Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.15 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
Search for more literature for 2.7.11.15

Activating Compound

Activating Compound Comment Organism Structure
additional information GRK3 bind the Gbetagamma subunit complex, a process that induces activation of the GRKs by phosphorylation Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
co-expression of rat thyrotropin receptor with GRK2 and GRK3 in HEK-293 cells, receptor phosphorylation occurs with both enzymes 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 + beta-adrenergic receptor Homo sapiens in human heart failure, impaired beta-adrenergic receptor signaling compromises cardiac sensitivity to inotropic stimulation, overview ADP + phosphorylated beta-adrenergic 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, selective binding of activated Galphaq and Galpha-11 to RH domains of GRK2 and GRK3 selectively inhibits Gq signaling ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

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

Source Tissue

Source Tissue Comment Organism Textmining
heart GRK3 expression is not increased in heart failure Homo sapiens
-
thyroid gland increased expression of GRK3 in hyperfunctioning thyroid nodule Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + beta-adrenergic receptor
-
 Homo sapiens ADP + phosphorylated beta-adrenergic receptor
-
 ?
ATP + beta-adrenergic receptor in human heart failure, impaired beta-adrenergic receptor signaling compromises cardiac sensitivity to inotropic stimulation, overview Homo sapiens ADP + phosphorylated beta-adrenergic 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, selective binding of activated Galphaq and Galpha-11 to RH domains of GRK2 and GRK3 selectively inhibits Gq signaling Homo sapiens ?
-
 ?
additional information GRK2 interacts with a component of the MAPK pathway, as well as with the PI-3K substrate AKT, GRK2 and GRK3 bind the Gbetagamma subunit complex, a process that induces activation of the GRKs Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 2
-
 Homo sapiens
GRK2
-
 Homo sapiens
GRK3
-
 Homo sapiens
More the enzyme belongs to the GRK2 subfamily, consisting of GRK2, beta-ARK1, GRK3, and beta-ARK2 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens