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Literature summary for 2.7.11.14 extracted from
- Phosphorylation of GRK1 and GRK7 by cAMP-dependent protein kinase attenuates their enzymatic activities (2005), J. Biol. Chem., 280, 28241-28250.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| additional information | GRK1 and GRK7 are activated by autophosphorylation and by phosphorylation through cAMP-dependent protein kinase, EC 2.7.11.11 | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of FLAG-tagged wild-type and mutant GRK1 and GRK7 in HEK-293 cells | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| K219R | kinase inactive mutant of GRK1 | Homo sapiens |
| K220R | kinase inactive mutant of GRK7 | Homo sapiens |
| S21A | site-directed mutagenesis of GRK1 PKA phosphorylation site, the mutant shows 87% of wild-type enzyme activity | Homo sapiens |
| S21E | site-directed mutagenesis of GRK1 PKA phosphorylation site, the mutant shows 80% of wild-type enzyme activity | Homo sapiens |
| S23A | site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 67% of wild-type enzyme activity | Homo sapiens |
| S23A/S36A | site-directed mutagenesis of GRK7 PKA phosphorylation sites, the mutant shows 81% of wild-type enzyme activity | Homo sapiens |
| S23E | site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 67% of wild-type enzyme activity | Homo sapiens |
| S23E/S36E | site-directed mutagenesis of GRK7 PKA phosphorylation sites, the mutant shows 79% of wild-type enzyme activity | Homo sapiens |
| S333A | site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme | Homo sapiens |
| S36A | site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 76% of wild-type enzyme activity | Homo sapiens |
| S36E | site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 77% of wild-type enzyme activity | Homo sapiens |
| S441A | site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme | Homo sapiens |
| S490A | site-directed mutagenesis of GRK7, the mutant is unable to autophosphorylate | Homo sapiens |
| S490E | site-directed mutagenesis of GRK7, the mutant is unable to autophosphorylate | Homo sapiens |
| T353A | site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetics | Homo sapiens | |
| 0.0019 | - |
rhodopsin | recombinant wild-type GRK7, pH 7.0, 30°C | Homo sapiens |  |
| 0.0035 | - |
rhodopsin | recombinant wild-type GRK1, pH 7.0, 30°C | Homo sapiens | |
| 0.0106 | - |
ATP | recombinant wild-type GRK1, pH 7.0, 30°C | Homo sapiens | |
| 0.0214 | - |
ATP | recombinant wild-type GRK7, pH 7.0, 30°C | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| photoreceptor outer segment membrane | - |
Homo sapiens | 42622 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 62200 | - |
x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE | Homo sapiens |
| 63500 | - |
x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + rhodopsin | Homo sapiens | GRK1 and GRK7 | ADP + phosphorhodopsin | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| phosphoprotein | GRK1 and GRK7 perform autophosphorylations, GRK7 at Ser490 and GRK1 at Ser488/Thr489, and are phosphorylated in vivo in forskolin-stimulated cells by cAMP-dependent protein kinase, PKA, EC 2.7.11.11, in the dark, when cAMP levels are elevated, PKA phosphorylation of GRK1 at Ser21 and of GRK7 at Ser23 and Ser36, no phosphorylation of the respective alanine mutants | Homo sapiens |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant FLAG-tagged wild-type and mutant GRK1 and GRK7 from HEK-293 cells | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| retina | GRK1 | Homo sapiens | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
- |
Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + rhodopsin | GRK1 and GRK7 | Homo sapiens | ADP + phosphorhodopsin | - |
? | |
| ATP + rhodopsin | bovine retina rhodopsin, GRK1 and GRK7 | Homo sapiens | ADP + phosphorhodopsin | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| ? | x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE | Homo sapiens |
| More | GRK1 and GRK7 peptide mapping | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| G-protein coupled receptor kinase | - |
Homo sapiens |
| GRK1 | - |
Homo sapiens |
| GRK7 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 1 | - |
rhodopsin | recombinant wild-type GRK7, pH 7.0, 30°C | Homo sapiens | |
| 1.2 | - |
rhodopsin | recombinant wild-type GRK1, pH 7.0, 30°C | Homo sapiens | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
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