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Literature summary extracted from

  • Benovic, J.L.
    Purification and characterization of beta-adrenergic receptor kinase (1991), Methods Enzymol., 200, 351-362.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.15 isoproterenol requirement, beta-agonist, beta-adrenergic receptor as substrate Bos taurus
2.7.11.15 additional information partial agonists promote reduced receptor phosphorylation Bos taurus
2.7.11.15 additional information not activated by polycations Bos taurus

General Stability

EC Number General Stability Organism
2.7.11.15 Triton X-100 stabilizes Bos taurus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.15 2,3-diphosphoglycerate weak Bos taurus
2.7.11.15 Chloropromazine IC50: 0.043 mM Bos taurus
2.7.11.15 D-sphingosine IC50: 0.027 mM Bos taurus
2.7.11.15 Dextran sulfate strong, IC50: 0.00015 mM with rhodopsin as substrate Bos taurus
2.7.11.15 Digitonin IC50: 0.05 mM Bos taurus
2.7.11.15 heparin most potent inhibitor to date Bos taurus
2.7.11.15 Inositol hexaphosphate weak, IC50: 3.6 mM with rhodopsin as substrate Bos taurus
2.7.11.15 Inositol hexasulfate good inhibitor; IC50: 0.0135 mM with rhodopsin as substrate Bos taurus
2.7.11.15 NaCl 0.1 M, 90% inhibition Bos taurus
2.7.11.15 Polyaspartic acid good inhibitor; IC50: 0.0013 mM with rhodopsin as substrate Bos taurus
2.7.11.15 Polyglutamic acid good inhibitor Bos taurus
2.7.11.15 polylysine IC50: 0.069 mM with rhodopsin as substrate Bos taurus
2.7.11.15 Protein kinase C inhibitor H7 IC50: 0.25 mM; weak Bos taurus
2.7.11.15 pyridoxal 5'-phosphate weak, IC50: 0.9 mM with rhodopsin as substrate Bos taurus
2.7.11.15 Sangivamycin IC50: 0.067 mM Bos taurus
2.7.11.15 spermine IC50: 1.6 mM; weak, less potent than polylysine Bos taurus
2.7.11.15 tamoxifen IC50: 0.04 mM Bos taurus
2.7.11.15 Trifluoperazine IC50: 0.035 mM Bos taurus
2.7.11.15 Triton X-100 IC50: 0.054 mM Bos taurus
2.7.11.15 Tween 20 IC50: 0.027 mM Bos taurus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.15 Mg2+ requirement 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
-
 ?
2.7.11.15 additional information Bos taurus beta-ARK is probably a general adenylate cyclase-coupled receptor kinase ?
-
 ?
2.7.11.15 additional information Bos taurus phosphorylates and regulates receptors coupled to either stimulation or inhibition of adenylate cyclase ?
-
 ?

Organic Solvent Stability

EC Number Organic Solvent Comment Organism
2.7.11.15 Triton X-100 stabilizes Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.15 Bos taurus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.15 about 20000fold, from brain Bos taurus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.15 brain cerebral cortex Bos taurus
-
2.7.11.15 cerebral cortex
-
 Bos taurus
-
2.7.11.15 additional information ubiquitous enzyme Bos taurus
-

Storage Stability

EC Number Storage Stability Organism
2.7.11.15 4°C, in presence of Triton X-100, 1 year, stable Bos taurus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.15 ATP + alpha2-adrenergic receptor from human platelets Bos taurus ADP + phospho-alpha2-adrenergic receptor
-
 ?
2.7.11.15 ATP + beta-adrenergic receptor phosphorylation sites are located mainly at the C-terminal tail of the receptor Bos taurus ADP + phospho-beta-adrenergic receptor
-
 ?
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 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 + muscarinic cholinergic receptor from chick heart Bos taurus ADP + phospho-muscarinic cholinergic receptor
-
 ?
2.7.11.15 ATP + rhodopsin light-dependent, actual substrate: light-bleached rhodopsin Bos taurus ADP + phosphorhodopsin
-
 ?
2.7.11.15 ATP + rhodopsin in form of bovine rod outer segments Bos taurus ADP + phosphorhodopsin
-
 ?
2.7.11.15 additional information domain structure Bos taurus ?
-
 ?
2.7.11.15 additional information beta-ARK is probably a general adenylate cyclase-coupled receptor kinase Bos taurus ?
-
 ?
2.7.11.15 additional information phosphorylates and regulates receptors coupled to either stimulation or inhibition of adenylate cyclase 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 7.5
-
 assay at Bos taurus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.15 ATP
-
 Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.15 0.00015
-
 strong, IC50: 0.00015 mM with rhodopsin as substrate Bos taurus Dextran sulfate
2.7.11.15 0.0013
-
 IC50: 0.0013 mM with rhodopsin as substrate Bos taurus Polyaspartic acid
2.7.11.15 0.0135
-
 IC50: 0.0135 mM with rhodopsin as substrate Bos taurus Inositol hexasulfate
2.7.11.15 0.027
-
 IC50: 0.027 mM Bos taurus Tween 20
2.7.11.15 0.027
-
 IC50: 0.027 mM Bos taurus D-sphingosine
2.7.11.15 0.035
-
 IC50: 0.035 mM Bos taurus Trifluoperazine
2.7.11.15 0.04
-
 IC50: 0.04 mM Bos taurus tamoxifen
2.7.11.15 0.043
-
 IC50: 0.043 mM Bos taurus Chloropromazine
2.7.11.15 0.05
-
 IC50: 0.05 mM Bos taurus Digitonin
2.7.11.15 0.054
-
 IC50: 0.054 mM Bos taurus Triton X-100
2.7.11.15 0.067
-
 IC50: 0.067 mM Bos taurus Sangivamycin
2.7.11.15 0.069
-
 IC50: 0.069 mM with rhodopsin as substrate Bos taurus polylysine
2.7.11.15 0.25
-
 IC50: 0.25 mM Bos taurus Protein kinase C inhibitor H7
2.7.11.15 0.9
-
 weak, IC50: 0.9 mM with rhodopsin as substrate Bos taurus pyridoxal 5'-phosphate
2.7.11.15 1.6
-
 IC50: 1.6 mM Bos taurus spermine
2.7.11.15 3.6
-
 weak, IC50: 3.6 mM with rhodopsin as substrate Bos taurus Inositol hexaphosphate