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Literature summary extracted from

  • Onorato, J.J.; Gillis, M.E.; Liu, Y.; Benovic, J.L.; Ruoho, A.E.
    The beta-adrenergic receptor kinase (GRK2) is regulated by phospholipids (1995), J. Biol. Chem., 270, 21346-21353.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment 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 Cloned (Comment) 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 Comment 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 Comment 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] Comment Organism
2.7.11.15 80000
-
Western blot analysis Bos taurus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.15 ATP + beta-adrenergic receptor Bos taurus agonist-occupied form of the receptor ADP + phospho-beta-adrenergic receptor
-
?
2.7.11.15 ATP + beta-adrenergic receptor Bos taurus involved in homologous desensitization of beta-adrenergic receptor ADP + phospho-beta-adrenergic receptor
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.15 Bos taurus
-
beta-ARK 1
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.15 additional information no autophosphorylation of beta-ARK 1 Bos taurus

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.15 recombinant beta-ARK 1 expressed in Sf9 cells Bos taurus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.15 ATP + beta-adrenergic receptor beta2-adrenergic receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
2.7.11.15 ATP + beta-adrenergic receptor specifically phosphorylates the agonist-occupied form of the receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
2.7.11.15 ATP + beta-adrenergic receptor incorporation of up to 5 mol phosphate/mol receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
2.7.11.15 ATP + beta-adrenergic receptor beta-AR from hamster lung Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
2.7.11.15 ATP + beta-adrenergic receptor agonist-occupied form of the receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
2.7.11.15 ATP + beta-adrenergic receptor involved in homologous desensitization of beta-adrenergic receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
2.7.11.15 ATP + RRREEEEESAAA nonreceptor peptide substrate Bos taurus ?
-
?

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.15 30
-
assay at Bos taurus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.15 7.4
-
assay at Bos taurus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.15 ATP
-
Bos taurus