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Literature summary extracted from

  • Kim, C.M.; Dion, S.B.; Onorato, J.J.; Benovic, J.L.
    Expression and characterization of two beta-adrenergic receptor kinase isoforms using the baculovirus expression system (1993), Receptor, 3, 39-55.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.15 G protein betagamma-subunit 10fold activation, beta-ARK 1 and 2, increases incorporation of phosphate from 4 to 10 mol phosphate/mol receptor Bos taurus
2.7.11.15 G protein Gbetagamma subunits activate both ARK1 and ARK2 about 2.5fold Bos taurus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.15 beta-ARK 1 and 2 are cloned and expressed in SF9 cells using the baculovirus expression system Bos taurus
2.7.11.15 overexpression of ARK1 and ARK2 in Spodoptera frugiperda Sf9 cells using the baculovirus infection system Bos taurus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.15 heparin beta-ARK 1: IC50 is 0.0014 mM, beta-ARK 2: IC50 is 0.0011 mM; inhibits both isozymes ARK1 and ARK2 potently with IC50 of 0.0014 mM and 0.0011 mM, respectively; most potent inhibitor to date Bos taurus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.11.15 additional information
-
 additional information kinetics of isozymes ARK1 and ARK2 Bos taurus
2.7.11.15 0.014
-
 rhodopsin beta-ARK 1 and 2 Bos taurus
2.7.11.15 0.014
-
 rhodopsin isozymes ARK1 and ARK2 Bos taurus
2.7.11.15 0.06 0.09 ATP MgATP2-, beta-ARK 1 and 2 Bos taurus
2.7.11.15 0.06 0.09 ATP isozymes ARK1 and ARK2 Bos taurus
2.7.11.15 0.06 0.09 ATP ATP in form of MgATP2- 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+ as MgATP2- 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 beta-ARK 1 and 2 may have a similar substrate specificity 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 agonist-activated receptor substrate ADP + phosphorylated beta-adrenergic receptor
-
 ?
2.7.11.15 ATP + rhodopsin Bos taurus light-activated rhodopsin ADP + phosphorylated rhodopsin
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.15 Bos taurus
-
 enzyme exists in 2 subtypes: beta-ARK 1 and beta-ARK 2
-
2.7.11.15 Bos taurus
-
 2 isozymes betaARK1 and betaARK2
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.15 recombinant ARK1 and ARK2 from Sf9 insect cells by sequential chromatography, including heparin affinity chromatography Bos taurus
2.7.11.15 recombinant beta-ARK 1 and 2 overexpressed in Sf9 cells Bos taurus

Reaction

EC Number Reaction Comment Organism Reaction ID
2.7.11.15 ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor] sequential mechanism Bos taurus
a

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 similar rates of beta-ARK 1 and 2 for beta2-adrenergic receptor phosphorylation Bos taurus ADP + phospho-beta-adrenergic receptor
-
 ?
2.7.11.15 ATP + beta-adrenergic receptor beta-ARK 1 and 2 may have a similar substrate specificity 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 agonist-activated receptor substrate Bos taurus ADP + phosphorylated beta-adrenergic receptor
-
 ?
2.7.11.15 ATP + peptide beta-ARK 1 and 2 prefer peptide substrates with acidic amino acids N-terminal to a Ser-residue Bos taurus ADP + phosphopeptide
-
 ?
2.7.11.15 ATP + peptide synthetic Bos taurus ADP + phosphopeptide
-
 ?
2.7.11.15 ATP + rhodopsin light-activated rhodopsin Bos taurus ADP + phosphorylated rhodopsin
-
 ?
2.7.11.15 ATP + rhodopsin light-activated rhodopsin, both isozymes ARK1 and ARK2 prefer acidic amino acids N-terminal to a serine for phosphorylation Bos taurus ADP + phosphorylated rhodopsin
-
 ?
2.7.11.15 ATP + rhodopsin light-dependent, actual substrate: light-bleached rhodopsin Bos taurus ADP + phosphorhodopsin
-
 ?
2.7.11.15 ATP + [beta-adrenergic receptor]
-
 Bos taurus ADP + phospho-[beta-adrenergic receptor]
-
 ?
2.7.11.15 additional information peptide phosphorylation study Bos taurus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.15 beta-adrenergic receptor kinase
-
 Bos taurus
2.7.11.15 betaARK1
-
 Bos taurus
2.7.11.15 betaARK2
-
 Bos taurus
2.7.11.15 More the enzymes belong to the family of G protein-coupled receptor kinases Bos taurus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.15 ATP
-
 Bos taurus
2.7.11.15 ATP as MgATP2- Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.15 0.0011
-
 beta-ARK 1: IC50 is 0.0014 mM, beta-ARK 2: IC50 is 0.0011 mM Bos taurus heparin
2.7.11.15 0.0014
-
 inhibits both isozymes ARK1 and ARK2 potently with IC50 of 0.0014 mM and 0.0011 mM, respectively Bos taurus heparin