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Literature summary extracted from

  • Premont, R.T.; Gainetdinov, R.R.
    Physiological roles of G protein-coupled receptor kinases and arrestins (2007), Annu. Rev. Physiol., 69, 511-534.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
2.7.11.16 additional information GRK short hairpin RNA knockdown, GRK5 knockout results in altered central and lung M2 muscarinic receptor regulation, with normal heart M2 receptor regulation, while GRK4 knockout does not result in an altered phenotype, GRK6 knockout leads to altered central dopamine receptor regulation deficient lymphocyte chemotaxis, increased acute inflammation and neutrophil chemotaxis, positive correlation between certain GRK4 polymorphisms, or haplotypes, and hypertensive disease Homo sapiens
2.7.11.16 additional information GRK short hairpin RNA knockdown, GRK5 knockout results in altered central and lung M2 muscarinic receptor regulation, with normal heart M2 receptor regulation, while GRK4 knockout does not result in an altered phenotype, GRK6 knockout leads to altered central dopamine receptor regulation deficient lymphocyte chemotaxis, increased acute inflammation and neutrophil chemotaxis, positive correlation between certain GRK4 polymorphisms, or haplotypes, and hypertensive disease, knockout mice phenotypes, detailed overview Mus musculus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.16 cytoplasm
-
 Mus musculus 5737
-
2.7.11.16 cytoplasm
-
 Homo sapiens 5737
-
2.7.11.16 additional information GRK4, GRK5, and GRK6 lack the G protein betagamma-subunit binding domain but use direct PIP2 binding and/or covalent lipid modification with palmitate to reside primarily at the plasma membrane Mus musculus
-
-
2.7.11.16 additional information GRK4, GRK5, and GRK6 lack the G protein betagamma-subunit binding domain but use direct PIP2 binding and/or covalent lipid modification with palmitate to reside primarily at the plasma membrane Homo sapiens
-
-
2.7.11.16 plasma membrane bound to GPC receptors Mus musculus 5886
-
2.7.11.16 plasma membrane bound to GPC receptors Homo sapiens 5886
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.16 ATP + a G protein-coupled receptor Mus musculus the GRKs are important in the cardiovascular system, the major G protein-coupled receptor regulatory pathway involves phosphorylation of activated receptors by GRKs, followed by binding of arrestin proteins, which prevent receptors from activating downstream heterotrimeric G protein pathways while allowing activation of arrestin-dependent signaling pathways, general mechanisms of GRK-arrestin regulation, overview, physiological functions and potential pathophysiological roles of GRKs and arrestins in human disorders, overview ADP + a phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + a G protein-coupled receptor Homo sapiens the GRKs are important in the cardiovascular system, the major G protein-coupled receptor regulatory pathway involves phosphorylation of activated receptors by GRKs, followed by binding of arrestin proteins, which prevent receptors from activating downstream heterotrimeric G protein pathways while allowing activation of arrestin-dependent signaling pathways, general mechanisms of GRK-arrestin regulation, overview, physiological functions and potential pathophysiological roles of GRKs and arrestins in human disorders, overview ADP + a phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + BLT1 receptor Mus musculus GRK6, ablation of GRK6 leads to augmented signaling by leukotriene B4 acting through the BLT1 receptor ADP + phosphorylated BLT1 receptor
-
 ?
2.7.11.16 ATP + BLT1 receptor Homo sapiens GRK6, ablation of GRK6 leads to augmented signaling by leukotriene B4 acting through the BLT1 receptor ADP + phosphorylated BLT1 receptor
-
 ?
2.7.11.16 ATP + CXCR4 receptor Mus musculus GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow ADP + phosphorylated CXCR4 receptor
-
 ?
2.7.11.16 ATP + CXCR4 receptor Homo sapiens GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow ADP + phosphorylated CXCR4 receptor
-
 ?
2.7.11.16 ATP + dopamine D1 receptor Mus musculus GRK4 ADP + phosphorylated dopamine D1 receptor
-
 ?
