Any feedback?
Literature summary for 2.7.11.15 extracted from
- Expression and characterization of two beta-adrenergic receptor kinase isoforms using the baculovirus expression system (1993), Receptor, 3, 39-55.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| 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 | |
| G protein Gbetagamma subunits | activate both ARK1 and ARK2 about 2.5fold | Bos taurus |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| beta-ARK 1 and 2 are cloned and expressed in SF9 cells using the baculovirus expression system | Bos taurus |
| overexpression of ARK1 and ARK2 in Spodoptera frugiperda Sf9 cells using the baculovirus infection system | Bos taurus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 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]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetics of isozymes ARK1 and ARK2 | Bos taurus | |
| 0.014 | - |
rhodopsin | beta-ARK 1 and 2 | Bos taurus | |
| 0.014 | - |
rhodopsin | isozymes ARK1 and ARK2 | Bos taurus | |
| 0.06 | 0.09 | ATP | MgATP2-, beta-ARK 1 and 2 | Bos taurus | |
| 0.06 | 0.09 | ATP | isozymes ARK1 and ARK2 | Bos taurus | |
| 0.06 | 0.09 | ATP | ATP in form of MgATP2- | Bos taurus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Bos taurus | 5829 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | as MgATP2- | 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 | beta-ARK 1 and 2 may have a similar substrate specificity in vivo | ADP + phospho-beta-adrenergic receptor | - |
? | |
| ATP + beta-adrenergic receptor | Bos taurus | agonist-occupied form of the receptor | ADP + phospho-beta-adrenergic receptor | - |
? | |
| ATP + beta-adrenergic receptor | Bos taurus | agonist-activated receptor substrate | ADP + phosphorylated beta-adrenergic receptor | - |
? | |
| ATP + rhodopsin | Bos taurus | light-activated rhodopsin | ADP + phosphorylated rhodopsin | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Bos taurus | - |
enzyme exists in 2 subtypes: beta-ARK 1 and beta-ARK 2 | - |
| Bos taurus | - |
2 isozymes betaARK1 and betaARK2 | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant ARK1 and ARK2 from Sf9 insect cells by sequential chromatography, including heparin affinity chromatography | Bos taurus |
| recombinant beta-ARK 1 and 2 overexpressed in Sf9 cells | Bos taurus |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor] | sequential mechanism | Bos taurus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 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 | similar rates of beta-ARK 1 and 2 for beta2-adrenergic receptor phosphorylation | Bos taurus | ADP + phospho-beta-adrenergic receptor | - |
? | |
| ATP + beta-adrenergic receptor | beta-ARK 1 and 2 may have a similar substrate specificity in vivo | 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 | agonist-activated receptor substrate | Bos taurus | ADP + phosphorylated beta-adrenergic receptor | - |
? | |
| ATP + peptide | beta-ARK 1 and 2 prefer peptide substrates with acidic amino acids N-terminal to a Ser-residue | Bos taurus | ADP + phosphopeptide | - |
? | |
| ATP + peptide | synthetic | Bos taurus | ADP + phosphopeptide | - |
? | |
| ATP + rhodopsin | light-activated rhodopsin | Bos taurus | ADP + phosphorylated rhodopsin | - |
? | |
| 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 | - |
? | |
| ATP + rhodopsin | light-dependent, actual substrate: light-bleached rhodopsin | Bos taurus | ADP + phosphorhodopsin | - |
? | |
| ATP + [beta-adrenergic receptor] | - |
Bos taurus | ADP + phospho-[beta-adrenergic receptor] | - |
? | |
| additional information | peptide phosphorylation study | Bos taurus | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| beta-adrenergic receptor kinase | - |
Bos taurus |
| betaARK1 | - |
Bos taurus |
| betaARK2 | - |
Bos taurus |
| More | the enzymes belong to the family of G protein-coupled receptor kinases | Bos taurus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Bos taurus | |
| ATP | as MgATP2- | Bos taurus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0011 | - |
beta-ARK 1: IC50 is 0.0014 mM, beta-ARK 2: IC50 is 0.0011 mM | Bos taurus | heparin | |
| 0.0014 | - |
inhibits both isozymes ARK1 and ARK2 potently with IC50 of 0.0014 mM and 0.0011 mM, respectively | Bos taurus | heparin | |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
