated with hypertension. There is an increased rate of autophosphorylation of a number of residues in the mutant relative to the wild type enzyme
K216M/K217M
a kinase-dead GRK4gamma mutant, that interacts with GalphaS and Galpha13 in the same way as the wild-type GRK4gamma
R65L
the mutation is associated with hypertension
A142V
A486V
-
naturally occuring functional polymorphism, the mutation leads to increased GRK4 activity and phosphorylation of dopamine receptors, phenotype
C561S/C562S/C565S
-
site-directed mutagenesis, mutation of palmitoylation sites, the mutant protein retains its ability to phosphorylate rhodopsin, albeit with a 5fold higher Km and 2fold lower Vmax compared with those of wild-type GRK6
F527D
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
G298S
the complete loss-of-function variant is identified in heterotaxy patients
I165E
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I165E/F527D
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I39E
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I39E/I165E
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
K215R
K216M/K217M
-
site-directed mutagenesis, kinase-dead GRK4 mutant, overexpression in HEK-293 cells leads to partially desensitization of GPCR
K220R
-
kinase-dead mutant
Q41L
the variant is identified in heterotaxy patients
R304C
the variant is identified in heterotaxy patients
R65L/A142V/A486V
-
co-expression in CHO cells with the dopamine D1 receptor causes enhanced desensitization and agonist-independent phosphorylation of the receptor
S500A
the mutant shows decreased activity compared to the wild type enzyme
T10A
the mutant shows increased activity compared to the wild type enzyme
T425M
the variant is identified in heterotaxy patients
additional information
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
HisTrap column chromatography, HiTrap SP column chromatography, HiTrap heparin column chromatography and Superdex 75 gel filtration
HiTrap S column chromatography and HiTrap Q column chromatography
Ni-NTA column chromatography
partial purification of GRK5 from HEK-293 cell membranes, separation from GRK2 and GRK6, overview
recombinant GST-tagged GRK5 from insect Sf9 cells by ion exchange and heparin affinity chromatography
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in Sf21 insect cells
expression of GRK4gamma in 293T cells, which are devoid of endogenous GRK4gamma
co-expression of isozyme GRK4gamma and dopamine D1 receptor in HEK-293 cells leads to phosphorylation of the receptor by GRK4, this effect is not seen with isozyme GRK4beta and GRK4delta
-
co-expression of rat thyrotropin receptor with GRK4, GRK5, and GRK6 in HEK-293 cells, receptor phosphorylation occurs with GRK5 and GRK6
-
expressed in BAEC cells and HEK-293 cells
-
expressed in Escherichia coli BL21 Rosetta cells
expressed in HEK293 cells and fertilized eggs from Danio rerio
expressed in High-5 cells
expressed in Mus musculus and HEK-293T cells
expression of GRK6 in both Spodoptera frugiperda Sf9 and Trichoplusia ni High5 insect cells as a soluble, palmitoylation-deficient mutant in which three potential palmitoylation sites, located at Cys561, Cys562, and Cys565, are converted to Ser
-
expression of GST-tagged GRK5 in Spodoptera frugiperda Sf9 cells using the baculovirus transfection method
expression of kinase-dead GRK4 mutant in HEK-293 cells
-
gene GRK5, co-expression with human alpha-synuclein in HEK-293 cells and co-localization in the plasma membrane, functional co-expression of GRK5 and alpha-synuclein in primary cortical neurons from the cerebral cortex of fetal mice
-
GRK4, DNA and amino acid sequence determination of polymorphisms, genotyping of American twins
-
GRK4, DNA and amino acid sequence determination of polymorphisms, genotyping of Han Chinese individuals
-
stable overexpression of wild-type and K215R mutant GRK6 in SH-SY5Y neuroblastoma cells via adenovirus infection system
-
transient overexpression of wild-types and dominant negative mutants of GRK5 and GRK6 in NG108-15 mouse neuroblastoma x rat glioma hybrid cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
isoform GRK6 is significantly downregulated in lung adenocarcinoma tissues. Inhibition of CCAAT/enhancer-binding protein-alpha significantly inhibits isoform GRK6 expression
treatment with 5-aza-2'-deoxycytidine significantly enhances isoform GRK6 gene expression. Overexpression of C/EBPalpha significantly promotes isoform GRK6 expression
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
diagnostics
-
GRK5 levels in heart and peripheral lymphocytes correlate well, therefore the lymphocytic enzyme level might be a very suitable marker for determining the sympathetic drive to heart failure during clinical course and treatment of human congestive heart failure patients
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Sallese, M.; Mariggio, S.; Collodel, G.; Moretti, E.; Piomboni, P.; Baccetti, B.; De Blasi, A.
