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Literature summary for 2.7.11.15 extracted from

  • Benovic, J.L.; Mayor, F.; Staniczewski, C.; Lefkowitz, R.J.; Caron, M.G.
    Purification and characterization of the beta-adrenergic receptor kinase (1987), J. Biol. Chem., 262, 9026-9032.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
isoproterenol requirement, beta-agonist, beta-adrenergic receptor as substrate Bos taurus
additional information not effected by Ca2+ or Co2+ Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
Digitonin 0.05-0.1%, 93-95% inhibition Bos taurus
additional information not affected by Ca2+ or Co2+ Bos taurus
NaCl 20 mM, 48% inhibition, as efficient as F-, I-, NO2- or acetate, less efficient than citrate, phosphate or sulfate Bos taurus
NaF as efficient as Cl-, I-, NO2- or acetate, less efficient than citrate, phosphate or sulfate Bos taurus
NaI as efficient as Cl-, F-, NO2- or acetate, less efficient than citrate, phosphate or sulfate Bos taurus
NaNO2 as efficient as Cl-, I-, F- or acetate, less efficient than citrate, phosphate or sulfate Bos taurus
Sodium acetate as efficient as Cl-, I-, NO2- or F-, less efficient than citrate, phosphate or sulfate Bos taurus
Sodium citrate 20 mM, 97% inhibition, more efficient than phosphate, sulfate, Cl-, F-, I-, NO2- or acetate Bos taurus
Sodium phosphate 20 mM, 76% inhibition, less efficient than citrate, as good as sulfate, more efficient than Cl-, F-, I-, NO2- or acetate Bos taurus
Sodium sulfate less efficient than citrate, as good as phosphate, more efficient than Cl-, F-, I-, NO2- or acetate Bos taurus
Zn2+ 0.1-0.2 mM ZnCl2, 94-98% inhibition Bos taurus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00025
-
beta-adrenergic receptor pH 7.5, 30°C Bos taurus
0.006
-
rhodopsin pH 7.5, 30°C Bos taurus
0.033
-
ATP pH 7.5, 30°C, beta-adrenergic receptor as substrate Bos taurus
0.037
-
ATP pH 7.5, 30°C, rhodopsin as substrate Bos taurus

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Bos taurus 5829
-
plasma membrane beta-AR may serve as membrane anchor for enzyme, translocation of beta-ARK from the cytosol to the plasma membrane Bos taurus 5886
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ requirement Bos taurus
Mg2+ optimal concentration: 2-6 mM Bos taurus
Mn2+ requirement, can replace Mg2+ with 50% efficiency, optimal concentration: 1-3 mM Bos taurus
additional information not activated by Ca2+, Co2+ or Zn2+ Bos taurus

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
80000
-
gel filtration Bos taurus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein enzyme appears to autophosphorylate Bos taurus

Purification (Commentary)

Purification (Comment) Organism
20300fold, to near homogeneity Bos taurus

Source Tissue

Source Tissue Comment Organism Textmining
brain cerebral cortex Bos taurus
-
brain highest beta-ARK activity in cerebral cortex Bos taurus
-
cerebral cortex highest beta-ARK activity Bos taurus
-
additional information tissue distribution Bos taurus
-
additional information ubiquitous enzyme Bos taurus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.00873
-
pH 7.5, 30°C Bos taurus

Storage Stability

Storage Stability Organism
4°C, crude enzyme: several months, stable, purified enzyme: t1/2 of 5-10 days Bos taurus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + beta-adrenergic receptor incorporation of about 9 mol phosphate/mol receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor specifically phosphorylates the agonist-occupied form of the receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor beta-AR from hamster lung Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor beta-AR is a much better substrate than rhodopsin Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor agonist-occupied form of the receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor involved in homologous desensitization of beta-adrenergic receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
?
ATP + rhodopsin beta-AR is a much better substrate than rhodopsin Bos taurus ADP + phosphorhodopsin
-
?
ATP + rhodopsin light-dependent, actual substrate: light-bleached rhodopsin Bos taurus ADP + phosphorhodopsin
-
?
ATP + rhodopsin incorporation of 0.15 mol phosphate/mol rhodopsin Bos taurus ADP + phosphorhodopsin
-
?
ATP + rhodopsin in form of bovine rod outer segments Bos taurus ADP + phosphorhodopsin
-
?
GTP + beta-adrenergic receptor agonist-occupied form of beta-AR from hamster lung, GTP can substitute ATP, 2% as effective as ATP Bos taurus GDP + phospho-beta-adrenergic receptor
-
?

Subunits

Subunits Comment Organism
monomer 1 * 80000, SDS-PAGE Bos taurus

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6 7.5
-
Bos taurus
7.5
-
assay at Bos taurus

Cofactor

Cofactor Comment Organism Structure
ATP requirement Bos taurus