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Information on EC 2.7.11.16 - G-protein-coupled receptor kinase and Organism(s) Bos taurus and UniProt Accession P43249

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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).
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Bos taurus
UNIPROT: P43249
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The taxonomic range for the selected organisms is: Bos taurus
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 5
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G protein-coupled receptor kinase GRK5
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G protein-coupled receptor kinase 5
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GRK5
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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
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SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + beta 2-adrenergic receptor
ADP + phosphorylated beta 2-adrenergic receptor
show the reaction diagram
phosphorylation in an agonist-dependent manner, phosphorylates the C-terminal tail regions of both receptor proteins
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-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
major autophosphorylation sites are Ser484 and Thr485
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-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
GRK5 phosphorylates rhodopsin in a light-dependent manner, phosphorylates the C-terminal tail region
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
show the reaction diagram
-
-
-
?
additional information
?
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GRK5 elevates blood pressure in vascular smooth muscle via Gi signaling involing the beta1-adrenergic receptor, mechanism overview
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-
?
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
-
-
-
?
additional information
?
-
-
GRK5 elevates blood pressure in vascular smooth muscle via Gi signaling involing the beta1-adrenergic receptor, mechanism overview
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
CCG215022
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GSK180736A
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paroxetine
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Takeda103A
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
very weak activity
Manually annotated by BRENDA team
high activity
Manually annotated by BRENDA team
very weak activity
Manually annotated by BRENDA team
very weak activity
Manually annotated by BRENDA team
high activity
Manually annotated by BRENDA team
high activity
Manually annotated by BRENDA team
very weak activity
Manually annotated by BRENDA team
additional information
most abundantly in lung, heart, retina, and lingual epithelium, but expressed very little in brain, liver, kidney, or testis
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GRK5 protein does not undergo agonist-dependent translocation from cytosol to membranes as do beta-adrenergic receptor kinase and rhodopsin kinase, but rather appears to associate with membranes constitutively
Manually annotated by BRENDA team
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
GRK5_BOVIN
590
0
67889
Swiss-Prot
other Location (Reliability: 2)
PDB
SCOP
CATH
UNIPROT
ORGANISM
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
major autophosphorylation sites are Ser484 and Thr485
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
in complex with CCG215022, hanging drop vapor diffusion method, using 100 mM HEPES, pH 7.5, 4% (v/v) ethylene glycol, and 12% (w/v) PEG3350
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
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construction of transgenic mice overexpressing GRK5 2fold in vascular smooth muscle leading to hypertension in the mutant mice with a 25-35% increase in blood pressure, which segregates with sex, male show higher blood pressure than female mice, and is dependent on Gi-mediated signaling, inhibition of the latter by pertussis toxin or inhibition of beta1-adrenergic receptor activity restore blood pressure to normal level
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
Ni-NTA column chromatography and S200 gel filtration
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
gene encoding GRK5 with SM22alpha promoter for construction of transgenic mice expressing the enzyme in vascular smooth muscle
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REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Premont, R.T.; Koch, W.J.; Inglese, J.; Lefkowitz, R.J.
Identification, purification, and characterization of GRK5, a member of the family of G protein-coupled receptor kinases
J. Biol. Chem.
269
6832-6841
1994
Bos taurus (P43249)
Manually annotated by BRENDA team
Keys, J.R.; Zhou, R.H.; Harris, D.M.; Druckman, C.A.; Eckhart, A.D.
Vascular smooth muscle overexpression of G protein-coupled receptor kinase 5 elevates blood pressure, which segregates with sex and is dependent on Gi-mediated signaling
Circulation
112
1145-1153
2005
Bos taurus
Manually annotated by BRENDA team
Homan, K.T.; Waldschmidt, H.V.; Glukhova, A.; Cannavo, A.; Song, J.; Cheung, J.Y.; Koch, W.J.; Larsen, S.D.; Tesmer, J.J.
Crystal structure of G protein-coupled receptor kinase 5 in complex with a rationally designed inhibitor
J. Biol. Chem.
290
20649-20659
2015
Bos taurus (P43249)
Manually annotated by BRENDA team