BRENDA - Enzyme Database show
show all sequences of 2.7.11.16

The G protein-coupled receptor kinase (GRK) interactome: Role of GRKs in GPCR regulation and signaling

Ribas, C.; Penela, P.; Murga, C.; Salcedo, A.; Garcia-Hoz, C.; Jurado-Pueyo, M.; Aymerich, I.; Mayor, F.; Biochim. Biophys. Acta 1768, 913-922 (2007)

Data extracted from this reference:

Activating Compound
Activating Compound
Commentary
Organism
Structure
additional information
phosphorylation activates the enzyme
Homo sapiens
Inhibitors
Inhibitors
Commentary
Organism
Structure
actin
-
Homo sapiens
alpha-actinin
-
Homo sapiens
Calmodulin
-
Homo sapiens
caveolin
-
Homo sapiens
RKIP
-
Homo sapiens
Localization
Localization
Commentary
Organism
GeneOntology No.
Textmining
membrane
-
Mammalia
16020
-
nucleus
GRK5
Mammalia
5634
-
Metals/Ions
Metals/Ions
Commentary
Organism
Structure
Mg2+
-
Homo sapiens
Molecular Weight [Da]
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
Organism
69000
-
x * 69000, GRK5, SDS-PAGE
Homo sapiens
69000
-
x * 69000, about, GRK5 catalytic domain, domain structure, overview
Mammalia
Natural Substrates/ Products (Substrates)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
additional information
Homo sapiens
GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview
?
-
-
-
additional information
Mammalia
G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP
?
-
-
-
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
-
-
-
Mammalia
-
-
-
Posttranslational Modification
Posttranslational Modification
Commentary
Organism
phosphoprotein
phosphorylation, e.g. by PKA, PKC, ERK1/2 or c-SRC, activates the enzyme
Homo sapiens
Source Tissue
Source Tissue
Commentary
Organism
Textmining
cerebellum
GRK4
Mammalia
-
kidney
GRK4
Mammalia
-
additional information
GRK5 and GRK6 are ubiquitously expressed in mammalian tissues
Mammalia
-
testis
GRK4
Mammalia
-
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
additional information
GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview
672408
Homo sapiens
?
-
-
-
-
additional information
G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP
672408
Mammalia
?
-
-
-
-
additional information
no interaction of the RH domains of GRK5 and GRK6 with Galpha proteins. GRK5 contains a DNA-binding nuclear localization sequence that allows its binding to DNA and its localization in the nucleus upon GPCR activation, interaction with other oroteins, detailed overview
672408
Mammalia
?
-
-
-
-
Subunits
Subunits
Commentary
Organism
?
x * 69000, GRK5, SDS-PAGE
Homo sapiens
?
x * 69000, about, GRK5 catalytic domain, domain structure, overview
Mammalia
More
domain structure of GRK4-6, overview
Homo sapiens
Cofactor
Cofactor
Commentary
Organism
Structure
ATP
-
Homo sapiens
Activating Compound (protein specific)
Activating Compound
Commentary
Organism
Structure
additional information
phosphorylation activates the enzyme
Homo sapiens
Cofactor (protein specific)
Cofactor
Commentary
Organism
Structure
ATP
-
Homo sapiens
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
actin
-
Homo sapiens
alpha-actinin
-
Homo sapiens
Calmodulin
-
Homo sapiens
caveolin
-
Homo sapiens
RKIP
-
Homo sapiens
Localization (protein specific)
Localization
Commentary
Organism
GeneOntology No.
Textmining
membrane
-
Mammalia
16020
-
nucleus
GRK5
Mammalia
5634
-
Metals/Ions (protein specific)
Metals/Ions
Commentary
Organism
Structure
Mg2+
-
Homo sapiens
Molecular Weight [Da] (protein specific)
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
Organism
69000
-
x * 69000, GRK5, SDS-PAGE
Homo sapiens
69000
-
x * 69000, about, GRK5 catalytic domain, domain structure, overview
Mammalia
Natural Substrates/ Products (Substrates) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
additional information
Homo sapiens
GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview
?
-
-
-
additional information
Mammalia
G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP
?
-
-
-
Posttranslational Modification (protein specific)
Posttranslational Modification
Commentary
Organism
phosphoprotein
phosphorylation, e.g. by PKA, PKC, ERK1/2 or c-SRC, activates the enzyme
Homo sapiens
Source Tissue (protein specific)
Source Tissue
Commentary
Organism
Textmining
cerebellum
GRK4
Mammalia
-
kidney
GRK4
Mammalia
-
additional information
GRK5 and GRK6 are ubiquitously expressed in mammalian tissues
Mammalia
-
testis
GRK4
Mammalia
-
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
additional information
GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview
672408
Homo sapiens
?
-
-
-
-
additional information
G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP
672408
Mammalia
?
-
-
-
-
additional information
no interaction of the RH domains of GRK5 and GRK6 with Galpha proteins. GRK5 contains a DNA-binding nuclear localization sequence that allows its binding to DNA and its localization in the nucleus upon GPCR activation, interaction with other oroteins, detailed overview
672408
Mammalia
?
-
-
-
-
Subunits (protein specific)
Subunits
Commentary
Organism
?
x * 69000, GRK5, SDS-PAGE
Homo sapiens
?
x * 69000, about, GRK5 catalytic domain, domain structure, overview
Mammalia
More
domain structure of GRK4-6, overview
Homo sapiens
Other publictions for EC 2.7.11.16
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
738372
Packiriswamy
Bacterial dose-dependent role ...
Mus musculus
Infect. Immun.
84
1633-1641
2016
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1
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2
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739053
Park
A novel role of G protein-coup ...
Rattus norvegicus
Mol. Cell. Biochem.
422
151-160
2016
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738643
Li
G protein-coupled receptor kin ...
