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Literature summary 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
| EC Number | Activating Compound | Comment | Organism | Structure |
|---|---|---|---|---|
| 2.7.11.11 | cAMP | dependent on | Homo sapiens |  |
| 2.7.11.11 | cAMP | dependent on | Bos taurus | |
| 2.7.11.11 | dibutyryl-cAMP | activates in vitro | Bos taurus | |
| 2.7.11.14 | 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)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 2.7.11.14 | expression of FLAG-tagged wild-type and mutant GRK1 and GRK7 in HEK-293 cells | Homo sapiens |
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 2.7.11.14 | K219R | kinase inactive mutant of GRK1 | Homo sapiens |
| 2.7.11.14 | K220R | kinase inactive mutant of GRK7 | Homo sapiens |
| 2.7.11.14 | S21A | site-directed mutagenesis of GRK1 PKA phosphorylation site, the mutant shows 87% of wild-type enzyme activity | Homo sapiens |
| 2.7.11.14 | S21E | site-directed mutagenesis of GRK1 PKA phosphorylation site, the mutant shows 80% of wild-type enzyme activity | Homo sapiens |
| 2.7.11.14 | S23A | site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 67% of wild-type enzyme activity | Homo sapiens |
| 2.7.11.14 | S23A/S36A | site-directed mutagenesis of GRK7 PKA phosphorylation sites, the mutant shows 81% of wild-type enzyme activity | Homo sapiens |
| 2.7.11.14 | S23E | site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 67% of wild-type enzyme activity | Homo sapiens |
| 2.7.11.14 | S23E/S36E | site-directed mutagenesis of GRK7 PKA phosphorylation sites, the mutant shows 79% of wild-type enzyme activity | Homo sapiens |
| 2.7.11.14 | S333A | site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme | Homo sapiens |
| 2.7.11.14 | S36A | site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 76% of wild-type enzyme activity | Homo sapiens |
| 2.7.11.14 | S36E | site-directed mutagenesis of GRK7 PKA phosphorylation site, the mutant shows 77% of wild-type enzyme activity | Homo sapiens |
| 2.7.11.14 | S441A | site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme | Homo sapiens |
| 2.7.11.14 | S490A | site-directed mutagenesis of GRK7, the mutant is unable to autophosphorylate | Homo sapiens |
| 2.7.11.14 | S490E | site-directed mutagenesis of GRK7, the mutant is unable to autophosphorylate | Homo sapiens |
| 2.7.11.14 | T353A | site-directed mutagenesis of GRK7, mutant is similar to the wild-type enzyme | Homo sapiens |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 2.7.11.14 | additional information | - |
additional information | kinetics | Homo sapiens | |
| 2.7.11.14 | 0.0019 | - |
rhodopsin | recombinant wild-type GRK7, pH 7.0, 30°C | Homo sapiens | |
| 2.7.11.14 | 0.0035 | - |
rhodopsin | recombinant wild-type GRK1, pH 7.0, 30°C | Homo sapiens | |
| 2.7.11.14 | 0.0106 | - |
ATP | recombinant wild-type GRK1, pH 7.0, 30°C | Homo sapiens | |
| 2.7.11.14 | 0.0214 | - |
ATP | recombinant wild-type GRK7, pH 7.0, 30°C | Homo sapiens | |
Localization
| EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|---|
| 2.7.11.14 | photoreceptor outer segment membrane | - |
Homo sapiens | 42622 | - |
Metals/Ions
| EC Number | Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|---|
| 2.7.11.11 | Mg2+ | - |
Homo sapiens | |
| 2.7.11.11 | Mg2+ | - |
Bos taurus | |
| 2.7.11.14 | Mg2+ | - |
Homo sapiens | |
Molecular Weight [Da]
| EC Number | Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|---|
| 2.7.11.14 | 62200 | - |
x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE | Homo sapiens |
| 2.7.11.14 | 63500 | - |
x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE | Homo sapiens |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 2.7.11.11 | ATP + G protein-coupled receptor GRK1 | Bos taurus | - |
ADP + phosphorylated G protein-coupled receptor GRK1 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK1 | Homo sapiens | recombinant FLAG-tagged GRK1 expressed in HEK-293 cells, enzymatic inactivation of the receptor activity inhibiting rhodopsin phosphorylation | ADP + phosphorylated G protein-coupled receptor GRK1 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK7 | Bos taurus | - |
ADP + phosphorylated G protein-coupled receptor GRK7 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK7 | Homo sapiens | recombinant FLAG-tagged GRK1 expressed in HEK-293 cells, enzymatic inactivation of the receptor activity inhibiting rhodopsin phosphorylation | ADP + phosphorylated G protein-coupled receptor GRK7 | - |
? | |
| 2.7.11.11 | additional information | Homo sapiens | regulation of GRK1 and GRK7 by cAMP level during light and dark phases | ? | - |
? | |
| 2.7.11.11 | additional information | Bos taurus | regulation of GRK1 and GRK7 by cAMP level during light and dark phases | ? | - |
? | |