G protein-coupled receptor kinase GRK4. Molecular analysis of the four isoforms and ultrastructural localization in spermatozoa and germinal cells
J. Biol. Chem.
272
10188-10195
1997
Homo sapiens (P32298), Homo sapiens
Manually annotated by BRENDA team
Sallese, M.; Lombardi, M.S.; De Blasi, A.
Two isoforms of G protein-coupled receptor kinase 4 identified by molecular cloning
Biochem. Biophys. Res. Commun.
199
848-854
1994
Homo sapiens (P32298)
Manually annotated by BRENDA team
Ambrose, C.; James, M.; Barnes, G.; Lin, C.; Bates, G.; Altherr, M.; Duyao, M.; Groot, N.; Church, D.; Wasmuth, J.J.; et al.
A novel G protein-coupled receptor kinase gene cloned from 4p16.3
Hum. Mol. Genet.
1
697-703
1992
Homo sapiens (P32298)
Manually annotated by BRENDA team
Kunapuli, P.; Benovic, J.L.
Cloning and expression of GRK5: a member of the G protein-coupled receptor kinase family
Proc. Natl. Acad. Sci. USA
90
5588-5592
1993
Homo sapiens (P34947)
Manually annotated by BRENDA team
Stoffel, R.H.; Randall, R.R.; Premont, R.T.; Lefkowitz, R.J.; Inglese, J.
Palmitoylation of G protein-coupled receptor kinase, GRK6. Lipid modification diversity in the GRK family
J. Biol. Chem.
269
27791-27794
1994
Homo sapiens (P43250)
Manually annotated by BRENDA team
Benovic, J.L.; Gomez, J.
Molecular cloning and expression of GRK6. A new member of the G protein-coupled receptor kinase family
J. Biol. Chem.
268
19521-19527
1993
Homo sapiens (P43250)
Manually annotated by BRENDA team
Ghadessy, R.S.; Willets, J.M.; Kelly, E.
G protein-coupled receptor kinase 6 (GRK6) selectively regulates endogenous secretin receptor responsiveness in NG108-15 cells
Br. J. Pharmacol.
138
660-670
2003
Homo sapiens
Manually annotated by BRENDA team
Penela, P.; Ribas, C.; Mayor, F.
Mechanisms of regulation of the expression and function of G protein-coupled receptor kinases
Cell. Signal.
15
973-981
2003
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Oyama, N.; Urasawa, K.; Kaneta, S.; Sakai, H.; Saito, T.; Takagi, C.; Yoshida, I.; Kitabatake, A.; Tsutsui, H.
Chronic beta-adrenergic receptor stimulation enhances the expression of G-protein coupled receptor kinases, GRK2 and GRK5, in both the heart and peripheral lymphocytes
Circ. J.
69
987-990
2005
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Voigt, C.; Holzapfel, H.P.; Paschke, R.
Decreased expression of G-protein coupled receptor kinase 2 in cold thyroid nodules
Exp. Clin. Endocrinol. Diabetes
113
102-106
2005
Homo sapiens
Manually annotated by BRENDA team
Picascia, A.; Capobianco, L.; Iacovelli, L.; De Blasi, A.
Analysis of differential modulatory activities of GRK2 and GRK4 on Galphaq-coupled receptor signaling
Methods Enzymol.
390
337-353
2004
Homo sapiens
Manually annotated by BRENDA team
Willets, J.M.; Mistry, R.; Nahorski, S.R.; Challiss, R.A.
Specificity of G protein-coupled receptor kinase 6-mediated phosphorylation and regulation of single-cell M3 muscarinic acetylcholine receptor signaling
Mol. Pharmacol.
64
1059-1068
2003
Homo sapiens
Manually annotated by BRENDA team
Neve, K.A.
Novel features of G protein-coupled receptor kinase 4
Mol. Pharmacol.
69
673-676
2006
Homo sapiens
Manually annotated by BRENDA team
Zhu, H.; Lu, Y.; Wang, X.; Treiber, F.A.; Harshfield, G.A.; Snieder, H.; Dong, Y.
The G protein-coupled receptor kinase 4 gene affects blood pressure in young normotensive twins
Am. J. Hypertens.
19
61-66
2006
Homo sapiens
Manually annotated by BRENDA team
Wang, Y.; Li, B.; Zhao, W.; Liu, P.; Zhao, Q.; Chen, S.; Li, H.; Gu, D.
Association study of G protein-coupled receptor kinase 4 gene variants with essential hypertension in northern Han Chinese
Ann. Hum. Genet.
70
778-783
2006
Homo sapiens
Manually annotated by BRENDA team
Premont, R.T.; Gainetdinov, R.R.
Physiological roles of G protein-coupled receptor kinases and arrestins
Annu. Rev. Physiol.
