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Literature summary extracted from

  • Hansen, J.L.; Theilade, J.; Aplin, M.; Sheikh, S.P.
    Role of G-protein-coupled receptor kinase 2 in the heart--do regulatory mechanisms open novel therapeutic perspectives? (2006), Trends Cardiovasc. Med., 16, 169-177.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.15 additional information GRK2 is activated by phosphorylation through c-Src in a positive feedback reaction, Hsp90 secures proper folding and maturation and protects GRK2 from ubiquitination and proteasomal degradation, it induces GRK2 expression, phosphoinositol kinase 3 binds GRK2 and enhances receptor internalization Homo sapiens
2.7.11.15 PIP2 activates GRK2 through binding to its PH domain Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.15 regulation of GRK2 expression, analysis, overview Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.7.11.15 S670A the GRK2 mutant shows reduced phosphorylation by ERK and is less degraded Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.15 alpha-actinin
-
 Homo sapiens
2.7.11.15 calveolin
-
 Homo sapiens
2.7.11.15 additional information ERK phosphorylates and inhibits GRK2, protein kinase C phosphorylated GRK2 at Ser685 and induces RKIP binding, RKIP binds to GRK2 and inhibits it after it has been phosphorylated by protein kinase C Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.15 plasma membrane recruitment of GRk2 to the plasma membrane is assisted by phospholipids and Gbetagamma proteins binding to the PH domain and another N-terminal site Homo sapiens 5886
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.15 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.15 ATP + angiotensin receptor Homo sapiens phosphorylation by GRK2 preceeds the binding of arrestins, which inhibits the seven-transmembrane receptor, but initiates internalization, overview ADP + phosphorylated angiotensin receptor
-
 ?
2.7.11.15 ATP + beta-adrenergic receptor Homo sapiens phosphorylation by GRK2 preceeds the binding of arrestins, which inhibits the seven-transmembrane receptor, but initiates internalization, overview ADP + phosphorylated beta-adrenergic receptor
-
 ?
2.7.11.15 ATP + epithelial Na+ channel Homo sapiens channel inactivation ADP + phosphorylated epithelial Na+ channel
-
 ?
2.7.11.15 ATP + ezrin Homo sapiens phosphorylation of ezrin affects the 7TM receptor mediated cytoskeletal reorganization ADP + phosphorylated ezrin
-
 ?
2.7.11.15 ATP + PDEgamma Homo sapiens phosphorylation of PDEgamma possibly stimulates EGFR-mediated ERK activation ADP + phosphorylated PDEgamma
-
 ?
2.7.11.15 ATP + PDGFRbeta Homo sapiens
-
 ADP + phosphorylated PDGFRbeta
-
 ?
2.7.11.15 ATP + phosducin Homo sapiens phosducin is activated to inhibit Gbetagamma protein ADP + phosphorylated phosducin
-
 ?
2.7.11.15 ATP + ribosomal protein P2 Homo sapiens activation of P2 ADP + phosphorylated ribosomal protein P2
-
 ?
2.7.11.15 ATP + synuclein Homo sapiens
-
 ADP + phosphorylated synuclein
-
 ?
2.7.11.15 additional information Homo sapiens GRK2 interacts with multiple signaling proteins and is involved in several cellular processes, e.g. expression and regulation of key cardiac seven-transmembrane receptors, 7TM receptors, such as the beta-adrenergic and angiotensin receptors, GRK2 interacts with NCS-1, mechanism, overview, GRK2 inhibition can ameliorate heart failure, molecular mechanism of GRK2 activity regulation, GRK2 is probably involved in regulation of hypertension, overview ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.15 Homo sapiens
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.15 phosphoprotein GRK2 is activated by phosphorylation through c-Src, while phosphorylation by ERK inhibits GRK2 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.15 cardiac myocyte
-
 Homo sapiens
-
2.7.11.15 heart
-
 Homo sapiens
-
2.7.11.15 HEK-293 cell
-
 Homo sapiens
-
2.7.11.15 HL-60 cell
-
 Homo sapiens
-
2.7.11.15 JURKAT cell
-
 Homo sapiens
-
2.7.11.15 lymphocyte
-
 Homo sapiens
-
2.7.11.15 additional information the enzyme is ubiquitously expressed, developmental regulation of GRK2 expression, overview Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.15 ATP + angiotensin receptor
-
 Homo sapiens ADP + phosphorylated angiotensin receptor
-
 ?
