BRENDA - Enzyme Database

The beta-adrenergic receptor kinase (GRK2) is regulated by phospholipids

Onorato, J.J.; Gillis, M.E.; Liu, Y.; Benovic, J.L.; Ruoho, A.E.; J. Biol. Chem. 270, 21346-21353 (1995)

Data extracted from this reference:

Activating Compound
EC Number
Activating Compound
Commentary
Organism
Structure
2.7.11.15
beta2-adrenergic receptor
interaction of beta-ARK 1 with the agonist-occupied receptor activates
Bos taurus
2.7.11.15
cardiolipin
activates, phosphorylation of beta2-AR
Bos taurus
2.7.11.15
G protein betagamma-subunit
-
Bos taurus
2.7.11.15
isoproterenol
stimulates
Bos taurus
2.7.11.15
phosphatidic acid
activates, phosphorylation of beta2-AR
Bos taurus
2.7.11.15
phosphatidylglycerol
activates, phosphorylation of beta2-AR
Bos taurus
2.7.11.15
phosphatidylinositol
activates, phosphorylation of beta2-AR, 6fold activation of phosphorylation of RRREEEEESAAA
Bos taurus
2.7.11.15
phosphatidylserine
activates, phosphorylation of beta2-AR
Bos taurus
2.7.11.15
Phospholipid
required for phosphorylation of beta2-AR, activation is associated with a conformational change in beta-ARK 1, acidic phospholipid specificity, not activated by phosphatidylinositol 4,5-diphosphate, direct regulation of beta-ARK 1 activity by phospholipids
Bos taurus
Cloned(Commentary)
EC Number
Commentary
Organism
2.7.11.15
beta-ARK 1 is cloned and expressed in SF9 cells using the baculovirus expression system
Bos taurus
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
2.7.11.15
heparin
potent inhibitor of beta-ARK 1
Bos taurus
2.7.11.15
phosphatidylinositol 4,5-bisphosphate
inhibits receptor phosphorylation, causes membrane association, 30% inhibition of phosphorylation of RRREEEEESAAA
Bos taurus
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.7.11.15
1.34
-
RRREEEEESAAA
pH 7.4, 30°C, recombinant beta-ARK 1
Bos taurus
Molecular Weight [Da]
EC Number
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
Organism
2.7.11.15
80000
-
Western blot analysis
Bos taurus
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.7.11.15
ATP + beta-adrenergic receptor
Bos taurus
agonist-occupied form of the receptor
ADP + phospho-beta-adrenergic receptor
-
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
Bos taurus
involved in homologous desensitization of beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
Bos taurus
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.7.11.15
Bos taurus
-
beta-ARK 1
-
Posttranslational Modification
EC Number
Posttranslational Modification
Commentary
Organism
2.7.11.15
additional information
no autophosphorylation of beta-ARK 1
Bos taurus
Purification (Commentary)
EC Number
Commentary
Organism
2.7.11.15
recombinant beta-ARK 1 expressed in Sf9 cells
Bos taurus
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.7.11.15
ATP + beta-adrenergic receptor
beta2-adrenergic receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
specifically phosphorylates the agonist-occupied form of the receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
incorporation of up to 5 mol phosphate/mol receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
beta-AR from hamster lung
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
agonist-occupied form of the receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
involved in homologous desensitization of beta-adrenergic receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + RRREEEEESAAA
nonreceptor peptide substrate
645028
Bos taurus
?
-
-
-
?
Temperature Optimum [°C]
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
2.7.11.15
30
-
assay at
Bos taurus
pH Optimum
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
2.7.11.15
7.4
-
assay at
Bos taurus
Cofactor
EC Number
Cofactor
Commentary
Organism
Structure
2.7.11.15
ATP
-
Bos taurus
Activating Compound (protein specific)
EC Number
Activating Compound
Commentary
Organism
Structure
2.7.11.15
beta2-adrenergic receptor
interaction of beta-ARK 1 with the agonist-occupied receptor activates
Bos taurus
2.7.11.15
cardiolipin
activates, phosphorylation of beta2-AR
Bos taurus
2.7.11.15
G protein betagamma-subunit
-
Bos taurus
2.7.11.15
isoproterenol
stimulates
Bos taurus
2.7.11.15
phosphatidic acid
activates, phosphorylation of beta2-AR
Bos taurus
2.7.11.15
phosphatidylglycerol
activates, phosphorylation of beta2-AR
Bos taurus
2.7.11.15
phosphatidylinositol
activates, phosphorylation of beta2-AR, 6fold activation of phosphorylation of RRREEEEESAAA
Bos taurus
2.7.11.15
phosphatidylserine
activates, phosphorylation of beta2-AR
Bos taurus
2.7.11.15
Phospholipid
required for phosphorylation of beta2-AR, activation is associated with a conformational change in beta-ARK 1, acidic phospholipid specificity, not activated by phosphatidylinositol 4,5-diphosphate, direct regulation of beta-ARK 1 activity by phospholipids
Bos taurus
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
2.7.11.15
beta-ARK 1 is cloned and expressed in SF9 cells using the baculovirus expression system
Bos taurus
Cofactor (protein specific)
EC Number
Cofactor
Commentary
Organism
Structure
2.7.11.15
ATP
-
Bos taurus
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
2.7.11.15
heparin
potent inhibitor of beta-ARK 1
Bos taurus
2.7.11.15
phosphatidylinositol 4,5-bisphosphate
inhibits receptor phosphorylation, causes membrane association, 30% inhibition of phosphorylation of RRREEEEESAAA
Bos taurus
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.7.11.15
1.34
-
RRREEEEESAAA
pH 7.4, 30°C, recombinant beta-ARK 1
Bos taurus
Molecular Weight [Da] (protein specific)
EC Number
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
Organism
2.7.11.15
80000
-
Western blot analysis
Bos taurus
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.7.11.15
ATP + beta-adrenergic receptor
Bos taurus
agonist-occupied form of the receptor
ADP + phospho-beta-adrenergic receptor
-
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
Bos taurus
involved in homologous desensitization of beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
Bos taurus
?
Posttranslational Modification (protein specific)
EC Number
Posttranslational Modification
Commentary
Organism
2.7.11.15
additional information
no autophosphorylation of beta-ARK 1
Bos taurus
Purification (Commentary) (protein specific)
EC Number
Commentary
Organism
2.7.11.15
recombinant beta-ARK 1 expressed in Sf9 cells
Bos taurus
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.7.11.15
ATP + beta-adrenergic receptor
beta2-adrenergic receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
specifically phosphorylates the agonist-occupied form of the receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
incorporation of up to 5 mol phosphate/mol receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
beta-AR from hamster lung
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
agonist-occupied form of the receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + beta-adrenergic receptor
involved in homologous desensitization of beta-adrenergic receptor
645028
Bos taurus
ADP + phospho-beta-adrenergic receptor
-
645028
Bos taurus
?
2.7.11.15
ATP + RRREEEEESAAA
nonreceptor peptide substrate
645028
Bos taurus
?
-
-
-
?
Temperature Optimum [°C] (protein specific)
EC Number
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
2.7.11.15
30
-
assay at
Bos taurus
pH Optimum (protein specific)
EC Number
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
2.7.11.15
7.4
-
assay at
Bos taurus