BRENDA - Enzyme Database show
show all sequences of 2.7.11.16

Regulation of G protein-coupled receptor kinases and arrestins during receptor desensitization

Kohout, T.A.; Lefkowitz, R.J.; Mol. Pharmacol. 63, 9-18 (2003)

Data extracted from this reference:

Activating Compound
Activating Compound
Commentary
Organism
Structure
arrestins
arrestins modulate the enzyme activity having a regulatory role, regulation of arrestins, overview
Mus musculus
additional information
autophosphorylation of GRK5 is stimulated by phospholipids, such as phosphatidylinositol-4,5-bisphosphate
Mus musculus
Engineering
Amino acid exchange
Commentary
Organism
additional information
phenotypes of several GRK and arrestin knockout mice mutants and of transgenic mice overexpressing GRK4 or GRK5, overview
Mus musculus
Inhibitors
Inhibitors
Commentary
Organism
Structure
Ca2+/calmodulin
inhibit GRK5 with an IC50 of 40-50 nM, inhibition mechanism via inducing inhibitory autophosphorylation and blocking of membrane association
Mus musculus
Localization
Localization
Commentary
Organism
GeneOntology No.
Textmining
plasma membrane
constitutive association, location of GRK4-6 near the activated receptors, covalent attachment by fatty acids to the C-terminus, e.g. palmitoylated GRK4 and GRK6, or by electrostatic interactions with phospholipids, e.g. for GRK5
Mus musculus
5886
-
Metals/Ions
Metals/Ions
Commentary
Organism
Structure
Mg2+
-
Mus musculus
Natural Substrates/ Products (Substrates)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
ATP + beta-adrenergic receptor
Mus musculus
desensitization of the receptor by GRK4, GRK5, and GRK6
ADP + phosphorylated beta-adrenergic receptor
-
-
?
ATP + G protein-coupled receptor
Mus musculus
phosphorylation has a regulatory role
ADP + phosphorylated G protein-coupled receptor
-
-
?
additional information
Mus musculus
G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview
?
-
-
-
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Mus musculus
-
-
-
Posttranslational Modification
Posttranslational Modification
Commentary
Organism
lipoprotein
GRK4-6 are permanently modulated by fatty acids and/or phospholipids
Mus musculus
phosphoprotein
regulation of GRK5 by phosphorylation through PKC, GRK5 is activated by autophosphorylation, autophosphorylation is stimulated by phospholipids, such as phosphatidylinositol-4,5-bisphosphate, overview
Mus musculus
Purification (Commentary)
Commentary
Organism
GRK2 by gel filtration from Sf9 cells
Mus musculus
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
ATP + beta-adrenergic receptor
desensitization of the receptor by GRK4, GRK5, and GRK6
662911
Mus musculus
ADP + phosphorylated beta-adrenergic receptor
-
-
-
?
ATP + G protein-coupled receptor
phosphorylation has a regulatory role
662911
Mus musculus
ADP + phosphorylated G protein-coupled receptor
-
-
-
?
ATP + G protein-coupled receptor
the GPCRs possess multiple phosphorylation sites for serine/threonine kinases
662911
Mus musculus
ADP + phosphorylated G protein-coupled receptor
-
-
-
?
additional information
G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview
662911
Mus musculus
?
-
-
-
-
additional information
the GRKs are specific for GPCRs and arrestins, overview
662911
Mus musculus
?
-
-
-
-
Cofactor
Cofactor
Commentary
Organism
Structure
ATP
-
Mus musculus
IC50 Value
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.00004
0.00005
inhibit GRK5 with an IC50 of 40-50 nM, inhibition mechanism via inducing inhibitory autophosphorylation and blocking of membrane association
Mus musculus
Ca2+/calmodulin
Activating Compound (protein specific)
Activating Compound
Commentary
Organism
Structure
arrestins
arrestins modulate the enzyme activity having a regulatory role, regulation of arrestins, overview
Mus musculus
additional information
autophosphorylation of GRK5 is stimulated by phospholipids, such as phosphatidylinositol-4,5-bisphosphate
Mus musculus
Cofactor (protein specific)
Cofactor
Commentary
Organism
Structure
ATP
-
Mus musculus
Engineering (protein specific)
Amino acid exchange
Commentary
Organism
additional information
phenotypes of several GRK and arrestin knockout mice mutants and of transgenic mice overexpressing GRK4 or GRK5, overview
Mus musculus
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.00004
0.00005
inhibit GRK5 with an IC50 of 40-50 nM, inhibition mechanism via inducing inhibitory autophosphorylation and blocking of membrane association
Mus musculus
Ca2+/calmodulin
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
Ca2+/calmodulin
inhibit GRK5 with an IC50 of 40-50 nM, inhibition mechanism via inducing inhibitory autophosphorylation and blocking of membrane association
Mus musculus
Localization (protein specific)
Localization
Commentary
Organism
GeneOntology No.
Textmining
plasma membrane
constitutive association, location of GRK4-6 near the activated receptors, covalent attachment by fatty acids to the C-terminus, e.g. palmitoylated GRK4 and GRK6, or by electrostatic interactions with phospholipids, e.g. for GRK5
Mus musculus
5886
-
Metals/Ions (protein specific)
Metals/Ions
Commentary
Organism
Structure
Mg2+
-
Mus musculus
Natural Substrates/ Products (Substrates) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
