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Literature summary for 2.7.11.15 extracted from

  • Penela, P.; Ribas, C.; Mayor, F.
    Mechanisms of regulation of the expression and function of G protein-coupled receptor kinases (2003), Cell. Signal., 15, 973-981.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
G protein binding and modulation of GRK2 and GRK3, Gbetagamma subunits bind GRK2 required for lipid association and G protein-coupled receptor phosphorylation and are released afterwards Mus musculus
G protein binding and modulation of GRK2 and GRK3, Gbetagamma subunits bind GRK2 required for lipid association and G protein-coupled receptor phosphorylation and are released afterwards Homo sapiens
G protein binding and modulation of GRK2 and GRK3, Gbetagamma subunits bind GRK2 required for lipid association and G protein-coupled receptor phosphorylation and are released afterwards Rattus norvegicus
additional information phosphorylation by c-Src activates GRK2 Mus musculus
additional information phosphorylation by c-Src activates GRK2 Homo sapiens
additional information phosphorylation by c-Src activates GRK2 Rattus norvegicus
phosphatidylinositol 4,5-bisphosphate binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Mus musculus
phosphatidylinositol 4,5-bisphosphate binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Homo sapiens
phosphatidylinositol 4,5-bisphosphate binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Rattus norvegicus
phosphatidylserine binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Mus musculus
phosphatidylserine binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Homo sapiens
phosphatidylserine binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Rattus norvegicus

Protein Variants

Protein Variants Comment Organism
additional information construction of transgenic tissue specific or knockout mice Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
actinin inhibits GRK2 Homo sapiens
actinin inhibits GRK2 Mus musculus
actinin inhibits GRK2 Rattus norvegicus
Ca2+ inhibits GRK2 Rattus norvegicus
Calmodulin inhibits GRK2 Homo sapiens
Calmodulin inhibits GRK2 Mus musculus
Calmodulin inhibits GRK2 Rattus norvegicus
caveolin microsomal anchor protein, inhibits GRK2 Homo sapiens
caveolin microsomal anchor protein, inhibits GRK2 Mus musculus
caveolin microsomal anchor protein, inhibits GRK2 Rattus norvegicus
additional information phosphorylation by ERK1/2 inhibits GRK2 Homo sapiens
additional information phosphorylation by ERK1/2 inhibits GRK2 Mus musculus
additional information phosphorylation by ERK1/2 inhibits GRK2 Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
cytoplasm GRK2 and GRK3 Mus musculus 5737
-
cytoplasm GRK2 and GRK3 Homo sapiens 5737
-
cytoplasm GRK2 and GRK3 Rattus norvegicus 5737
-
plasma membrane GRK2 and GRK3, transient translocation upon G protein-coupled receptor activation Mus musculus 5886
-
plasma membrane GRK2 and GRK3, transient translocation upon G protein-coupled receptor activation Homo sapiens 5886
-
plasma membrane GRK2 and GRK3, transient translocation upon G protein-coupled receptor activation Rattus norvegicus 5886
-

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ inhibits GRK2 Mus musculus
Ca2+ inhibits GRK2 Homo sapiens
Ca2+ inhibits GRK2 Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + G protein-coupled receptor Mus musculus regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview ADP + phosphorylated G protein-coupled receptor
-
?
ATP + G protein-coupled receptor Homo sapiens regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview ADP + phosphorylated G protein-coupled receptor
-
?
ATP + G protein-coupled receptor Rattus norvegicus regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview ADP + phosphorylated G protein-coupled receptor
-
?
additional information Mus musculus GRKs are involved in diverse physiological processes and pathologies, overview ?
-
?
additional information Homo sapiens GRKs are involved in diverse physiological processes and pathologies, overview ?
-
?
additional information Rattus norvegicus GRKs are involved in diverse physiological processes and pathologies, overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
additional information mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquination or protease cleavage, overview Rattus norvegicus
additional information mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquitination or protease cleavage, overview Mus musculus
additional information mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquitination or protease cleavage, overview Homo sapiens
phosphoprotein GRK2 is phosphorylated by c-Src kinase, ERK1 and ERK2, protein kinase C, and PKA, overview Mus musculus
phosphoprotein GRK2 is phosphorylated by c-Src kinase, ERK1 and ERK2, protein kinase C, and PKA, overview Homo sapiens
phosphoprotein GRK2 is phosphorylated by c-Src kinase, ERK1 and ERK2, protein kinase C, and PKA, overview Rattus norvegicus

