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Literature summary for 2.7.11.15 extracted from

  • Kim, K.M.; Gainetdinov, R.R.; Laporte, S.A.; Caron, M.G.; Barak, L.S.
    G protein-coupled receptor kinase regulates dopamine D3 receptor signaling by modulating the stability of a receptor-filamin-beta-arrestin complex. A case of autoreceptor regulation (2005), J. Biol. Chem., 280, 12774-12780.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
beta-arrestin2 mediates GRK activity, forms a signaling complex with filamin and dopamine D3 receptor, interactions, overview Bos taurus

Cloned(Commentary)

Cloned (Comment) Organism
overexpression of GRK2 in HEK-293 cells and in COS-7 cells, co-expression with FLAG-tagged dopamine D3 receptor, and filamin A and/or beta-arrestin, recombinant beta-arrestin is accumulated in the plasma membrane in presence of GRK2 and absence of agonist Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
quinpirole inhibits GRK2 and GRK3 Bos taurus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + dopamine D3 receptor Bos taurus the receptor is activated by GRK2 and GRK3 phosphorylation involving beta-arrestins, GRK-mediated regulation of receptor-filamin complex stability and receptor-G protein signaling potential, GRK2 reduces the dopamine D3 receptor signaling, overview ADP + phosphorylated dopamine D3 receptor
-
?
additional information Bos taurus dopamine D3 receptor binds to G proteins, the coupling is regulated by the filamin expression level ?
-
?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + dopamine D3 receptor
-
Bos taurus ADP + phosphorylated dopamine D3 receptor
-
?
ATP + dopamine D3 receptor the receptor is activated by GRK2 and GRK3 phosphorylation involving beta-arrestins, GRK-mediated regulation of receptor-filamin complex stability and receptor-G protein signaling potential, GRK2 reduces the dopamine D3 receptor signaling, overview Bos taurus ADP + phosphorylated dopamine D3 receptor
-
?
additional information dopamine D3 receptor binds to G proteins, the coupling is regulated by the filamin expression level Bos taurus ?
-
?

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 2
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Bos taurus
G protein-coupled receptor kinase 3
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Bos taurus
GRK2
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Bos taurus
GRK3
-
Bos taurus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Bos taurus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information
-
Bos taurus