2.7.11.15 ATP + angiotensin receptor phosphorylation by GRK2 preceeds the binding of arrestins, which inhibits the seven-transmembrane receptor, but initiates internalization, overview Homo sapiens ADP + phosphorylated angiotensin receptor
-
 ?
2.7.11.15 ATP + beta-adrenergic receptor
-
 Homo sapiens ADP + phosphorylated beta-adrenergic receptor
-
 ?
2.7.11.15 ATP + beta-adrenergic receptor phosphorylation by GRK2 preceeds the binding of arrestins, which inhibits the seven-transmembrane receptor, but initiates internalization, overview Homo sapiens ADP + phosphorylated beta-adrenergic receptor
-
 ?
2.7.11.15 ATP + epidermal growth factor receptor
-
 Homo sapiens ADP + phosphorylated epidermal growth factor receptor
-
 ?
2.7.11.15 ATP + epithelial Na+ channel
-
 Homo sapiens ADP + phosphorylated epithelial Na+ channel
-
 ?
2.7.11.15 ATP + epithelial Na+ channel channel inactivation Homo sapiens ADP + phosphorylated epithelial Na+ channel
-
 ?
2.7.11.15 ATP + ezrin
-
 Homo sapiens ADP + phosphorylated ezrin
-
 ?
2.7.11.15 ATP + ezrin phosphorylation of ezrin affects the 7TM receptor mediated cytoskeletal reorganization Homo sapiens ADP + phosphorylated ezrin
-
 ?
2.7.11.15 ATP + PDEgamma
-
 Homo sapiens ADP + phosphorylated PDEgamma
-
 ?
2.7.11.15 ATP + PDEgamma phosphorylation of PDEgamma possibly stimulates EGFR-mediated ERK activation Homo sapiens ADP + phosphorylated PDEgamma
-
 ?
2.7.11.15 ATP + PDGFRbeta
-
 Homo sapiens ADP + phosphorylated PDGFRbeta
-
 ?
2.7.11.15 ATP + phosducin
-
 Homo sapiens ADP + phosphorylated phosducin
-
 ?
2.7.11.15 ATP + phosducin phosducin is activated to inhibit Gbetagamma protein Homo sapiens ADP + phosphorylated phosducin
-
 ?
2.7.11.15 ATP + ribosomal protein P2
-
 Homo sapiens ADP + phosphorylated ribosomal protein P2
-
 ?
2.7.11.15 ATP + ribosomal protein P2 activation of P2 Homo sapiens ADP + phosphorylated ribosomal protein P2
-
 ?
2.7.11.15 ATP + synuclein
-
 Homo sapiens ADP + phosphorylated synuclein
-
 ?
2.7.11.15 ATP + tubulin
-
 Homo sapiens ADP + phosphorylated tubulin
-
 ?
2.7.11.15 additional information GRK2 interacts with multiple signaling proteins and is involved in several cellular processes, e.g. expression and regulation of key cardiac seven-transmembrane receptors, 7TM receptors, such as the beta-adrenergic and angiotensin receptors, GRK2 interacts with NCS-1, mechanism, overview, GRK2 inhibition can ameliorate heart failure, molecular mechanism of GRK2 activity regulation, GRK2 is probably involved in regulation of hypertension, overview Homo sapiens ?
-
 ?
2.7.11.15 additional information GRK2 binds to and inhibits Galphaq protein via its N-terminal RGS domain, GRK2 interacts with NCS-1 Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.15 beta-adrenergic receptor kinase
-
 Homo sapiens
2.7.11.15 G-protein-coupled receptor kinase 2
-
 Homo sapiens
2.7.11.15 GRK2
-
 Homo sapiens
2.7.11.15 More the enzyme belongs to the G-protein-coupled receptor kinase family Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.15 ATP
-
 Homo sapiens