69
511-534
2007
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Ribas, C.; Penela, P.; Murga, C.; Salcedo, A.; Garcia-Hoz, C.; Jurado-Pueyo, M.; Aymerich, I.; Mayor, F.
The G protein-coupled receptor kinase (GRK) interactome: Role of GRKs in GPCR regulation and signaling
Biochim. Biophys. Acta
1768
913-922
2007
Homo sapiens, Mammalia
Manually annotated by BRENDA team
Lodowski, D.T.; Tesmer, V.M.; Benovic, J.L.; Tesmer, J.J.
The structure of G protein-coupled receptor kinase (GRK)-6 defines a second lineage of GRKs
J. Biol. Chem.
281
16785-16793
2006
Homo sapiens
Manually annotated by BRENDA team
rawaka, S.; Wada, M.; Goto, S.; Karube, H.; Sakamoto, M.; Ren, C.H.; Koyama, S.; Nagasawa, H.; Kimura, H.; Kawanami, T.; Kurita, K.; Tajima, K.; Daimon, M.; Baba, M.; Kido, T.; Saino, S.; Goto, K.; Asao, H.; Kitanaka, C.; Takashita, E.; Hongo, S.; Nakamura, T.; Kayama, T.; Suzuki, Y.; Kobayashi, K.; Kat, K.a.t.a.
The role of G-protein-coupled receptor kinase 5 in pathogenesis of sporadic Parkinsons disease
J. Neurosci.
26
9227-9238
2006
Homo sapiens
Manually annotated by BRENDA team
Yang, W.; Xia, S.
Mechanisms of regulation and function of G-protein-coupled receptor kinases
World J. Gastroenterol.
12
7753-7757
2006
Homo sapiens
Manually annotated by BRENDA team
Keever, L.B.; Jones, J.E.; Andresen, B.T.
G protein-coupled receptor kinase 4gamma interacts with inactive GalphaS and Galpha13
Biochem. Biophys. Res. Commun.
367
649-655
2008
Homo sapiens (P32298)
Manually annotated by BRENDA team
Tran, T.M.; Jorgensen, R.; Clark, R.B.
Phosphorylation of the beta2-adrenergic receptor in plasma membranes by intrinsic GRK5
Biochemistry
46
14438-14449
2007
Homo sapiens (P34947)
Manually annotated by BRENDA team
Mayer, G.; Wulffen, B.; Huber, C.; Brockmann, J.; Flicke, B.; Neumann, L.; Hafenbradl, D.; Klebl, B.M.; Lohse, M.J.; Krasel, C.; Blind, M.
An RNA molecule that specifically inhibits G-protein-coupled receptor kinase 2 in vitro
RNA
14
524-534
2008
Homo sapiens (P34947)
Manually annotated by BRENDA team
Wang, L.; Gesty-Palmer, D.; Fields, T.A.; Spurney, R.F.
Inhibition of WNT signaling by G protein-coupled receptor (GPCR) kinase 2 (GRK2)
Mol. Endocrinol.
23
1455-1465
2009
Homo sapiens
Manually annotated by BRENDA team
Sorriento, D.; Ciccarelli, M.; Santulli, G.; Campanile, A.; Altobelli, G.G.; Cimini, V.; Galasso, G.; Astone, D.; Piscione, F.; Pastore, L.; Trimarco, B.; Iaccarino, G.
The G-protein-coupled receptor kinase 5 inhibits NFkappaB transcriptional activity by inducing nuclear accumulation of IkappaB alpha
Proc. Natl. Acad. Sci. USA
105
17818-17823
2008
Homo sapiens
Manually annotated by BRENDA team
Chen, X.; Zhu, H.; Yuan, M.; Fu, J.; Zhou, Y.; Ma, L.
G-protein-coupled receptor kinase 5 phosphorylates p53 and inhibits DNA damage-induced apoptosis
J. Biol. Chem.
285
12823-12830
2010
Homo sapiens
Manually annotated by BRENDA team
So, C.H.; Michal, A.M.; Mashayekhi, R.; Benovic, J.L.
G protein-coupled receptor kinase 5 phosphorylates nucleophosmin and regulates cell sensitivity to polo-like kinase 1 inhibition
J. Biol. Chem.
287
17088-17099
2012
Homo sapiens
Manually annotated by BRENDA team
Michal, A.M.; So, C.H.; Beeharry, N.; Shankar, H.; Mashayekhi, R.; Yen, T.J.; Benovic, J.L.
G Protein-coupled receptor kinase 5 is localized to centrosomes and regulates cell cycle progression
J. Biol. Chem.
287
6928-6940
2012
Homo sapiens
Manually annotated by BRENDA team
Kim, J.I.; Chakraborty, P.; Wang, Z.; Daaka, Y.