2.7.11.16 ATP + dopamine D1 receptor Homo sapiens GRK4 ADP + phosphorylated dopamine D1 receptor
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.16 Homo sapiens
-
-
-
2.7.11.16 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.16 brain expression of GRK4 in the brain is limited to cerebellar Purkinje cells Mus musculus
-
2.7.11.16 brain expression of GRK4 in the brain is limited to cerebellar Purkinje cells Homo sapiens
-
2.7.11.16 cerebellum
-
 Mus musculus
-
2.7.11.16 cerebellum
-
 Homo sapiens
-
2.7.11.16 heart
-
 Mus musculus
-
2.7.11.16 heart
-
 Homo sapiens
-
2.7.11.16 lung
-
 Mus musculus
-
2.7.11.16 lung
-
 Homo sapiens
-
2.7.11.16 lymphocyte
-
 Mus musculus
-
2.7.11.16 lymphocyte
-
 Homo sapiens
-
2.7.11.16 neuron GRK4, GRK5, and GRK6 Mus musculus
-
2.7.11.16 neuron GRK4, GRK5, and GRK6 Homo sapiens
-
2.7.11.16 neutrophil
-
 Mus musculus
-
2.7.11.16 neutrophil
-
 Homo sapiens
-
2.7.11.16 Purkinje cell GRK4 Mus musculus
-
2.7.11.16 Purkinje cell GRK4 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.16 ATP + a G protein-coupled receptor the GRKs are important in the cardiovascular system, the major G protein-coupled receptor regulatory pathway involves phosphorylation of activated receptors by GRKs, followed by binding of arrestin proteins, which prevent receptors from activating downstream heterotrimeric G protein pathways while allowing activation of arrestin-dependent signaling pathways, general mechanisms of GRK-arrestin regulation, overview, physiological functions and potential pathophysiological roles of GRKs and arrestins in human disorders, overview Mus musculus ADP + a phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + a G protein-coupled receptor the GRKs are important in the cardiovascular system, the major G protein-coupled receptor regulatory pathway involves phosphorylation of activated receptors by GRKs, followed by binding of arrestin proteins, which prevent receptors from activating downstream heterotrimeric G protein pathways while allowing activation of arrestin-dependent signaling pathways, general mechanisms of GRK-arrestin regulation, overview, physiological functions and potential pathophysiological roles of GRKs and arrestins in human disorders, overview Homo sapiens ADP + a phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + a G protein-coupled receptor cell surface localized receptors Mus musculus ADP + a phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + a G protein-coupled receptor cell surface localized receptors Homo sapiens ADP + a phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + BLT1 receptor GRK6, ablation of GRK6 leads to augmented signaling by leukotriene B4 acting through the BLT1 receptor Mus musculus ADP + phosphorylated BLT1 receptor
-
 ?
2.7.11.16 ATP + BLT1 receptor GRK6, ablation of GRK6 leads to augmented signaling by leukotriene B4 acting through the BLT1 receptor Homo sapiens ADP + phosphorylated BLT1 receptor
-
 ?
2.7.11.16 ATP + BLT1 receptor GRK6 Mus musculus ADP + phosphorylated BLT1 receptor
-
 ?
2.7.11.16 ATP + BLT1 receptor GRK6 Homo sapiens ADP + phosphorylated BLT1 receptor
-
 ?
2.7.11.16 ATP + CXCR4 receptor GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow Mus musculus ADP + phosphorylated CXCR4 receptor
-
 ?
2.7.11.16 ATP + CXCR4 receptor GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow Homo sapiens ADP + phosphorylated CXCR4 receptor
-
 ?
2.7.11.16 ATP + CXCR4 receptor GRK6 Mus musculus ADP + phosphorylated CXCR4 receptor
-
 ?
2.7.11.16 ATP + CXCR4 receptor GRK6 Homo sapiens ADP + phosphorylated CXCR4 receptor
-
 ?
2.7.11.16 ATP + dopamine D1 receptor GRK4 Mus musculus ADP + phosphorylated dopamine D1 receptor
-
 ?
2.7.11.16 ATP + dopamine D1 receptor GRK4 Homo sapiens ADP + phosphorylated dopamine D1 receptor
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.16 More GRK4, GRK5, and GRK6 lack the G protein betagamma-subunit binding domain but use direct PIP2 binding and/or covalent lipid modification with palmitate to reside primarily at the plasma membrane Mus musculus
2.7.11.16 More GRK4, GRK5, and GRK6 lack the G protein betagamma-subunit binding domain but use direct PIP2 binding and/or covalent lipid modification with palmitate to reside primarily at the plasma membrane Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.11.16 G protein-coupled receptor kinase
-
 Mus musculus
2.7.11.16 G protein-coupled receptor kinase
-
 Homo sapiens
2.7.11.16 GRK
-
 Mus musculus
2.7.11.16 GRK
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.16 ATP
-
 Mus musculus
2.7.11.16 ATP
-
 Homo sapiens