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Information on EC 2.7.11.14 - rhodopsin kinase and Organism(s) Homo sapiens and UniProt Accession Q8WTQ7

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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). Acts on the bleached or activated form of rhodopsin; also phosphorylates the beta-adrenergic receptor, but more slowly. Does not act on casein, histones or phosphvitin. Inhibited by Zn2+ and digitonin (cf. EC 2.7.11.15, beta-adrenergic-receptor kinase and EC 2.7.11.16, G-protein-coupled receptor kinase).
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Homo sapiens
UNIPROT: Q8WTQ7
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
Synonyms
rk, rhodopsin kinase, g protein-coupled receptor kinase, g-protein receptor kinase, g-protein coupled receptor kinase, g protein-coupled receptor kinase 1, gprk1, g-protein coupled receptor kinase 1, g-protein-coupled receptor kinase 1, g-protein receptor kinase-1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
G protein-coupled receptor kinase GRK7
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G protein-coupled receptor kinase
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G protein-coupled receptor kinase 1
-
-
-
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G-protein coupled receptor kinase
-
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GPCR kinase 1
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-
-
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GRK7
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kinase (phosphorylating), opsin
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-
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kinase (phosphorylating), rhodopsin
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-
-
-
opsin kinase
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-
-
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rhodopsin kinase
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RK
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
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-
-
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SYSTEMATIC NAME
IUBMB Comments
ATP:rhodopsin phosphotransferase
Requires G-protein for activation and therefore belongs to the family of G-protein-dependent receptor kinases (GRKs). Acts on the bleached or activated form of rhodopsin; also phosphorylates the beta-adrenergic receptor, but more slowly. Does not act on casein, histones or phosphvitin. Inhibited by Zn2+ and digitonin (cf. EC 2.7.11.15, beta-adrenergic-receptor kinase and EC 2.7.11.16, G-protein-coupled receptor kinase).
CAS REGISTRY NUMBER
COMMENTARY hide
54004-64-7
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + rhodopsin
ADP + phosphorhodopsin
show the reaction diagram
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
ATP + RRREEEEESAAA
ADP + RRREEEEE-(P)SAAA
show the reaction diagram
-
synthetic peptide substrate
-
-
?
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 + rhodopsin
ADP + phosphorhodopsin
show the reaction diagram
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
additional information
?
-
kinase plays a role in human visual signaling
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-
?
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
paroxetine
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0106 - 0.0214
ATP
0.0019 - 0.0044
rhodopsin
2
RRREEEEESAAA
-
pH 7.5, 30°C
additional information
additional information
-
kinetics
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1 - 1.2
rhodopsin
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7
-
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
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
recombinant RK, in both plasma membranes and cytosolic fractions
Manually annotated by BRENDA team
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recombinant RK, in both plasma membranes and cytosolic fractions
Manually annotated by BRENDA team
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
GRK7_HUMAN
553
0
62212
Swiss-Prot
other Location (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
62200
-
x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE
63000
-
x * 63000, Western blot analysis
63500
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x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
lipoprotein
-
the enzyme contains a myristoylation site at the N-terminus and a C-terminal farnesylation site, overview
phosphoprotein
side-chain modification
prenylated and carboxyl-methylated at Cys-558
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D116R
the mutant shows reduced activity compared to the wild type enzyme
E238A
the mutant shows reduced activity compared to the wild type enzyme
E521A
the mutant shows reduced activity compared to the wild type enzyme
F122E
the mutant shows increased activity compared to the wild type enzyme
F125E
the mutant shows reduced activity compared to the wild type enzyme
F528E
inactive
G529A
the mutant shows increased activity compared to the wild type enzyme
K120E
the mutant shows reduced activity compared to the wild type enzyme
K219A
inactive
K219R
K220R
-
kinase inactive mutant of GRK7
K33E
the mutant shows reduced activity compared to the wild type enzyme
K34A
the mutant shows reduced activity compared to the wild type enzyme
K38A
the mutant shows reduced activity compared to the wild type enzyme
