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Literature summary for 2.7.11.15 extracted from

  • Picascia, A.; Capobianco, L.; Iacovelli, L.; De Blasi, A.
    Analysis of differential modulatory activities of GRK2 and GRK4 on Galphaq-coupled receptor signaling (2004), Methods Enzymol., 390, 337-353.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
G protein interaction via GRK2 N-terminal RGS domain, binding of free Gbetagamma subunits initiates GRK2 translocation from cytosol to the plasma membrane and its activation for receptor phosphorylation Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of kinase-dead GRK2 mutant and of the N-terminal region of GRK2, residues Ala2-Thr187, in HEK-293 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
K220R site-directed mutagenesis, kinase-dead GRK2 mutant, overexpression in HEK-293 cells leads to partially desensitization of G protein-coupled receptor Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-
membrane
-
Homo sapiens 16020
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the enzyme is involved in G protein-coupled receptor signal transduction pathways and desensitization, GRK2 is a multiple domain kinase regulating by multiple mechanisms, overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
no splicing variants of GRK2
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme is involved in G protein-coupled receptor signal transduction pathways and desensitization, GRK2 is a multiple domain kinase regulating by multiple mechanisms, overview Homo sapiens ?
-
?
additional information GRK2 interacts with calmodulin, substrate specificity, GRK2 phosphorylates serine and threonine residues with preceeding acidic amino acid residues Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
More GRK family domain structure, the N-terminal RGS domain of GRK2 has regulatory function on G protein binding and receptor phosphorylation and activity, overview Homo sapiens

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 2
-
Homo sapiens
GPCR kinase
-
Homo sapiens
GRK2
-
Homo sapiens
More the enzyme belongs to the betaARK subfamily of the GRK family Homo sapiens