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Literature summary for 2.7.11.16 extracted from
- Endogenous G protein-coupled receptor kinase 6 triggers homologous beta-adrenergic receptor desensitization in primary uterine smooth muscle cells (2003), Endocrinology, 144, 3058-3066.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| transient overexpression of wild-types and dominant negative mutants of GRK5 and GRK6 in COS-7 cells | Rattus norvegicus |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| K215R | inactive dominant negative mutants of GRK5 or GRK6, overexpression of the GRK5 mutant in myometrial cells does not influence beta-adrenergic receptor sensitivity, while overexpression of GRK6 mutant leads to a 70% increase in isoproterenol-stimulated beta-adrenergic signaling via the beta-adrenergic receptor | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| heparin | GRK inhibitor | Rattus norvegicus |  |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Rattus norvegicus | the GRK4-6 family member enzymes mediate beta-adrenergic receptor desensitization, the beta-adrenergic receptor is stimulated by agonists such as isoproterenol, cholera toxin, or forskolin, and induces cAMP production | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Rattus norvegicus | - |
Sprague-Dawley rats | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| myometrium | primary cells | Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + rhodopsin | urea treated outer segments of rhodopsin | Rattus norvegicus | ADP + phosphorylated rhodopsin | - |
? | |
| additional information | the GRK4-6 family member enzymes mediate beta-adrenergic receptor desensitization, the beta-adrenergic receptor is stimulated by agonists such as isoproterenol, cholera toxin, or forskolin, and induces cAMP production | Rattus norvegicus | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| G protein-coupled receptor kinase 5 | - |
Rattus norvegicus |
| G protein-coupled receptor kinase 6 | - |
Rattus norvegicus |
| GRK5 | - |
Rattus norvegicus |
| GRK6 | - |
Rattus norvegicus |
| More | the enzyme belongs to the GRK4-6 family | Rattus norvegicus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Rattus norvegicus | |
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Release 2023.1 (January 2023)
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