K40C
the mutant shows reduced activity compared to the wild type enzyme
L169A
the mutant shows reduced activity compared to the wild type enzyme
L172C
the mutant shows reduced activity compared to the wild type enzyme
L39G
inactive
L41G
inactive
L531E
the mutant shows reduced activity compared to the wild type enzyme
L71A
inactive
P117A
the mutant shows reduced activity compared to the wild type enzyme
P391H
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a naturally occuring homozygous mutation in gene GRK1 leading to the Oguchi disease, a stationary blindness with autosomal recessive transmission, with markedly reduced cone response
P42A
the mutant shows reduced activity compared to the wild type enzyme
Q118A
the mutant shows reduced activity compared to the wild type enzyme
Q176A
inactive
Q74A
the mutant shows reduced activity compared to the wild type enzyme
R173A
the mutant shows reduced activity compared to the wild type enzyme
R461A
the mutant shows wild type activity
S124L
the mutant shows wild type activity
S21A
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site-directed mutagenesis of GRK1 PKA phosphorylation site, the mutant shows 87% of wild-type enzyme activity
S21E
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site-directed mutagenesis of GRK1 PKA phosphorylation site, the mutant shows 80% of wild-type enzyme activity
S23A
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site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 67% of wild-type enzyme activity
S23A/S36A
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site-directed mutagenesis of GRK7 PKA phosphorylation sites, the mutant shows 81% of wild-type enzyme activity
S23E
-
site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 67% of wild-type enzyme activity
S23E/S36E
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site-directed mutagenesis of GRK7 PKA phosphorylation sites, the mutant shows 79% of wild-type enzyme activity
S333A
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site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme
S36A
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site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 76% of wild-type enzyme activity
S36E
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site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 77% of wild-type enzyme activity
S441A
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site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme
S490A
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site-directed mutagenesis of GRK7, the mutant is unable to autophosphorylate
S490E
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site-directed mutagenesis of GRK7, the mutant is unable to autophosphorylate
T212G
inactive
T353A
-
site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme
T97G
the mutant shows wild type activity
W177A
inactive
Y170A/Q176A
inactive
Y170A/W177A
inactive
Y255A
the mutant shows reduced activity compared to the wild type enzyme
Y35A
the mutant shows reduced activity compared to the wild type enzyme
additional information
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant FLAG-tagged wild-type and mutant GRK1 and GRK7 from HEK-293 cells
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recombinant His-tagged GRK1 and GRK1b, expressed in Escherichia coli M15
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
cDNA encoding RK is cloned, amino acid sequence
cDNAs encoding full-length RK and C-terminus-truncated mutant RK lacking the last 59 amino acids are cloned and expressed in HEK-293 cells
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expressed in Sf9 insect cells
expression of FLAG-tagged wild-type and mutant GRK1 and GRK7 in HEK-293 cells
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gene GRK1, DNA and amino acid sequence determination and analysis, spatial profile and transcriptional mechanism, interactions with cone-rod homeodomain transcription factor Crx, as well as transcription factors Otx2, Nr2e3, and Nrl at the homeodomain in the 5' flanking sequence of the promoter region, overview, phylogenetic analysis
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gene GRK1, DNA and amino acid sequence determination and anaylsis of wild-type enzyme mutant genes
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GRK1 and GRK1b are cloned from fovea, sequenced and expressed in Escherichia coli M15, GRK1b is a splice variant of GRK1 with low catalytic activity transcribed in photoreceptors, GRK1b is produced by retention of the last intron 6 and differs in its C-terminal region next to the catalytic domain
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GRK1 gene with 7 exons is located on chromosome 13q34 and encodes a 561 amino acids protein
RK gene encodes a 564 amino acids polypeptide
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RK gene is located on chromosome 13q34
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Khani, S.C.; Abitbol, M.; Yamamoto, S.; Maravic-Magovcevic, I.; Dryja, T.P.
Characterization and chromosomal localization of the gene for human rhodopsin kinase
Genomics
35
571-576
1996
Homo sapiens (Q15835), Homo sapiens
Manually annotated by BRENDA team
Yamamoto, S.; Sippel, K.C.; Berson, E.L.; Dryja, T.P.
Defects in the rhodopsin kinase gene in the Oguchi form of stationary night blindness
Nat. Genet.
