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Literature summary for 2.7.11.15 extracted from
- Purification and characterization of beta-adrenergic receptor kinase (1991), Methods Enzymol., 200, 351-362.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| isoproterenol | requirement, beta-agonist, beta-adrenergic receptor as substrate | Bos taurus |  |
| additional information | partial agonists promote reduced receptor phosphorylation | Bos taurus | |
| additional information | not activated by polycations | Bos taurus |
General Stability
| General Stability | Organism |
|---|---|
| Triton X-100 stabilizes | Bos taurus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2,3-diphosphoglycerate | weak | Bos taurus | |
| Chloropromazine | IC50: 0.043 mM | Bos taurus | |
| D-sphingosine | IC50: 0.027 mM | Bos taurus | |
| Dextran sulfate | strong, IC50: 0.00015 mM with rhodopsin as substrate | Bos taurus | |
| Digitonin | IC50: 0.05 mM | Bos taurus | |
| heparin | most potent inhibitor to date | Bos taurus | |
| Inositol hexaphosphate | weak, IC50: 3.6 mM with rhodopsin as substrate | Bos taurus | |
| Inositol hexasulfate | good inhibitor; IC50: 0.0135 mM with rhodopsin as substrate | Bos taurus | |
| NaCl | 0.1 M, 90% inhibition | Bos taurus | |
| Polyaspartic acid | good inhibitor; IC50: 0.0013 mM with rhodopsin as substrate | Bos taurus | |
| Polyglutamic acid | good inhibitor | Bos taurus | |
| polylysine | IC50: 0.069 mM with rhodopsin as substrate | Bos taurus | |
| Protein kinase C inhibitor H7 | IC50: 0.25 mM; weak | Bos taurus | |
| pyridoxal 5'-phosphate | weak, IC50: 0.9 mM with rhodopsin as substrate | Bos taurus | |
| Sangivamycin | IC50: 0.067 mM | Bos taurus | |
| spermine | IC50: 1.6 mM; weak, less potent than polylysine | Bos taurus | |
| tamoxifen | IC50: 0.04 mM | Bos taurus | |
| Trifluoperazine | IC50: 0.035 mM | Bos taurus | |
| Triton X-100 | IC50: 0.054 mM | Bos taurus | |
| Tween 20 | IC50: 0.027 mM | Bos taurus | |
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 | 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 | - |
? | |
| additional information | Bos taurus | beta-ARK is probably a general adenylate cyclase-coupled receptor kinase | ? | - |
? | |
| additional information | Bos taurus | phosphorylates and regulates receptors coupled to either stimulation or inhibition of adenylate cyclase | ? | - |
? | |
Organic Solvent Stability
| Organic Solvent | Comment | Organism |
|---|---|---|
| Triton X-100 | stabilizes | Bos taurus |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Bos taurus | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| about 20000fold, from brain | Bos taurus |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | cerebral cortex | Bos taurus | - |
| cerebral cortex | - |
Bos taurus | - |
| additional information | ubiquitous enzyme | Bos taurus | - |
Storage Stability
| Storage Stability | Organism |
|---|---|
| 4°C, in presence of Triton X-100, 1 year, stable | Bos taurus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + alpha2-adrenergic receptor | from human platelets | Bos taurus | ADP + phospho-alpha2-adrenergic receptor | - |
? | |
| ATP + beta-adrenergic receptor | phosphorylation sites are located mainly at the C-terminal tail of the receptor | Bos taurus | ADP + phospho-beta-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 | beta-AR from hamster lung | 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 + muscarinic cholinergic receptor | from chick heart | Bos taurus | ADP + phospho-muscarinic cholinergic 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 | domain structure | Bos taurus | ? | - |
? | |
| additional information | beta-ARK is probably a general adenylate cyclase-coupled receptor kinase | Bos taurus | ? | - |
? | |
| additional information | phosphorylates and regulates receptors coupled to either stimulation or inhibition of adenylate cyclase | 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 |
|---|---|---|---|
| 7.5 | - |
assay at | Bos taurus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Bos taurus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 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 | |
| 0.0135 | - |
IC50: 0.0135 mM with rhodopsin as substrate | Bos taurus | Inositol hexasulfate | |
| 0.027 | - |
IC50: 0.027 mM | Bos taurus | Tween 20 | |
| 0.027 | - |
IC50: 0.027 mM | Bos taurus | D-sphingosine | |
| 0.035 | - |
IC50: 0.035 mM | Bos taurus | Trifluoperazine | |
| 0.04 | - |
IC50: 0.04 mM | Bos taurus | tamoxifen | |
| 0.043 | - |
IC50: 0.043 mM | Bos taurus | Chloropromazine | |
| 0.05 | - |
IC50: 0.05 mM | Bos taurus | Digitonin | |
| 0.054 | - |
IC50: 0.054 mM | Bos taurus | Triton X-100 | |
| 0.067 | - |
IC50: 0.067 mM | Bos taurus | Sangivamycin | |
| 0.069 | - |
IC50: 0.069 mM with rhodopsin as substrate | Bos taurus | polylysine | |
| 0.25 | - |
IC50: 0.25 mM | Bos taurus | Protein kinase C inhibitor H7 | |
| 0.9 | - |
weak, IC50: 0.9 mM with rhodopsin as substrate | Bos taurus | pyridoxal 5'-phosphate | |
| 1.6 | - |
IC50: 1.6 mM | Bos taurus | spermine | |
| 3.6 | - |
weak, IC50: 3.6 mM with rhodopsin as substrate | Bos taurus | Inositol hexaphosphate | |
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