Information on EC 2.7.11.14 - rhodopsin kinase

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The enzyme appears in viruses and cellular organisms

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EC NUMBER
COMMENTARY hide
2.7.11.14
-
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RECOMMENDED NAME
GeneOntology No.
rhodopsin kinase
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + rhodopsin = ADP + phosphorhodopsin
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
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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).
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CAS REGISTRY NUMBER
COMMENTARY hide
54004-64-7
-
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
-
Manually annotated by BRENDA team
C57BL/6J mice
-
-
Manually annotated by BRENDA team
fly
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
a mouse line RKS561L is generated in which GRK1 is overexpressed (S56L mutant cDNA is used). Overexpressed GRK1 in RKS561L mice is located in the outer segment and greatly accelerates the rate of rhodopsin phosphorylation. Transgenic mice show that the light response amplitude is only modestly diminished, but the exponential decay constant of the response (tau REC) and the limiting time constant (tau D) are both highly significantly accelerated. It is concluded that GRK1 and recoverin, in addition to their role in phosphorylating rhodopsin, may also regulate light-activated phosphodiesterase decay and mediate the increase in temporal resolution of rods during light adaptation
physiological function
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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 + 11-cis-retinal-rhodopsin
ADP + 11-cis-retinal-phosphorhodopsin
show the reaction diagram
-
-
-
-
?
ATP + 13-cis-retinal-rhodopsin
ADP + 13-cis-retinal-phosphorhodopsin
show the reaction diagram
-
-
-
-
?
ATP + 338-SKTETSQVAPA-348
?
show the reaction diagram
ATP + 9-cis-retinal-rhodopsin
ADP + 9-cis-retinal-phosphorhodopsin
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + Ac-RRRAAAAASAAA-NH2
ADP + Ac-RRRAAAAApSAAA-NH2
show the reaction diagram
-
synthetic peptide substrate
-
-
?
ATP + arrestin
ADP + phospho-arrestin
show the reaction diagram
ATP + arrestin
ADP + phosphoarrestin
show the reaction diagram
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
show the reaction diagram
-
phosphorylates rhodopsin better than betaAR
-
-
?
ATP + cone opsin
ADP + phosphorylated cone opsin
show the reaction diagram
Q49HM8, Q49HM9
light-dependent phosporylation
-
-
?
ATP + DDEASTTVSKTETSQVARRR
?
show the reaction diagram
-
synthetic peptide C, very poor substrate
-
-
?
ATP + M cone opsin
ADP + phosphorylated M cone opsin
show the reaction diagram
ATP + M opsin
ADP + phosphorylated m opsin
show the reaction diagram
ATP + opsin
ADP + phosphoopsin
show the reaction diagram
ATP + peptide
ADP + phosphopeptide
show the reaction diagram
ATP + protein
ADP + phosphoprotein
show the reaction diagram
-
autophosphorylation
-
-
?
ATP + rhodopsin
ADP + phospho-rhodopsin
show the reaction diagram
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
show the reaction diagram
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
ATP + rhodopsin 1
ADP + phosphorhodopsin 1
show the reaction diagram
-
-
-
-
?
ATP + rhodopsin TM5
ADP + phosphorhodopsin TM5
show the reaction diagram
-
-
-
-
?
ATP + RRREEEEESAAA
ADP + RRREEEEE-(P)SAAA
show the reaction diagram
-
synthetic peptide substrate
-
-
?
ATP + S cone opsin
ADP + phosphorylated S cone opsin
show the reaction diagram
ATP + S opsin
ADP + phosphorylated S opsin
show the reaction diagram
ATPgammaS + rhodopsin
?
show the reaction diagram
-
ATPgammaS is a good substrate, 2-3 mol phosphate/mol rhodopsin
-
-
?
GTP + rhodopsin
GDP + phosphorhodopsin
show the reaction diagram
additional information
?
-
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + arrestin
ADP + phospho-arrestin
show the reaction diagram
-
the enzyme interacts with the squid visual arrestin, arrestin binding to photoactivated rhodopsin is a key mechanism of desensitization, overview
-
-
?
ATP + arrestin
ADP + phosphoarrestin
show the reaction diagram
-
phosphorylation of arrestin in the presence of Ca2+, occurs only after photoactivation in vivo, dual role of RK in the inactivation of the squid visual system
-
-
?
ATP + cone opsin
ADP + phosphorylated cone opsin
show the reaction diagram
Q49HM8, Q49HM9
light-dependent phosporylation
-
-
?
ATP + M opsin
ADP + phosphorylated m opsin
show the reaction diagram
ATP + opsin
ADP + phosphoopsin
show the reaction diagram
Q1XHL7, Q1XHM0, Q49HM9, Q49HN0
the enzyme is involved in the opsin deactivation process, GRK subtypes play a role in phosphorylating non-visual opsins in the particular extraretinal tissues
-
-
?
