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Literature summary for 2.7.11.16 extracted from

  • Yang, W.; Xia, S.
    Mechanisms of regulation and function of G-protein-coupled receptor kinases (2006), World J. Gastroenterol., 12, 7753-7757.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
co-expression of rat thyrotropin receptor with GRK4, GRK5, and GRK6 in HEK-293 cells, receptor phosphorylation occurs with GRK5 and GRK6 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + G-protein-coupled receptor Homo sapiens leading to receptor endocytosis ADP + phosphorylated G-protein-coupled receptor
-
?
additional information Homo sapiens GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling and desensitization, beta-arrestin-mediated receptor internalization, activity of GRKs and subcellular targeting is tightly regulated by interaction with receptor domains, G protein subunits, lipids, anchoring proteins and calcium-sensitive proteins ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
multiple splice variants of GRK4 and GRK6
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein GRKs are regulated by phopshorylation Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
brain GRK4 predominantly Homo sapiens
-
heart GRK5 expression is increased in heart failure Homo sapiens
-
kidney GRK4 predominantly Homo sapiens
-
additional information wide tissue distribution of GRK5 and GRK6 Homo sapiens
-
testis GRK4 predominantly Homo sapiens
-
thyroid gland increased expression of GRK4 in hyperfunctioning thyroid nodule Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + G-protein-coupled receptor
-
Homo sapiens ADP + phosphorylated G-protein-coupled receptor
-
?
ATP + G-protein-coupled receptor leading to receptor endocytosis Homo sapiens ADP + phosphorylated G-protein-coupled receptor
-
?
additional information GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling and desensitization, beta-arrestin-mediated receptor internalization, activity of GRKs and subcellular targeting is tightly regulated by interaction with receptor domains, G protein subunits, lipids, anchoring proteins and calcium-sensitive proteins Homo sapiens ?
-
?
additional information no binding to RH domain of G protein Galphaq and Galpha-11 by GRK4 Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
GRK4
-
Homo sapiens
GRK5
-
Homo sapiens
GRK6
-
Homo sapiens
More the enzyme belongs to the GRK4 subfamily, consisting of GRK4, GRK5 and GRK6 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens