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Literature summary 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

EC Number Activating Compound Comment Organism Structure
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 additional information phosphorylation by c-Src activates GRK2 Mus musculus
2.7.11.15 additional information phosphorylation by c-Src activates GRK2 Homo sapiens
2.7.11.15 additional information phosphorylation by c-Src activates GRK2 Rattus norvegicus
2.7.11.15 phosphatidylinositol 4,5-bisphosphate binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Mus musculus
2.7.11.15 phosphatidylinositol 4,5-bisphosphate binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Homo sapiens
2.7.11.15 phosphatidylinositol 4,5-bisphosphate binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Rattus norvegicus
2.7.11.15 phosphatidylserine binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Mus musculus
2.7.11.15 phosphatidylserine binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Homo sapiens
2.7.11.15 phosphatidylserine binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity Rattus norvegicus
2.7.11.16 phosphatidylinositol 4,5-bisphosphate activates the receptor phosphorylation activity of GRK5, but not its autophosphorylation or peptide phosphorylation activity Mus musculus
2.7.11.16 phosphatidylinositol 4,5-bisphosphate activates the receptor phosphorylation activity of GRK5, but not its autophosphorylation or peptide phosphorylation activity Homo sapiens
2.7.11.16 Phospholipids activate GRK5 Homo sapiens

Protein Variants

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.15 actinin inhibits GRK2 Homo sapiens
2.7.11.15 actinin inhibits GRK2 Mus musculus
2.7.11.15 actinin inhibits GRK2 Rattus norvegicus
2.7.11.15 Ca2+ inhibits GRK2 Rattus norvegicus
2.7.11.15 Calmodulin inhibits GRK2 Homo sapiens
2.7.11.15 Calmodulin inhibits GRK2 Mus musculus
2.7.11.15 Calmodulin inhibits GRK2 Rattus norvegicus
2.7.11.15 caveolin microsomal anchor protein, inhibits GRK2 Homo sapiens
2.7.11.15 caveolin microsomal anchor protein, inhibits GRK2 Mus musculus
2.7.11.15 caveolin microsomal anchor protein, inhibits GRK2 Rattus norvegicus
2.7.11.15 additional information phosphorylation by ERK1/2 inhibits GRK2 Homo sapiens
2.7.11.15 additional information phosphorylation by ERK1/2 inhibits GRK2 Mus musculus
2.7.11.15 additional information phosphorylation by ERK1/2 inhibits GRK2 Rattus norvegicus
2.7.11.16 actinin inhibits GRK5 Homo sapiens
2.7.11.16 actinin inhibits GRK5 Mus musculus
2.7.11.16 Ca2+ inhibits GRK5 Mus musculus
2.7.11.16 Calmodulin inhibits GRK5 Homo sapiens
2.7.11.16 Calmodulin inhibits GRK5 Mus musculus
2.7.11.16 caveolin inhibits GRK5 Homo sapiens
2.7.11.16 caveolin inhibits GRK5 Mus musculus
2.7.11.16 additional information phosphorylation by PKC inhibits GRK5 Homo sapiens
2.7.11.16 additional information phosphorylation by PKC inhibits GRK5 Mus musculus

Localization

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

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.15 Ca2+ inhibits GRK2 Mus musculus
2.7.11.15 Ca2+ inhibits GRK2 Homo sapiens
2.7.11.15 Ca2+ inhibits GRK2 Rattus norvegicus
2.7.11.16 Ca2+ inhibits GRK5 Mus musculus
2.7.11.16 Ca2+ inhibits GRK5 Homo sapiens

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 regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 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
-
 ?
2.7.11.15 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
-
 ?
2.7.11.15 additional information Mus musculus GRKs are involved in diverse physiological processes and pathologies, overview ?
-
 ?
2.7.11.15 additional information Homo sapiens GRKs are involved in diverse physiological processes and pathologies, overview ?
-
 ?
2.7.11.15 additional information Rattus norvegicus GRKs are involved in diverse physiological processes and pathologies, overview ?
-
 ?
2.7.11.16 ATP + G protein-coupled receptor Mus musculus regulation mechanism of GRK5, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + G protein-coupled receptor Homo sapiens regulation mechanism of GRK5, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 additional information Mus musculus GRKs are involved in diverse physiological processes and pathologies, overview ?
-
 ?
2.7.11.16 additional information Homo sapiens GRKs are involved in diverse physiological processes and pathologies, overview ?
-
 ?

