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Literature summary extracted from

  • Jimenez-Sainz, M.C.; Murga, C.; Kavelaars, A.; Jurado-Pueyo, M.; Krakstad, B.F.; Heijnen, C.J.; Mayor, F.Jr.; Aragay, A.M.
    G protein-coupled receptor kinase 2 negatively regulates chemokine signaling at a level downstream from G protein subunits (2006), Mol. Biol. Cell, 17, 25-31.
    View publication on PubMedView publication on EuropePMC

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.15 G protein required for GRK2 activation Mus musculus
2.7.11.15 G protein required for GRK2 activation Bos taurus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.15 expression of wild-type GRK2 and mutants in HEK-293 cells, co-expression of GRK2 and CCR2B produces a 65-70% reduction for the wild-type GRK2 and 52% for the mutant GRK2 K220R in ERK phosphorylation by inhibition of CCL2 Bos taurus

Protein Variants

EC Number Protein Variants Comment Organism
2.7.11.15 D110A the mutant shows impaired binding to Galphaq proteins, mutant GRK2 inhibits ERK phosphorylation similar to the wild-type enzyme when co-expressed with CCR2B in HEK-293 cells Bos taurus
2.7.11.15 K220R mutant GRK2 inhibits ERK phosphorylation in a slightly reduced rate compared to the wild-type enzyme when co-expressed with CCR2B in HEK-293 cells Bos taurus
2.7.11.15 additional information construction of a deletion GRK2 mutant comprising residues 438-689, which does not inhibit ERK phosphorylation when co-expressed with CCR2B in HEK-293 cells Bos taurus
2.7.11.15 additional information construction of a phosphorylation-defective CCR2 mutant mice, in the mutant mice GRK2 inhibits ERK activation similar to the wild-type mice, the inhibitory effect is eliminated by co-expression of Galphaq-binding RGS-like RH domain of GRK2 or its Gbetagamma-binding domain Mus musculus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.15 ATP + G protein-coupled receptor Mus musculus desensitization by GRK2 of the ligand-activated receptor ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 ATP + G protein-coupled receptor Bos taurus desensitization by GRK2 of the ligand-activated receptor ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 additional information Mus musculus GRK2 regulation mechanism of ERK activation involving interaction with mitogen-activated protein kinase, GRK2 diminishes the level of activating phosphorylation of ERK by CCL2 binding to chemokine receptor CCR2 in endothelial cells ?
-
 ?
2.7.11.15 additional information Bos taurus GRK2 regulation mechanism of ERK activation involving interaction with mitogen-activated protein kinase, GRK2 diminishes the level of activating phosphorylation of ERK by CCL2 binding to chemokine receptor CCR2 in endothelial cells ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.15 Bos taurus
-
-
-
2.7.11.15 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.15 splenocyte primary Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.15 ATP + G protein-coupled receptor
-
 Mus musculus ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 ATP + G protein-coupled receptor
-
 Bos taurus ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 ATP + G protein-coupled receptor desensitization by GRK2 of the ligand-activated receptor Mus musculus ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 ATP + G protein-coupled receptor desensitization by GRK2 of the ligand-activated receptor Bos taurus ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 additional information GRK2 regulation mechanism of ERK activation involving interaction with mitogen-activated protein kinase, GRK2 diminishes the level of activating phosphorylation of ERK by CCL2 binding to chemokine receptor CCR2 in endothelial cells Mus musculus ?
-
 ?
2.7.11.15 additional information GRK2 regulation mechanism of ERK activation involving interaction with mitogen-activated protein kinase, GRK2 diminishes the level of activating phosphorylation of ERK by CCL2 binding to chemokine receptor CCR2 in endothelial cells Bos taurus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.15 G protein-coupled receptor kinase 2
-
 Mus musculus
2.7.11.15 G protein-coupled receptor kinase 2
-
 Bos taurus
2.7.11.15 GRK2
-
 Mus musculus
2.7.11.15 GRK2
-
 Bos taurus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.15 ATP
-
 Mus musculus
2.7.11.15 ATP
-
 Bos taurus