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Information on EC 2.7.11.16 - G-protein-coupled receptor kinase and Organism(s) Rattus norvegicus and UniProt Accession P97711

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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).
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Rattus norvegicus
UNIPROT: P97711
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The taxonomic range for the selected organisms is: Rattus norvegicus
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, grk-6, g-protein coupled receptor kinase 5, g protein-coupled receptor kinase grk6, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
G protein-coupled receptor kinase GRK6
-
by G protein-coupled receptor kinase 6
-
-
G protein-coupled receptor kinase 4
-
-
G protein-coupled receptor kinase 5
G protein-coupled receptor kinase 6
-
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G protein-coupled receptor kinase GRK5
-
additional information
-
the enzyme belongs to the GRK4-6 family
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 + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
show the reaction diagram
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
-
urea treated outer segments of rhodopsin
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
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 + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
show the reaction diagram
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
show the reaction diagram
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
amlexanox
selective inhibitor
heparin
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
30
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
predominantly expressed in
Manually annotated by BRENDA team
-
enriched in GRK2 and GRK5
Manually annotated by BRENDA team
-
intestinal epithelial cell line
Manually annotated by BRENDA team
-
peripheral
Manually annotated by BRENDA team
-
primary cells
Manually annotated by BRENDA team
-
parvalbumin-positive interneurons express more of GRK2 and less of arrestin-2 than medium spiny
Manually annotated by BRENDA team
additional information
-
analysis of GRK5 expression rate and mRNA level in heart and lymphocytes by RT-PCR
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
the GRK5 subcellular distribution in the human striatal neurons is altered by its phosphorylation: unphosphorylated enzyme preferentially localizes to synaptic membranes
Manually annotated by BRENDA team
-
the GRK5 subcellular distribution in the human striatal neurons is altered by its phosphorylation: phosphorylated GRK5 is found in plasma membrane and cytosolic fractions
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
GRK6_RAT
576
0
65963
Swiss-Prot
other Location (Reliability: 2)
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
-
the GRK5 subcellular distribution in the human striatal neurons is altered by its phosphorylation
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K215R
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inactive dominant negative mutants of GRK5 or GRK6, overexpression of the GRK5 mutant in myometrial cells does not influence beta-adrenergic receptor sensitivity, while overexpression of GRK6 mutant leads to a 70% increase in isoproterenol-stimulated beta-adrenergic signaling via the beta-adrenergic receptor
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
transient overexpression of wild-types and dominant negative mutants of GRK5 and GRK6 in COS-7 cells
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
CP55940 exposure selectively up-regulates GRK5 proteins in rat prefrontal cortex. Sustained activation of CB2 receptors enhances enzyme expression
enzyme expression is significantly up-regulated in the hippocampal CA1, DG, and H areas at 7 days and 14 days after status epilepticus
parvalbumin-positive interneurons express more of GRK2 and less of arrestin-2 than medium spiny neurons
-
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Fehr, C.; Fickova, M.; Hiemke, C.; Reuss, S.; Dahmen, N.
Molecular cloning of rat G-protein-coupled receptor kinase 6 (GRK6) from brain tissue, and its mRNA expression in different brain regions and peripheral tissues
Brain Res. Mol. Brain Res.
49
278-282
1997
Rattus norvegicus (P97711)
Manually annotated by BRENDA team
Nagayama, Y.; Tanaka, K.; Hara, T.; Namba, H.; Yamashita, S.; Taniyama, K.; Niwa, M.
Involvement of G protein-coupled receptor kinase 5 in homologous desensitization of the thyrotropin receptor
J. Biol. Chem.
271
10143-10148
1996
Rattus norvegicus (Q62833)
Manually annotated by BRENDA team
Fraga, S.; Jose, P.A.; Soares-da-Silva, P.
Involvement of G protein-coupled receptor kinase 4 and 6 in rapid desensitization of dopamine D1 receptor in rat IEC-6 intestinal epithelial cells
Am. J. Physiol.
287
R772-779
2004
Rattus norvegicus
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
Simon, V.; Robin, M.T.; Legrand, C.; Cohen-Tannoudji, J.
Endogenous G protein-coupled receptor kinase 6 triggers homologous beta-adrenergic receptor desensitization in primary uterine smooth muscle cells
Endocrinology
144
3058-3066
2003
Rattus norvegicus
Manually annotated by BRENDA team
Fraga, S.; Luo, Y.; Jose, P.; Zandi-Nejad, K.; Mount, D.B.; Soares-da-Silva, P.
Dopamine D1-like receptor-mediated inhibition of Cl/HCO3- exchanger activity in rat intestinal epithelial IEC-6 cells is regulated by G protein-coupled receptor kinase 6 (GRK 6)
Cell. Physiol. Biochem.
18
347-360
2006
Rattus norvegicus
Manually annotated by BRENDA team
Bychkov, E.; Zurkovsky, L.; Garret, M.B.; Ahmed, M.R.; Gurevich, E.V.
Distinct cellular and subcellular distributions of G protein-coupled receptor kinase and arrestin isoforms in the striatum
PLoS ONE
7
e48912
2012
Rattus norvegicus
Manually annotated by BRENDA team
Franklin, J.M.; Carrasco, G.A.
G-protein receptor kinase 5 regulates the cannabinoid receptor 2-induced up-regulation of serotonin 2A receptors
J. Biol. Chem.
288
15712-15724
2013
Rattus norvegicus (Q62833)
Manually annotated by BRENDA team
Park, C.H.; Lee, J.H.; Lee, M.Y.; Lee, J.H.; Lee, B.H.; Oh, K.S.
A novel role of G protein-coupled receptor kinase 5 in urotensin II-stimulated cellular hypertrophy in H9c2UT cells
Mol. Cell. Biochem.
422
151-160
2016
Rattus norvegicus (Q62833)
Manually annotated by BRENDA team
Zeng, X.; Chen, S.; Gao, Q.; Zong, W.; Jiang, D.; Zeng, G.; Zhou, L.; Chen, L.; Luo, W.; Xiao, J.; Xiao, B.; Ouyang, D.; Hu, K.
The expression of G protein-coupled receptor kinase 5 and its interaction with dendritic marker microtubule-associated protein-2 after status epilepticus
Epilepsy Res.
138
62-70
2017
Rattus norvegicus (Q62833)
Manually annotated by BRENDA team