Organism

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

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.15 additional information mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquination or protease cleavage, overview Rattus norvegicus
2.7.11.15 additional information mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquitination or protease cleavage, overview Mus musculus
2.7.11.15 additional information mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquitination or protease cleavage, overview Homo sapiens
2.7.11.15 phosphoprotein GRK2 is phosphorylated by c-Src kinase, ERK1 and ERK2, protein kinase C, and PKA, overview Mus musculus
2.7.11.15 phosphoprotein GRK2 is phosphorylated by c-Src kinase, ERK1 and ERK2, protein kinase C, and PKA, overview Homo sapiens
2.7.11.15 phosphoprotein GRK2 is phosphorylated by c-Src kinase, ERK1 and ERK2, protein kinase C, and PKA, overview Rattus norvegicus
2.7.11.16 additional information mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquitination or protease cleavage, overview Mus musculus
2.7.11.16 additional information mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquitination or protease cleavage, overview Homo sapiens
2.7.11.16 phosphoprotein GRK5 performs autophosphorylation and is phosphorylated by protein kinase C Mus musculus
2.7.11.16 phosphoprotein GRK5 performs autophosphorylation and is phosphorylated by protein kinase C Homo sapiens

Reaction

EC Number Reaction Comment Organism Reaction ID
2.7.11.15 ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor] regulation mechanism Mus musculus
a
2.7.11.15 ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor] regulation mechanism Homo sapiens
a
2.7.11.15 ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor] regulation mechanism Rattus norvegicus
a
2.7.11.16 ATP + [G protein-coupled receptor] = ADP + [G protein-coupled receptor]phosphate regulation mechanism Mus musculus
a
2.7.11.16 ATP + [G protein-coupled receptor] = ADP + [G protein-coupled receptor]phosphate regulation mechanism Homo sapiens
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.15 heart
-
 Mus musculus
-
2.7.11.15 heart
-
 Homo sapiens
-
2.7.11.15 heart
-
 Rattus norvegicus
-
2.7.11.15 additional information GRK2 and GRK3 are expressed in a wide variety of tissues, expression patterns, overview Mus musculus
-
2.7.11.15 additional information GRK2 and GRK3 are expressed in a wide variety of tissues, expression patterns, overview Homo sapiens
-
2.7.11.15 additional information GRK2 and GRK3 are expressed in a wide variety of tissues, expression patterns, overview Rattus norvegicus
-
2.7.11.15 myelomonocytic leukemia cell GRK2 Mus musculus
-
2.7.11.15 myelomonocytic leukemia cell GRK2 Homo sapiens
-
2.7.11.15 myelomonocytic leukemia cell GRK2 Rattus norvegicus
-
2.7.11.15 T-lymphocyte
-
 Mus musculus
-
2.7.11.15 T-lymphocyte
-
 Homo sapiens
-
2.7.11.15 T-lymphocyte
-
 Rattus norvegicus
-
2.7.11.16 heart
-
 Mus musculus
-
2.7.11.16 heart
-
 Homo sapiens
-
2.7.11.16 additional information GRK5 and GRK6 are expressed in a wide variety of tissues, expression patterns, overview Mus musculus
-
2.7.11.16 additional information GRK5 and GRK6 are expressed in a wide variety of tissues, expression patterns, overview Homo sapiens
-
2.7.11.16 myelomonocytic leukemia cell GRK6 Mus musculus
-
2.7.11.16 myelomonocytic leukemia cell GRK6 Homo sapiens
-
2.7.11.16 T-lymphocyte
-
 Mus musculus
-
2.7.11.16 T-lymphocyte
-
 Homo sapiens
-
2.7.11.16 testis GRK4, mainly Mus musculus
-
2.7.11.16 testis GRK4, mainly Homo sapiens
-