Reaction

Reaction Comment Organism Reaction ID
ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor] regulation mechanism Mus musculus
ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor] regulation mechanism Homo sapiens
ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor] regulation mechanism Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
heart
-
Mus musculus
-
heart
-
Homo sapiens
-
heart
-
Rattus norvegicus
-
additional information GRK2 and GRK3 are expressed in a wide variety of tissues, expression patterns, overview Mus musculus
-
additional information GRK2 and GRK3 are expressed in a wide variety of tissues, expression patterns, overview Homo sapiens
-
additional information GRK2 and GRK3 are expressed in a wide variety of tissues, expression patterns, overview Rattus norvegicus
-
myelomonocytic leukemia cell GRK2 Mus musculus
-
myelomonocytic leukemia cell GRK2 Homo sapiens
-
myelomonocytic leukemia cell GRK2 Rattus norvegicus
-
T-lymphocyte
-
Mus musculus
-
T-lymphocyte
-
Homo sapiens
-
T-lymphocyte
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + G protein-coupled receptor
-
Mus musculus ADP + phosphorylated G protein-coupled receptor
-
?
ATP + G protein-coupled receptor
-
Homo sapiens ADP + phosphorylated G protein-coupled receptor
-
?
ATP + G protein-coupled receptor
-
Rattus norvegicus ADP + phosphorylated G protein-coupled receptor
-
?
ATP + G protein-coupled receptor regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview Mus musculus ADP + phosphorylated G protein-coupled receptor
-
?
ATP + G protein-coupled receptor regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview Homo sapiens ADP + phosphorylated G protein-coupled receptor
-
?
ATP + G protein-coupled receptor regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview Rattus norvegicus ADP + phosphorylated G protein-coupled receptor
-
?
additional information GRKs are involved in diverse physiological processes and pathologies, overview Mus musculus ?
-
?
additional information GRKs are involved in diverse physiological processes and pathologies, overview Homo sapiens ?
-
?
additional information GRKs are involved in diverse physiological processes and pathologies, overview Rattus norvegicus ?
-
?
additional information GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and G protein-coupled receptor kinase interacting protein, GIT Mus musculus ?
-
?
additional information GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and G protein-coupled receptor kinase interacting protein, GIT Homo sapiens ?
-
?
additional information GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and GIT Rattus norvegicus ?
-
?

Subunits

Subunits Comment Organism
More betaARK subfamily multidomain structure, overview Mus musculus
More betaARK subfamily multidomain structure, overview Homo sapiens
More betaARK subfamily multidomain structure, overview Rattus norvegicus

Synonyms

Synonyms Comment Organism
betaARK1
-
Mus musculus
betaARK1
-
Homo sapiens
betaARK1
-
Rattus norvegicus
betaARK2
-
Mus musculus
betaARK2
-
Homo sapiens
betaARK2
-
Rattus norvegicus
G protein-coupled receptor kinase
-
Mus musculus
G protein-coupled receptor kinase
-
Homo sapiens
G protein-coupled receptor kinase
-
Rattus norvegicus
GRK2
-
Mus musculus
GRK2
-
Homo sapiens
GRK2
-
Rattus norvegicus
GRK3
-
Mus musculus
GRK3
-
Homo sapiens
GRK3
-
Rattus norvegicus
More enzymes belong to the GRK family, GRK2 and GRK3, i.e. betaARK1 and betaARK2, form the betaARK subfamily Mus musculus
More enzymes belong to the GRK family, GRK2 and GRK3, i.e. betaARK1 and betaARK2, form the betaARK subfamily Homo sapiens
More enzymes belong to the GRK family, GRK2 and GRK3, i.e. betaARK1 and betaARK2, form the betaARK subfamily Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Mus musculus
ATP
-
Homo sapiens
ATP
-
Rattus norvegicus