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Literature summary for 2.7.11.15 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

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

Inhibitors

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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
80000
-
x * 80000, GRK2, SDS-PAGE Homo sapiens
80000
-
x * 80000, GRK2 catalytic domain, domain structure, overview Mammalia

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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 ?
-
?
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 ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mammalia
-
-
-

Posttranslational Modification

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

Source Tissue

Source Tissue Comment Organism Textmining
additional information GRK2 and GRK3 are ubiquitously expressed in mammalian tissues Mammalia
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + ezrin GRK2 Homo sapiens ADP + phosphorylated ezrin
-
?
ATP + phosducin GRK2 Homo sapiens ADP + phosphorylated phosducin
-
?
ATP + R-smad GRK2 Homo sapiens ADP + phosphorylated R-smad
-
?
ATP + ribosomal protein P2 GRK2 Homo sapiens ADP + phosphorylated ribosomal protein P2
-
?
ATP + synuclein GRK2 Homo sapiens ADP + phosphorylated synuclein
-
?
ATP + tubulin GRK2 Homo sapiens ADP + phosphorylated tubulin
-
?
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 ?
-
?
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 ?
-
?
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 ?
-
?

Subunits

Subunits Comment Organism
? x * 80000, GRK2, SDS-PAGE Homo sapiens
? x * 80000, GRK2 catalytic domain, domain structure, overview Mammalia
More domain structure of GRK2, overview Homo sapiens

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 2
-
Homo sapiens
G protein-coupled receptor kinase 3
-
Homo sapiens
GRK2
-
Mammalia
GRK2
-
Homo sapiens
GRK3
-
Homo sapiens
More the enzyme belongs to the beta-adrenergic receptor kinase subfamily Homo sapiens
More the enzyme belongs to the beta-adrenergic receptor kinases subfamily Mammalia

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens