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Literature summary extracted from

  • Benovic, J.L.; Stone, W.C.; Caron, M.G.; Lefkowitz, R.J.
    Inhibition of the beta-adrenergic receptor kinase by polyanions (1989), J. Biol. Chem., 264, 6707-6710.
    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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.15 2,3-diphosphoglycerate inhibits in the millimolar range, IC50: 1.1 mM with rhodopsin as substrate; weak Bos taurus
2.7.11.15 chondroitin sulfate B weak Bos taurus
2.7.11.15 chondroitin sulfate C less inhibitory than heparin Bos taurus
2.7.11.15 D-glucosamine 2,6-disulfate inhibits in the millimolar range, weak, IC50: 7.3 mM with rhodopsin as substrate Bos taurus
2.7.11.15 Dextran sulfate strong, IC50: 0.00015 mM with rhodopsin as substrate Bos taurus
2.7.11.15 heparan sulfate less inhibitory than heparin Bos taurus
2.7.11.15 heparin de-N-sulfated heparin is 8fold less effective; most potent inhibitor to date; polylysine, spermine or spermidine at lower concentrations partially reverses; strong, kinetics, IC50: 0.00003 mM with beta-AR as substrate, 0.00015 mM with rhodopsin as substrate 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 270fold more potent than inositol hexaphosphate; IC50: 0.0135 mM with rhodopsin as substrate Bos taurus
2.7.11.15 Polyaspartic acid IC50: 0.0013 mM with rhodopsin as substrate Bos taurus
2.7.11.15 Polyglutamic acid IC50: 0.002 mM with rhodopsin as substrate Bos taurus
2.7.11.15 polylysine IC50: 0.069 mM with rhodopsin as substrate; weak, more potent than spermine and spermidine Bos taurus
2.7.11.15 pyridoxal 5'-phosphate inhibits in the millimolar range; weak, IC50: 0.9 mM with rhodopsin as substrate Bos taurus
2.7.11.15 spermidine weak, less potent than polylysine Bos taurus
2.7.11.15 spermine weak, less potent than polylysine Bos taurus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.11.15 0.0053
-
 rhodopsin pH 7.4, 30°C, in absence of heparin Bos taurus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.15 cytosol
-
 Bos taurus 5829
-

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 regulation of the beta-AR function in vivo ADP + phospho-beta-adrenergic receptor
-
 ?
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
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.15
-
 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
-

Storage Stability

EC Number Storage Stability Organism
2.7.11.15 4°C, several months, 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
-
 Bos taurus ADP + phospho-alpha2-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 regulation of the beta-AR function in vivo 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 + 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 very poor substrates: casein, phosvitin 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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.15 0.00003
-
 strong, kinetics, IC50: 0.00003 mM with beta-AR as substrate, 0.00015 mM with rhodopsin as substrate Bos taurus heparin
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 0.002
-
 IC50: 0.002 mM with rhodopsin as substrate Bos taurus Polyglutamic acid
2.7.11.15 0.0135
-
 IC50: 0.0135 mM with rhodopsin as substrate Bos taurus Inositol hexasulfate
2.7.11.15 0.069
-
 IC50: 0.069 mM with rhodopsin as substrate Bos taurus polylysine
2.7.11.15 0.9
-
 weak, IC50: 0.9 mM with rhodopsin as substrate Bos taurus pyridoxal 5'-phosphate
2.7.11.15 1.1
-
 inhibits in the millimolar range, IC50: 1.1 mM with rhodopsin as substrate Bos taurus 2,3-diphosphoglycerate
2.7.11.15 3.6
-
 weak, IC50: 3.6 mM with rhodopsin as substrate Bos taurus Inositol hexaphosphate
2.7.11.15 7.3
-
 inhibits in the millimolar range, weak, IC50: 7.3 mM with rhodopsin as substrate Bos taurus D-glucosamine 2,6-disulfate