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Literature summary for 2.7.11.15 extracted from

  • Wang, J.; Liu, X.J.
    A G protein-coupled receptor kinase induces Xenopus oocyte maturation (2003), J. Biol. Chem., 278, 15809-15814.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
beta-arrestin-2 forms a complex with GRK3 causing G protein-coupled receptor desensitization Rattus norvegicus

Cloned(Commentary)

Cloned (Comment) Organism
functional expression of HA-tagged wild-type and mutant GRK3, and coexpression with beta-arrestin-2, in Xenopus laevis oocytes via injection of mRNA, leads to induction of maturation of the oocytes Rattus norvegicus

Protein Variants

Protein Variants Comment Organism
K220R site-directed mutagenesis, kinase-dead mutant of GRK3, the mutant is unable to induce germinal vesicle breakdown Rattus norvegicus
additional information truncated GRK3DELTAC lacking the C-terminal Gbetagamma binding domain is unable to induce germinal vesicle breakdown, and is defective in membrane association Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
concanavalin A inhibitor of clathrin-mediated receptor endocytosis via clathrin binding domain of beta-arrestin-2, inhibitor reduces the GRK3/beta-arrestin-2 induction activity of germinal vesicle breakdown Rattus norvegicus
monodansyl cadaverin inhibitor of clathrin-mediated receptor endocytosis via clathrin binding domain of beta-arrestin-2, inhibitor reduces the GRK3/beta-arrestin-2 induction activity of germinal vesicle breakdown Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane associated with, membrane association is required for activity on G protein-coupled receptors, and mediated by the C-terminal Gbetagamma binding domain Rattus norvegicus 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Rattus norvegicus
Mn2+
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + G protein-coupled receptor Rattus norvegicus
-
ADP + phosphorylated G protein-coupled receptor
-
?
additional information Rattus norvegicus GRK3 is essential for induction of germinal vesicle breakdown, GRK3 forms a complex with beta-arrestin-2 causing G protein-coupled receptor desensitization ?
-
?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + beta-casein recombinant HA-tagged wild-type and mutant GRK3 Rattus norvegicus ADP + phosphorylated beta-casein
-
?
ATP + G protein-coupled receptor
-
Rattus norvegicus ADP + phosphorylated G protein-coupled receptor
-
?
ATP + myelin basic protein recombinant HA-tagged wild-type and mutant GRK3 Rattus norvegicus ADP + phosphorylated myelin basic protein
-
?
additional information GRK3 is essential for induction of germinal vesicle breakdown, GRK3 forms a complex with beta-arrestin-2 causing G protein-coupled receptor desensitization Rattus norvegicus ?
-
?

Subunits

Subunits Comment Organism
More GRK3 wild-type and mutant domain structures, overview Rattus norvegicus

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 3
-
Rattus norvegicus
GRK3
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.3
-
assay at Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Rattus norvegicus