ATP + rhodopsin
ADP + phospho-rhodopsin
show the reaction diagram
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
show the reaction diagram
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
ATP + rhodopsin 1
ADP + phosphorhodopsin 1
show the reaction diagram
-
-
-
-
?
ATP + rhodopsin TM5
ADP + phosphorhodopsin TM5
show the reaction diagram
-
-
-
-
?
ATP + S opsin
ADP + phosphorylated S opsin
show the reaction diagram
additional information
?
-
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
Ca2+-independent phosphorylation of rhodopsin
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INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-(6-Amino-9H-purin-9-yl)-1-deoxy-N-ethyl-beta-D-furanuronamide
-
good inhibitor
2',3'-dideoxyadenosine
-
-
2-chloroadenosine
-
-
3'-deoxyadenosine
-
-
5'-(N-ethylcarbamoyl)adenosine
-
-
5'-AMP
5'-deoxyadenosine
-
-
5'-[p-(fluorosulfonyl)benzoyl]adenosine
-
pseudo-first-order kinetics, MgATP and ATP protect almost completely, rhodopsin only slightly, Mg2+ not at all
5,6-Dichloro-1-(beta-ribofuranosyl)-benzimidazole
-
-
8,2'-Anhydro-8-mercapto-9-(beta-D-arabinofuranosyl)adenine
-
weak
8,3'-Anhydro-8-oxy-9-(beta-D-xylofuranosyl)adenine
-
good inhibitor
8,5'-Anhydro-8-oxy-9-(beta-D-ribofuranosyl)adenine
-
-
8-Bromoadenosine
-
good inhibitor
adenine
-
-
adenosine
adenosine 5'-monosulfate
-
-
ADPbetaS
-
-
AMPS
-
-
arrestin
-
competes for binding to rhodopsin
-
ATP-analogues
-
weak or no inhibition, overview
ATPalphaS
-
S-isomer
Ca2+
-
at concentrations equal to Mg2+, forms an unproductive Ca-ATP complex, Mg2+ partially reverses
Calmodulin
cAMP
-
weak
chelator
-
-
-
D-myo-Inositol 1-phosphate
-
weak, above 0.1 mM, stimulates below
Dextran sulfate
-
strong
-
dibutyryl-cAMP
-
weak, not in the dark
Digitonin
diphosphate
-
-
EDTA
-
-
emulphogene
-
Formycin monophosphate
-
-
G-protein
-
competes for binding to rhodopsin
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GRK1 peptides
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bovine commercial preparation, inhibition analysis of enzyme binding to S-modulin, overview
-
heparin
inositol triphosphate
-
weak
isoquinoline derivative
-
-
-
K+
-
weak, only at high concentrations
Mastoparan
-
potent inhibitor
nucleoside analogue
-
overview
papaverine
-
weak, not in the dark
Peptides from cytosolic surface of rhodopsin
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-
-
Phosphodiesterase inhibitor SQ 20009
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light-dependent
polyanion
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polycation
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e.g. polyamines or polylysine, potent inhibitor
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Polyglutamic acid
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weak
polylysine
-
potent inhibitor
purine nucleotide
-
overview
-
pyrrolopyrimidine derivative
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preferentially in anti-configuration, strong
-
recoverin
-
S-modulin/recoverin
-
recombinant myristoylated S-modulin overexpressed in Escherichia coli, GRK1 activity is inhibited by binding of the Ca2+-bound form of S-modulin/recoverin, determination of the binding site by peptide mapping, binding involves Leu6, Asn12, and Tyr15, mutation of these residues reduces the inhibition significantly, inhibition mechanism, overview
-
Sangivamycin
-
strong, in vivo and in vitro
spermidine
-
potent inhibitor
spermine
-
at higher concentrations, activates at low concentrations
Synthetic peptide
-
corresponding to sequences within opsin loops 3-4 and 5-6 and the C-terminus, bleached rhodopsin as substrate
-
theophylline
-
light-dependent
Toyocamycin
-
strong
Transducin
-
inhibits the enzyme, recoverin expression is reduced in diabetic rat retina
-
Triphosphate
-
-
tubercidin 5'-phosphate
-
good inhibitor
Zn2+
-
1 mM, 90% inhibition
additional information
-
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
betagamma-subunit of a photoreceptor G protein
-
directly activates, 2.5fold
-
D-myo-Inositol 1-phosphate
-
about 20% activation, between 0.0003 mM and 0.1 mM, slightly inhibitory at higher concentrations
