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Literature summary for 2.7.11.15 extracted from

  • Kwatra, M.M.; Benovic, J.L.; Caron, M.G.; Lefkowitz, R.J.; Hosey, M.M.
    Phosphorylation of chick heart muscarinic cholinergic receptors by the beta-adrenergic receptor kinase (1989), Biochemistry, 28, 4543-4547.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
Carbachol requirement, agonist, muscarinic cholinergic receptor as substrate Bos taurus
isoproterenol requirement, beta-agonist, beta-adrenergic receptor as substrate Bos taurus
additional information agonists induce specific conformational changes allowing phosphorylation Bos taurus
Oxytremorine requirement, agonist, muscarinic cholinergic receptor as substrate Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
atropine receptor antagonist Bos taurus
heparin 0.001 mM, complete inhibition of muscarinic cholinergic receptor phosphorylation Bos taurus
McN-A343 weak, partial antagonist Bos taurus

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ requirement 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
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Bos taurus

Source Tissue

Source Tissue Comment Organism Textmining
brain cerebral cortex Bos taurus
-
cerebral cortex
-
Bos taurus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.05 0.08 pH 7.5, 30°C Bos taurus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + alpha2-adrenergic receptor
-
Bos taurus ADP + phospho-alpha2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor beta2-adrenergic 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 at a similar rate as muscarinic cholinergic receptor 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 + muscarinic cholinergic receptor in vitro as good as beta-adrenergic receptor, phosphorylation depends on the presence of a muscarinic agonist ligand, not merely receptor occupancy, the agonist induces a conformational change, which allows phosphorylation, phosphorylation sites: 70% Ser- and 30% Thr-residues, incorporation of 3-4 mol phosphate/mol receptor Bos taurus ADP + phospho-muscarinic cholinergic receptor
-
?
ATP + muscarinic cholinergic receptor from chick heart Bos taurus ADP + phospho-muscarinic cholinergic receptor
-
?

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
7.5
-
assay at Bos taurus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Bos taurus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00015
-
heparin
-
Bos taurus