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Literature summary extracted from

  • Ribas, C.; Penela, P.; Murga, C.; Salcedo, A.; Garcia-Hoz, C.; Jurado-Pueyo, M.; Aymerich, I.; Mayor, F.
    The G protein-coupled receptor kinase (GRK) interactome: Role of GRKs in GPCR regulation and signaling (2007), Biochim. Biophys. Acta, 1768, 913-922.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.15 additional information phosphorylation activates the enzyme Homo sapiens
2.7.11.15 additional information GRK2 is activated by phosphorylation through kinases c-SRC, PKA and PKC, and it is activated by phospholipids Mammalia
2.7.11.16 additional information phosphorylation activates the enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.15 actin
-
 Homo sapiens
2.7.11.15 actinin
-
 Mammalia
2.7.11.15 alpha-actinin
-
 Homo sapiens
2.7.11.15 Ca2+/calmodulin
-
 Mammalia
2.7.11.15 Calmodulin
-
 Homo sapiens
2.7.11.15 caveolin
-
 Homo sapiens
2.7.11.15 caveolin
-
 Mammalia
2.7.11.15 Raf kinase inhibitor protein RKIP Mammalia
2.7.11.15 RKIP
-
 Homo sapiens
2.7.11.16 actin
-
 Homo sapiens
2.7.11.16 alpha-actinin
-
 Homo sapiens
2.7.11.16 Calmodulin
-
 Homo sapiens
2.7.11.16 caveolin
-
 Homo sapiens
2.7.11.16 RKIP
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.16 membrane
-
 Mammalia 16020
-
2.7.11.16 nucleus GRK5 Mammalia 5634
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.15 Mg2+
-
 Homo sapiens
2.7.11.16 Mg2+
-
 Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.7.11.15 80000
-
 x * 80000, GRK2, SDS-PAGE Homo sapiens
2.7.11.15 80000
-
 x * 80000, GRK2 catalytic domain, domain structure, overview Mammalia
2.7.11.16 69000
-
 x * 69000, GRK5, SDS-PAGE Homo sapiens
2.7.11.16 69000
-
 x * 69000, about, GRK5 catalytic domain, domain structure, overview Mammalia

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.15 additional information Homo sapiens GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview ?
-
 ?
2.7.11.15 additional information Mammalia G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP. Different mechanisms of signalling pathways modulation by GRK2, and regulation of GRK2, overview ?
-
 ?
2.7.11.16 additional information Homo sapiens GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview ?
-
 ?
2.7.11.16 additional information Mammalia G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.15 Homo sapiens
-
-
-
2.7.11.15 Mammalia
-
-
-
2.7.11.16 Homo sapiens
-
-
-
2.7.11.16 Mammalia
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.15 phosphoprotein phosphorylation, e.g. by PKA, PKC, ERK1/2 or c-SRC, activates the enzyme Homo sapiens
2.7.11.16 phosphoprotein phosphorylation, e.g. by PKA, PKC, ERK1/2 or c-SRC, activates the enzyme Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.15 additional information GRK2 and GRK3 are ubiquitously expressed in mammalian tissues Mammalia
-
2.7.11.16 cerebellum GRK4 Mammalia
-
2.7.11.16 kidney GRK4 Mammalia
-
2.7.11.16 additional information GRK5 and GRK6 are ubiquitously expressed in mammalian tissues Mammalia
-
2.7.11.16 testis GRK4 Mammalia
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.15 ATP + ezrin GRK2 Homo sapiens ADP + phosphorylated ezrin
-
 ?
2.7.11.15 ATP + phosducin GRK2 Homo sapiens ADP + phosphorylated phosducin
-
 ?
2.7.11.15 ATP + R-smad GRK2 Homo sapiens ADP + phosphorylated R-smad
-
 ?
2.7.11.15 ATP + ribosomal protein P2 GRK2 Homo sapiens ADP + phosphorylated ribosomal protein P2
-
 ?
2.7.11.15 ATP + synuclein GRK2 Homo sapiens ADP + phosphorylated synuclein
-
 ?
2.7.11.15 ATP + tubulin GRK2 Homo sapiens ADP + phosphorylated tubulin
-
 ?
2.7.11.15 additional information GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview Homo sapiens ?
-
 ?
2.7.11.15 additional information G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP. Different mechanisms of signalling pathways modulation by GRK2, and regulation of GRK2, overview Mammalia ?
-
 ?
2.7.11.15 additional information GRK2 can also phosphorylate non-receptor substrates such as phosducins, synucleins, tubulin, ribosomal protein P2, ezrin, and receptor regulated Smads. The RH domain of GRK2 specifically interacts with Galphaq family members, although it does not stimulate the GTPase activity of Galphaq as efficiently as other classical RGS proteins do, interaction with other oroteins, detailed overview Mammalia ?
-
 ?
2.7.11.16 additional information GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview Homo sapiens ?
-
 ?
2.7.11.16 additional information G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP Mammalia ?
-
 ?
2.7.11.16 additional information no interaction of the RH domains of GRK5 and GRK6 with Galpha proteins. GRK5 contains a DNA-binding nuclear localization sequence that allows its binding to DNA and its localization in the nucleus upon GPCR activation, interaction with other oroteins, detailed overview Mammalia ?
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.15 ? x * 80000, GRK2, SDS-PAGE Homo sapiens
2.7.11.15 ? x * 80000, GRK2 catalytic domain, domain structure, overview Mammalia
2.7.11.15 More domain structure of GRK2, overview Homo sapiens
2.7.11.16 ? x * 69000, GRK5, SDS-PAGE Homo sapiens
2.7.11.16 ? x * 69000, about, GRK5 catalytic domain, domain structure, overview Mammalia
2.7.11.16 More domain structure of GRK4-6, overview Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.11.15 G protein-coupled receptor kinase 2
-
 Homo sapiens
2.7.11.15 G protein-coupled receptor kinase 3
-
 Homo sapiens
2.7.11.15 GRK2
-
 Mammalia
2.7.11.15 GRK2
-
 Homo sapiens
2.7.11.15 GRK3
-
 Homo sapiens
2.7.11.15 More the enzyme belongs to the beta-adrenergic receptor kinase subfamily Homo sapiens
2.7.11.15 More the enzyme belongs to the beta-adrenergic receptor kinases subfamily Mammalia
2.7.11.16 G protein-coupled receptor kinase 5
-
 Homo sapiens
2.7.11.16 GRK4
-
 Mammalia
2.7.11.16 GRK4
-
 Homo sapiens
2.7.11.16 GRK5
-
 Mammalia
2.7.11.16 GRK5
-
 Homo sapiens
2.7.11.16 GRK6
-
 Mammalia
2.7.11.16 GRK6
-
 Homo sapiens
2.7.11.16 More the enzyme belongs to the GRK4 subfamily Mammalia
2.7.11.16 More the enzyme belongs to the GRK4 subfamily Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.15 ATP
-
 Homo sapiens
2.7.11.16 ATP
-
 Homo sapiens