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Literature summary for 2.7.11.16 extracted from
- Physiological roles of G protein-coupled receptor kinases and arrestins (2007), Annu. Rev. Physiol., 69, 511-534.
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| 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 |
| 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
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytoplasm | - |
Mus musculus | 5737 | - |
| cytoplasm | - |
Homo sapiens | 5737 | - |
| 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 | - |
- |
| 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 | - |
- |
| plasma membrane | bound to GPC receptors | Mus musculus | 5886 | - |
| plasma membrane | bound to GPC receptors | Homo sapiens | 5886 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 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 | - |
? |  |
| 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 | - |
? | |
| 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 | - |
? | |
| 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 | - |
? | |
| ATP + CXCR4 receptor | Mus musculus | GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow | ADP + phosphorylated CXCR4 receptor | - |
? | |
| ATP + CXCR4 receptor | Homo sapiens | GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow | ADP + phosphorylated CXCR4 receptor | - |
? | |
| ATP + dopamine D1 receptor | Mus musculus | GRK4 | ADP + phosphorylated dopamine D1 receptor | - |
? | |
| ATP + dopamine D1 receptor | Homo sapiens | GRK4 | ADP + phosphorylated dopamine D1 receptor | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | expression of GRK4 in the brain is limited to cerebellar Purkinje cells | Mus musculus | - |
| brain | expression of GRK4 in the brain is limited to cerebellar Purkinje cells | Homo sapiens | - |
| cerebellum | - |
Mus musculus | - |
| cerebellum | - |
Homo sapiens | - |
| heart | - |
Mus musculus | - |
| heart | - |
Homo sapiens | - |
| lung | - |
Mus musculus | - |
| lung | - |
Homo sapiens | - |
| lymphocyte | - |
Mus musculus | - |
| lymphocyte | - |
Homo sapiens | - |
| neuron | GRK4, GRK5, and GRK6 | Mus musculus | - |
| neuron | GRK4, GRK5, and GRK6 | Homo sapiens | - |
| neutrophil | - |
Mus musculus | - |
| neutrophil | - |
Homo sapiens | - |
| Purkinje cell | GRK4 | Mus musculus | - |
| Purkinje cell | GRK4 | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 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 | - |
? | |
| 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 | - |
? | |
| ATP + a G protein-coupled receptor | cell surface localized receptors | Mus musculus | ADP + a phosphorylated G protein-coupled receptor | - |
? | |
| ATP + a G protein-coupled receptor | cell surface localized receptors | Homo sapiens | ADP + a phosphorylated G protein-coupled receptor | - |
? | |
| 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 | - |
? | |
| 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 | - |
? | |
| ATP + BLT1 receptor | GRK6 | Mus musculus | ADP + phosphorylated BLT1 receptor | - |
? | |
| ATP + BLT1 receptor | GRK6 | Homo sapiens | ADP + phosphorylated BLT1 receptor | - |
? | |
| ATP + CXCR4 receptor | GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow | Mus musculus | ADP + phosphorylated CXCR4 receptor | - |
? | |
| ATP + CXCR4 receptor | GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow | Homo sapiens | ADP + phosphorylated CXCR4 receptor | - |
? | |
| ATP + CXCR4 receptor | GRK6 | Mus musculus | ADP + phosphorylated CXCR4 receptor | - |
? | |
| ATP + CXCR4 receptor | GRK6 | Homo sapiens | ADP + phosphorylated CXCR4 receptor | - |
? | |
| ATP + dopamine D1 receptor | GRK4 | Mus musculus | ADP + phosphorylated dopamine D1 receptor | - |
? | |
| ATP + dopamine D1 receptor | GRK4 | Homo sapiens | ADP + phosphorylated dopamine D1 receptor | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| 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 |
| 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
| Synonyms | Comment | Organism |
|---|---|---|
| G protein-coupled receptor kinase | - |
Mus musculus |
| G protein-coupled receptor kinase | - |
Homo sapiens |
| GRK | - |
Mus musculus |
| GRK | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Mus musculus | |
| ATP | - |
Homo sapiens | |
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