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
-
 Homo sapiens ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 ATP + G protein-coupled receptor
-
 Rattus norvegicus ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.15 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
-
 ?
2.7.11.15 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
-
 ?
2.7.11.15 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
-
 ?
2.7.11.15 additional information GRKs are involved in diverse physiological processes and pathologies, overview Mus musculus ?
-
 ?
2.7.11.15 additional information GRKs are involved in diverse physiological processes and pathologies, overview Homo sapiens ?
-
 ?
2.7.11.15 additional information GRKs are involved in diverse physiological processes and pathologies, overview Rattus norvegicus ?
-
 ?
2.7.11.15 additional information GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and G protein-coupled receptor kinase interacting protein, GIT Mus musculus ?
-
 ?
2.7.11.15 additional information GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and G protein-coupled receptor kinase interacting protein, GIT Homo sapiens ?
-
 ?
2.7.11.15 additional information GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and GIT Rattus norvegicus ?
-
 ?
2.7.11.16 ATP + G protein-coupled receptor
-
 Mus musculus ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + G protein-coupled receptor
-
 Homo sapiens ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + G protein-coupled receptor regulation mechanism of GRK5, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview Mus musculus ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 ATP + G protein-coupled receptor regulation mechanism of GRK5, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview Homo sapiens ADP + phosphorylated G protein-coupled receptor
-
 ?
2.7.11.16 additional information GRKs are involved in diverse physiological processes and pathologies, overview Mus musculus ?
-
 ?
2.7.11.16 additional information GRKs are involved in diverse physiological processes and pathologies, overview Homo sapiens ?
-
 ?
2.7.11.16 additional information GRK5 performs autophosphorylation Mus musculus ?
-
 ?
2.7.11.16 additional information GRK5 performs autophosphorylation Homo sapiens ?
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.15 More betaARK subfamily multidomain structure, overview Mus musculus
2.7.11.15 More betaARK subfamily multidomain structure, overview Homo sapiens
2.7.11.15 More betaARK subfamily multidomain structure, overview Rattus norvegicus
2.7.11.16 More GRK4 subfamily multidomain structure, overview Mus musculus
2.7.11.16 More GRK4 subfamily multidomain structure, overview Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.11.15 betaARK1
-
 Mus musculus
2.7.11.15 betaARK1
-
 Homo sapiens
2.7.11.15 betaARK1
-
 Rattus norvegicus
2.7.11.15 betaARK2
-
 Mus musculus
2.7.11.15 betaARK2
-
 Homo sapiens
2.7.11.15 betaARK2
-
 Rattus norvegicus
2.7.11.15 G protein-coupled receptor kinase
-
 Mus musculus
2.7.11.15 G protein-coupled receptor kinase
-
 Homo sapiens
2.7.11.15 G protein-coupled receptor kinase
-
 Rattus norvegicus
2.7.11.15 GRK2
-
 Mus musculus
2.7.11.15 GRK2
-
 Homo sapiens
2.7.11.15 GRK2
-
 Rattus norvegicus
2.7.11.15 GRK3
-
 Mus musculus
2.7.11.15 GRK3
-
 Homo sapiens
2.7.11.15 GRK3
-
 Rattus norvegicus
2.7.11.15 More enzymes belong to the GRK family, GRK2 and GRK3, i.e. betaARK1 and betaARK2, form the betaARK subfamily Mus musculus
2.7.11.15 More enzymes belong to the GRK family, GRK2 and GRK3, i.e. betaARK1 and betaARK2, form the betaARK subfamily Homo sapiens
2.7.11.15 More enzymes belong to the GRK family, GRK2 and GRK3, i.e. betaARK1 and betaARK2, form the betaARK subfamily Rattus norvegicus
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 GRK4
-
 Mus musculus
2.7.11.16 GRK4
-
 Homo sapiens
2.7.11.16 GRK5
-
 Mus musculus
2.7.11.16 GRK5
-
 Homo sapiens
2.7.11.16 GRK6
-
 Mus musculus
2.7.11.16 GRK6
-
 Homo sapiens
2.7.11.16 More enzymes belong to the GRK family, GRK4, GRK5, and GRK6 form the GRK4 subfamily Mus musculus
2.7.11.16 More enzymes belong to the GRK family, GRK4, GRK5, and GRK6 form the GRK4 subfamily Homo sapiens

Cofactor

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