Homo sapiens
J. Biol. Chem.
290
10775-10790
2015
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738655
Allen
Structure and function of the ...
Homo sapiens
J. Biol. Chem.
290
20360-20373
2015
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738658
Homan
Crystal structure of G protein ...
Bos taurus
J. Biol. Chem.
290
20649-20659
2015
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1
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5
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1
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737975
Chakraborty
G protein-coupled receptor kin ...
Homo sapiens
Cancer Res.
74
3489-3500
2014
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1
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1
1
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738580
Franklin
G-protein receptor kinase 5 re ...
Rattus norvegicus
J. Biol. Chem.
288
15712-15724
2013
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1
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1
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739464
Johnson
Distinct structural features o ...
Homo sapiens
PLoS ONE
8
e62508
2013
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1
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1
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1
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725471
So
G protein-coupled receptor kin ...
Homo sapiens
J. Biol. Chem.
287
17088-17099
2012
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1
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1
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2
2
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725509
Michal
G Protein-coupled receptor kin ...
Homo sapiens
J. Biol. Chem.
287
6928-6940
2012
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1
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1
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2
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725847
Kim
G-protein coupled receptor kin ...
Homo sapiens
J. Urol.
187
322-329
2012
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1
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2
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726308
Bychkov
Distinct cellular and subcellu ...
Rattus norvegicus
PLoS ONE
7
e48912
2012
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4
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1
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726276
Guo
Regulation of C3a receptor sig ...
Homo sapiens
PLoS ONE
6
e22559
2011
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725394
Chen
G-protein-coupled receptor kin ...
Homo sapiens
J. Biol. Chem.
285
12823-12830
2010
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2
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705737
Wang
Inhibition of WNT signaling by ...
Homo sapiens
Mol. Endocrinol.
23
1455-1465
2009
-
1
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1
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2
2
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684355
Cohn
Inhibition of vascular smooth ...
Mus musculus
Am. J. Physiol. Heart Circ. Physiol.
295
H1695-H1704
2008
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-
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1
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2
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2
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2
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1
1
1
1
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684898
Keever
G protein-coupled receptor kin ...
Homo sapiens
Biochem. Biophys. Res. Commun.
367
649-655
2008
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1
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1
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685871
Eijkelkamp
G protein-coupled receptor kin ...
Mus musculus
Brain Behav. Immun.
23
18-26
2008
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1
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1
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3
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Nagayama
Involvement of G protein-coupl ...
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1996
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4
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4
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491136
Sallese
Two isoforms of G protein-coup ...
Homo sapiens
Biochem. Biophys. Res. Commun.
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848-854
1994
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491154
Premont
Identification, purification, ...
Bos taurus
J. Biol. Chem.
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9
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3
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491155
Stoffel
Palmitoylation of G protein-co ...
Homo sapiens
J. Biol. Chem.
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27791-27794
1994
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491143
Kunapuli
Cloning and expression of GRK5 ...
Homo sapiens
Proc. Natl. Acad. Sci. USA
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5588-5592
1993
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491156
Benovic
Molecular cloning and expressi ...
Homo sapiens
J. Biol. Chem.
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19521-19527
1993
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7
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491137
Ambrose
A novel G protein-coupled rece ...
Homo sapiens
Hum. Mol. Genet.
1
697-703
1992
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