G-protein
-
dependent on
-
light
-
Mastoparan
polycation
-
activates approximately 2fold
-
rhodopsin
spermidine
-
slight stimulation
spermine
-
at low concentrations: up to 20% activation, inhibits at higher concentrations
additional information
-
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0016 - 0.166
ATP
0.027
ATPgammaS
-
pH 7.5, 30°C
7.1
DDEASTTVSKTETSQVARRR
-
pH 7.5, 30°C, peptide C
0.4 - 1
GTP
0.00062 - 30
rhodopsin
2
RRREEEEESAAA
-
pH 7.5, 30°C
-
additional information
additional information
-
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1 - 1.2
rhodopsin
additional information
additional information
-
ATP: 2.2 mol of phosphate bound/min, GTP: 0.12 mol of phosphate bound/min
-
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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.016
1-(6-Amino-9H-purin-9-yl)-1-deoxy-N-ethyl-beta-D-furanuronamide
-
pH 7.5, 30°C
0.065
2',3'-dideoxyadenosine
-
pH 7.5, 25°C
0.016
3'-deoxyadenosine
-
pH 7.5, 25°C
0.005
5'-AMP
0.01
5'-deoxyadenosine
-
pH 7.5, 25°C
0.9
5'-[p-(fluorosulfonyl)benzoyl]adenosine
-
pH 7.5, 25°C
0.004
5,6-Dichloro-1-(beta-ribofuranosyl)-benzimidazole
-
pH 7.5, 30°C
0.52
8,2'-Anhydro-8-mercapto-9-(beta-D-arabinofuranosyl)adenine
-
pH 7.5, 30°C
0.01
8,3'-Anhydro-8-oxy-9-(beta-D-xylofuranosyl)adenine
-
pH 7.5, 30°C
0.027
8,5'-Anhydro-8-oxy-9-(beta-D-ribofuranosyl)adenine
-
pH 7.5, 30°C
0.02
8-Bromoadenosine
-
pH 7.5, 30°C
0.0087
adenine
-
pH 7.5, 30°C
0.004
adenosine
0.08
adenosine 5'-monosulfate
-
pH 7.5, 25°C
0.012
ADP
0.022
ADPbetaS
-
pH 7.5, 30°C
0.022
AMPS
-
pH 7.5, 30°C
0.035
ATPalphaS
-
pH 7.5, 30°C, S-isomer
0.024
diphosphate
-
pH 7.5, 30°C
0.036
Formycin monophosphate
-
pH 7.5, 30°C
0.3
heparin
-
pH 7.5, 30°C
0.00018
Sangivamycin
-
pH 7.5, 30°C
0.014
Triphosphate
-
pH 7.5, 30°C
0.0036
tubercidin 5'-phosphate
-
pH 7.5, 30°C
additional information
additional information
-
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.01
-
pH 7.4
0.013
-
-
0.017
-
pH 7.4, 37°C
0.026 - 0.033
0.028
-
pH 7.4, 37°C
0.04
-
pH 7.4, 30°C, recombinant RK expressed in COS-1 cells, purified in absence or presence of ATP
0.046
-
pH 7.4, 15°C
0.062
-
pH 7.5, 23°C
0.097
-
pH 7.5, 30°C
0.1 - 0.7
-
-
0.18 - 0.55
-
32°C
0.5 - 0.85
0.555
-
pH 7.5
0.96
-
pH 7.5, 25°C
1.2
-
recombinant RK expressed in SF9 cells
additional information
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 8
-
-
6.5
-
recombinant RK expressed in Sf21 cells
6.67
-
RK from rod outer segments
7.2
-
assay at
8.5
-
assay at, synthetic peptide substrates
additional information
-
activity/pH-profile with synthetic peptide 327-347 as substrate
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.3 - 8.7
-
pH 6.3: about 75% of maximal activity, pH 8.7: about half-maximal activity
6.67
-
RK from rod outer segments: 60% of activity is lost with one pH unit change, recombinant RK expressed in COS-1 cells shows broader activity profile
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
23
-
assay at
25 - 30
assay at; assay at; assay at; assay at
26
-
assay at
32
-
assay at
36
-
about, native RK and recombinant RK expressed in Sf21 cells
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
GRK7-2, almost exclusively in the brain
Manually annotated by BRENDA team
Q49HM8, Q49HM9
-
Manually annotated by BRENDA team
additional information
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
recombinant RK, in both plasma membranes and cytosolic fractions
Manually annotated by BRENDA team
additional information
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
50000
-
1 * 50000, SDS-PAGE
53000
-
gel filtration
62200
-
x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE
62900
-
x * 62900, calculated from the amino acid sequence
63000
-
x * 63000, Western blot analysis
63500
-
x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE
67000
-
gel filtration
68000
-
sucrose density gradient centrifugation
70000
-
1 * 70000, SDS-PAGE
80000
-
x * 80000, SDS-PAGE, predicted from the ork gene sequence
additional information
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SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
-
wild-type, crystal structure
monomer
additional information