15
175-178
1997
Homo sapiens (Q15835), Homo sapiens
Manually annotated by BRENDA team
Zhao, X.; Haeseleer, F.; Fariss, R.N.; Huang, J.; Baehr, W.; Milam, A.H.; Palczewski, K.
Molecular cloning and localization of rhodopsin kinase in the mammalian pineal
Vis. Neurosci.
14
225-232
1997
Homo sapiens (Q15835), Homo sapiens, Rattus norvegicus (Q63651)
Manually annotated by BRENDA team
Weiss, E.R.; Ducceschi, M.H.; Horner, T.J.; Li, A.; Craft, C.M.; Osawa, S.
Species-specific differences in expression of G-protein-coupled receptor kinase (GRK) 7 and GRK1 in mammalian cone photoreceptor cells: implications for cone cell phototransduction
J. Neurosci.
21
9175-9184
2001
Homo sapiens (Q8WTQ7)
Manually annotated by BRENDA team
Yu, Q.M.; Cheng, Z.J.; Zhao, J.; Zhou, T.H.; Wu, Y.L.; Ma, L.; Pei, G.
Carboxyl terminal of rhodopsin kinase is required for the phosphorylation of photo-activated rhodopsin
Cell Res.
8
303-310
1998
Homo sapiens
Manually annotated by BRENDA team
Chen, C.K.
Recoverin and rhodopsin kinase
Adv. Exp. Med. Biol.
514
101-107
2002
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Senin, I.I.; Koch, K.W.; Akhtar, M.; Philippov, P.P.
Ca2+-dependent control of rhodopsin phosphorylation: Recoverin and rhodopsin kinase
Adv. Exp. Med. Biol.
514
69-99
2002
Bos taurus, Homo sapiens, Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Sokal, I.; Pulvermller, A.; Buczylko, J.; Hofmann, K.P.; Palczewski, K.
Rhodopsin and its kinase
Methods Enzymol.
343
578-600
2001
Bos taurus, Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Zhao, X.; Huang, J.; Khani, S.C.; Palczewski, K.
Molecular forms of human rhodopsin kinase (GRK1)
J. Biol. Chem.
273
5124-5131
1998
Homo sapiens, Gallus gallus (O73685), Gallus gallus
Manually annotated by BRENDA team
Maeda, T.; Imanishi, Y.; Palczewski, K.
Rhodopsin phosphorylation: 30 years later
Prog. Retin. Eye Res.
22
417-434
2003
Bos taurus, Homo sapiens, Homo sapiens (Q15835), Oryzias latipes, Mus musculus, Rattus norvegicus, Gallus gallus (O73685), Enteroctopus dofleini (O97020), Doryteuthis pealeii (Q9N2R0)
Manually annotated by BRENDA team
Horner, T.J.; Osawa, S.; Schaller, M.D.; Weiss, E.R.
Phosphorylation of GRK1 and GRK7 by cAMP-dependent protein kinase attenuates their enzymatic activities
J. Biol. Chem.
280
28241-28250
2005
Homo sapiens
Manually annotated by BRENDA team
Young, J.E.; Kasperek, E.M.; Vogt, T.M.; Lis, A.; Khani, S.C.
Conserved interactions of a compact highly active enhancer/promoter upstream of the rhodopsin kinase (GRK1) gene
Genomics
90
236-248
2007
Homo sapiens
Manually annotated by BRENDA team
Hayashi, T.; Gekka, T.; Takeuchi, T.; Goto-Omoto, S.; Kitahara, K.
A novel homozygous GRK1 mutation (P391H) in 2 siblings with Oguchi disease with markedly reduced cone responses
Ophthalmology
114
134-141
2007
Homo sapiens
Manually annotated by BRENDA team
He, Y.; Gao, X.; Goswami, D.; Hou, L.; Pal, K.; Yin, Y.; Zhao, G.; Ernst, O.P.; Griffin, P.; Melcher, K.; Xu, H.E.
Molecular assembly of rhodopsin with G protein-coupled receptor kinases
Cell Res.
27
728-747
2017
Homo sapiens (Q15835)
Manually annotated by BRENDA team