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Literature summary for 2.7.11.15 extracted from
- Inhibition of the beta-adrenergic receptor kinase by polyanions (1989), J. Biol. Chem., 264, 6707-6710.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| isoproterenol | requirement, beta-agonist, beta-adrenergic receptor as substrate | Bos taurus |  |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2,3-diphosphoglycerate | inhibits in the millimolar range, IC50: 1.1 mM with rhodopsin as substrate; weak | Bos taurus | |
| chondroitin sulfate B | weak | Bos taurus | |
| chondroitin sulfate C | less inhibitory than heparin | Bos taurus | |
| D-glucosamine 2,6-disulfate | inhibits in the millimolar range, weak, IC50: 7.3 mM with rhodopsin as substrate | Bos taurus | |
| Dextran sulfate | strong, IC50: 0.00015 mM with rhodopsin as substrate | Bos taurus | |
| heparan sulfate | less inhibitory than heparin | Bos taurus | |
| 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 | |
| Inositol hexaphosphate | weak, IC50: 3.6 mM with rhodopsin as substrate | Bos taurus | |
| Inositol hexasulfate | 270fold more potent than inositol hexaphosphate; IC50: 0.0135 mM with rhodopsin as substrate | Bos taurus | |
| Polyaspartic acid | IC50: 0.0013 mM with rhodopsin as substrate | Bos taurus | |
| Polyglutamic acid | IC50: 0.002 mM with rhodopsin as substrate | Bos taurus | |
| polylysine | IC50: 0.069 mM with rhodopsin as substrate; weak, more potent than spermine and spermidine | Bos taurus | |
| pyridoxal 5'-phosphate | inhibits in the millimolar range; weak, IC50: 0.9 mM with rhodopsin as substrate | Bos taurus | |
| spermidine | weak, less potent than polylysine | Bos taurus | |
| spermine | weak, less potent than polylysine | Bos taurus | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0053 | - |
rhodopsin | pH 7.4, 30°C, in absence of heparin | Bos taurus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Bos taurus | 5829 | - |
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 | regulation of the beta-AR function 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 | 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 | - |
Storage Stability
| Storage Stability | Organism |
|---|---|
| 4°C, several months, stable | 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 | regulation of the beta-AR function 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 | involved in homologous desensitization of beta-adrenergic receptor | Bos taurus | ADP + phospho-beta-adrenergic receptor | - |
? | |
| ATP + rhodopsin | light-dependent, actual substrate: light-bleached rhodopsin | Bos taurus | ADP + phosphorhodopsin | - |
? | |
| ATP + rhodopsin | in form of bovine rod outer segments | Bos taurus | ADP + phosphorhodopsin | - |
? | |
| additional information | very poor substrates: casein, phosvitin | Bos taurus | ? | - |
? | |
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 |
|---|---|---|---|
| 7.4 | - |
assay at | Bos taurus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Bos taurus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00003 | - |
strong, kinetics, IC50: 0.00003 mM with beta-AR as substrate, 0.00015 mM with rhodopsin as substrate | Bos taurus | heparin | |
| 0.00015 | - |
strong, IC50: 0.00015 mM with rhodopsin as substrate | Bos taurus | Dextran sulfate | |
| 0.0013 | - |
IC50: 0.0013 mM with rhodopsin as substrate | Bos taurus | Polyaspartic acid | |
| 0.002 | - |
IC50: 0.002 mM with rhodopsin as substrate | Bos taurus | Polyglutamic acid | |
| 0.0135 | - |
IC50: 0.0135 mM with rhodopsin as substrate | Bos taurus | Inositol hexasulfate | |
| 0.069 | - |
IC50: 0.069 mM with rhodopsin as substrate | Bos taurus | polylysine | |
| 0.9 | - |
weak, IC50: 0.9 mM with rhodopsin as substrate | Bos taurus | pyridoxal 5'-phosphate | |
| 1.1 | - |
inhibits in the millimolar range, IC50: 1.1 mM with rhodopsin as substrate | Bos taurus | 2,3-diphosphoglycerate | |
| 3.6 | - |
weak, IC50: 3.6 mM with rhodopsin as substrate | Bos taurus | Inositol hexaphosphate | |
| 7.3 | - |
inhibits in the millimolar range, weak, IC50: 7.3 mM with rhodopsin as substrate | Bos taurus | D-glucosamine 2,6-disulfate | |
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