G-protein coupled receptor kinase 5 regulates prostate tumor growth
J. Urol.
187
322-329
2012
Homo sapiens
Manually annotated by BRENDA team
Guo, Q.; Subramanian, H.; Gupta, K.; Ali, H.
Regulation of C3a receptor signaling in human mast cells by G protein coupled receptor kinases
PLoS ONE
6
e22559
2011
Homo sapiens
Manually annotated by BRENDA team
Chakraborty, P.K.; Zhang, Y.; Coomes, A.S.; Kim, W.J.; Stupay, R.; Lynch, L.D.; Atkinson, T.; Kim, J.I.; Nie, Z.; Daaka, Y.
G protein-coupled receptor kinase GRK5 phosphorylates moesin and regulates metastasis in prostate cancer
Cancer Res.
74
3489-3500
2014
Homo sapiens (P34947), Homo sapiens
Manually annotated by BRENDA team
Li, L.; Homan, K.T.; Vishnivetskiy, S.A.; Manglik, A.; Tesmer, J.J.; Gurevich, V.V.; Gurevich, E.V.
G protein-coupled receptor kinases of the GRK4 protein subfamily phosphorylate inactive G protein-coupled receptors (GPCRs)
J. Biol. Chem.
290
10775-10790
2015
Homo sapiens (P34947)
Manually annotated by BRENDA team
Allen, S.J.; Parthasarathy, G.; Darke, P.L.; Diehl, R.E.; Ford, R.E.; Hall, D.L.; Johnson, S.A.; Reid, J.C.; Rickert, K.W.; Shipman, J.M.; Soisson, S.M.; Zuck, P.; Munshi, S.K.; Lumb, K.J.
Structure and function of the hypertension variant A486V of G protein-coupled receptor kinase 4
J. Biol. Chem.
290
20360-20373
2015
Homo sapiens (P32298), Homo sapiens
Manually annotated by BRENDA team
Johnson, L.R.; Robinson, J.D.; Lester, K.N.; Pitcher, J.A.
Distinct structural features of G protein-coupled receptor kinase 5 (GRK5) regulate its nuclear localization and DNA-binding ability
PLoS ONE
8
e62508
2013
Homo sapiens (P34947)
Manually annotated by BRENDA team
Rowlands, R.A.; Cato, M.C.; Waldschmidt, H.V.; Bouley, R.A.; Chen, Q.; Avramova, L.; Larsen, S.D.; Tesmer, J.J.G.; White, A.D.
Structure-based design of selective, covalent G protein-coupled receptor kinase 5 inhibitors
ACS Med. Chem. Lett.
10
1628-1634
2019
Homo sapiens (P34947)
Manually annotated by BRENDA team
Yao, S.; Wu, D.; Chen, J.; Wang, P.; Lv, X.; Huang, J.
Hypermethylation of the G protein-coupled receptor kinase 6 (GRK6) promoter inhibits binding of C/EBPalpha, and GRK6 knockdown promotes cell migration and invasion in lung adenocarcinoma cells
FEBS Open Bio
9
605-617
2019
Homo sapiens (P43250)
Manually annotated by BRENDA team
Lagman, J.; Sayegh, P.; Lee, C.S.; Sulon, S.M.; Jacinto, A.Z.; Sok, V.; Peng, N.; Alp, D.; Benovic, J.L.; So, C.H.
G protein-coupled receptor kinase 5 modifies cancer cell resistance to paclitaxel
Mol. Cell. Biochem.
461
103-118
2019
Homo sapiens (P34947)
Manually annotated by BRENDA team
Wu, W.; Sung, C.C.; Yu, P.; Li, J.; Chung, K.K.K.
S-nitrosylation of G protein-coupled receptor kinase 6 and casein kinase 2 alpha modulates their kinase activity toward alpha-synuclein phosphorylation in an animal model of Parkinsons disease
PLoS ONE
15
e0232019
2020
Homo sapiens (P43250)
Manually annotated by BRENDA team
Beyett, T.; Chen, Q.; Labudde, E.; Krampen, J.; Sharma, P.; Tesmer, J.
Characterization of a hyperphosphorylated variant of G protein-coupled receptor kinase 5 expressed in E. coli
Protein Expr. Purif.
168
105547
2020
Homo sapiens (P34947), Homo sapiens
Manually annotated by BRENDA team
Lessel, D.; Muhammad, T.; Casar Tena, T.; Moepps, B.; Burkhalter, M.D.; Hitz, M.P.; Toka, O.; Rentzsch, A.; Schubert, S.; Schalinski, A.; Bauer, U.M.; Kubisch, C.; Ware, S.M.; Philipp, M.
The analysis of heterotaxy patients reveals new loss-of-function variants of GRK5
Sci. Rep.
6
33231
2016
Homo sapiens (P34947), Homo sapiens
Manually annotated by BRENDA team