| 2.7.11.14 | ATP + rhodopsin | Homo sapiens | GRK1 and GRK7 | ADP + phosphorhodopsin | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 2.7.11.11 | Bos taurus | - |
- |
- |
| 2.7.11.11 | Homo sapiens | - |
- |
- |
| 2.7.11.14 | Homo sapiens | - |
- |
- |
Posttranslational Modification
| EC Number | Posttranslational Modification | Comment | Organism |
|---|---|---|---|
| 2.7.11.14 | 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)
| EC Number | Purification (Comment) | Organism |
|---|---|---|
| 2.7.11.14 | recombinant FLAG-tagged wild-type and mutant GRK1 and GRK7 from HEK-293 cells | Homo sapiens |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 2.7.11.11 | HEK-293 cell | - |
Homo sapiens | - |
| 2.7.11.11 | retina | - |
Bos taurus | - |
| 2.7.11.11 | retinal rod | - |
Homo sapiens | - |
| 2.7.11.11 | retinal rod | - |
Bos taurus | - |
| 2.7.11.14 | retina | GRK1 | Homo sapiens | - |
Specific Activity [micromol/min/mg]
| EC Number | Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|---|
| 2.7.11.14 | additional information | - |
- |
Homo sapiens |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 2.7.11.11 | ATP + G protein-coupled receptor GRK1 | - |
Bos taurus | ADP + phosphorylated G protein-coupled receptor GRK1 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK1 | recombinant FLAG-tagged GRK1 expressed in HEK-293 cells, enzymatic inactivation of the receptor activity inhibiting rhodopsin phosphorylation | Homo sapiens | ADP + phosphorylated G protein-coupled receptor GRK1 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK1 | phosphorylation at Ser21, enzymatic inactivation of the receptor activity inhibiting rhodopsin phosphorylation, no activity with GRK1 mutant S21A | Homo sapiens | ADP + phosphorylated G protein-coupled receptor GRK1 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK1 | recombinant FLAG-tagged GRK1, phosphorylation at Ser21 | Bos taurus | ADP + phosphorylated G protein-coupled receptor GRK1 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK7 | - |
Bos taurus | ADP + phosphorylated G protein-coupled receptor GRK7 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK7 | recombinant FLAG-tagged GRK1 expressed in HEK-293 cells, enzymatic inactivation of the receptor activity inhibiting rhodopsin phosphorylation | Homo sapiens | ADP + phosphorylated G protein-coupled receptor GRK7 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK7 | phosphorylation at Ser23 and Ser36, enzymatic inactivation of the receptor activity inhibiting rhodopsin phosphorylation, no activity with GRK1 mutants S23A/S36A and S23E/S36E | Homo sapiens | ADP + phosphorylated G protein-coupled receptor GRK7 | - |
? | |
| 2.7.11.11 | ATP + G protein-coupled receptor GRK7 | recombinant FLAG-tagged GRK7, phosphorylation at Ser23 and Ser36 | Bos taurus | ADP + phosphorylated G protein-coupled receptor GRK7 | - |
? | |
| 2.7.11.11 | additional information | regulation of GRK1 and GRK7 by cAMP level during light and dark phases | Homo sapiens | ? | - |
? | |
| 2.7.11.11 | additional information | regulation of GRK1 and GRK7 by cAMP level during light and dark phases | Bos taurus | ? | - |
? | |
| 2.7.11.14 | ATP + rhodopsin | GRK1 and GRK7 | Homo sapiens | ADP + phosphorhodopsin | - |
? | |
| 2.7.11.14 | ATP + rhodopsin | bovine retina rhodopsin, GRK1 and GRK7 | Homo sapiens | ADP + phosphorhodopsin | - |
? | |
Subunits
| EC Number | Subunits | Comment | Organism |
|---|---|---|---|
| 2.7.11.14 | ? | x * 63500, recombinant FLAG-tagged GRK1, SDS-PAGE, x * 62200, recombinant FLAG-tagged GRK7, SDS-PAGE | Homo sapiens |
| 2.7.11.14 | More | GRK1 and GRK7 peptide mapping | Homo sapiens |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 2.7.11.11 | PKA | - |
Homo sapiens |
| 2.7.11.11 | PKA | - |
Bos taurus |
| 2.7.11.14 | G-protein coupled receptor kinase | - |
Homo sapiens |
| 2.7.11.14 | GRK1 | - |
Homo sapiens |
| 2.7.11.14 | GRK7 | - |
Homo sapiens |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 2.7.11.11 | 30 | - |
assay at | Homo sapiens |
| 2.7.11.11 | 30 | - |
assay at | Bos taurus |
| 2.7.11.14 | 30 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| EC Number | Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 2.7.11.14 | 1 | - |
rhodopsin | recombinant wild-type GRK7, pH 7.0, 30°C | Homo sapiens | |
| 2.7.11.14 | 1.2 | - |
rhodopsin | recombinant wild-type GRK1, pH 7.0, 30°C | Homo sapiens | |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 2.7.11.11 | 7.6 | - |
assay at | Homo sapiens |
| 2.7.11.11 | 7.6 | - |
assay at | Bos taurus |
| 2.7.11.14 | 7 | - |
assay at | Homo sapiens |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 2.7.11.11 | ATP | - |
Homo sapiens | |
| 2.7.11.11 | ATP | - |
Bos taurus | |
| 2.7.11.14 | ATP | - |
Homo sapiens | |
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