ATP + beta-adrenergic receptor
Mus musculus
desensitization of the receptor by GRK4, GRK5, and GRK6
ADP + phosphorylated beta-adrenergic receptor
-
-
?
ATP + G protein-coupled receptor
Mus musculus
phosphorylation has a regulatory role
ADP + phosphorylated G protein-coupled receptor
-
-
?
additional information
Mus musculus
G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview
?
-
-
-
Posttranslational Modification (protein specific)
Posttranslational Modification
Commentary
Organism
lipoprotein
GRK4-6 are permanently modulated by fatty acids and/or phospholipids
Mus musculus
phosphoprotein
regulation of GRK5 by phosphorylation through PKC, GRK5 is activated by autophosphorylation, autophosphorylation is stimulated by phospholipids, such as phosphatidylinositol-4,5-bisphosphate, overview
Mus musculus
Purification (Commentary) (protein specific)
Commentary
Organism
GRK2 by gel filtration from Sf9 cells
Mus musculus
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
ATP + beta-adrenergic receptor
desensitization of the receptor by GRK4, GRK5, and GRK6
662911
Mus musculus
ADP + phosphorylated beta-adrenergic receptor
-
-
-
?
ATP + G protein-coupled receptor
phosphorylation has a regulatory role
662911
Mus musculus
ADP + phosphorylated G protein-coupled receptor
-
-
-
?
ATP + G protein-coupled receptor
the GPCRs possess multiple phosphorylation sites for serine/threonine kinases
662911
Mus musculus
ADP + phosphorylated G protein-coupled receptor
-
-
-
?
additional information
G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview
662911
Mus musculus
?
-
-
-
-
additional information
the GRKs are specific for GPCRs and arrestins, overview
662911
Mus musculus
?
-
-
-
-
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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739053
Park
A novel role of G protein-coup ...
Rattus norvegicus
Mol. Cell. Biochem.
422
151-160
2016
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738643
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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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5
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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
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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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739464
Johnson
Distinct structural features o ...
Homo sapiens
PLoS ONE
8
e62508
2013
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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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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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725847
Kim
G-protein coupled receptor kin ...
Homo sapiens
J. Urol.
187
322-329
2012
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726308
Bychkov
Distinct cellular and subcellu ...
Rattus norvegicus
PLoS ONE
7
e48912
2012
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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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705737
Wang
Inhibition of WNT signaling by ...
Homo sapiens
Mol. Endocrinol.
23
1455-1465
2009
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1
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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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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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689035
Loniewski
Toll-like receptors differenti ...
Mus musculus, Mus musculus C57BL/6
Mol. Immunol.
45
2312-2322
2008
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1
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4
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4
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1
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4
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491136
Sallese
Two isoforms of G protein-coup ...
Homo sapiens
Biochem. Biophys. Res. Commun.
199
848-854
1994
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491154
Premont
Identification, purification, ...
Bos taurus
J. Biol. Chem.
269
6832-6841
1994
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9
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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.
269
27791-27794
1994
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491143
Kunapuli
Cloning and expression of GRK5 ...
Homo sapiens
Proc. Natl. Acad. Sci. USA
90
5588-5592
1993
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1
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491156
Benovic
Molecular cloning and expressi ...
Homo sapiens
J. Biol. Chem.
268
19521-19527
1993
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1
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7
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2
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7
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2
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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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