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Literature summary for 2.7.11.16 extracted from

  • Kohout, T.A.; Lefkowitz, R.J.
    Regulation of G protein-coupled receptor kinases and arrestins during receptor desensitization (2003), Mol. Pharmacol., 63, 9-18.
    View publication on PubMed
Search for more literature for 2.7.11.16

Activating Compound

Activating Compound Comment Organism Structure
arrestins arrestins modulate the enzyme activity having a regulatory role, regulation of arrestins, overview Mus musculus
additional information autophosphorylation of GRK5 is stimulated by phospholipids, such as phosphatidylinositol-4,5-bisphosphate Mus musculus

Protein Variants

Protein Variants Comment Organism
additional information phenotypes of several GRK and arrestin knockout mice mutants and of transgenic mice overexpressing GRK4 or GRK5, overview Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
Ca2+/calmodulin inhibit GRK5 with an IC50 of 40-50 nM, inhibition mechanism via inducing inhibitory autophosphorylation and blocking of membrane association Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
plasma membrane constitutive association, location of GRK4-6 near the activated receptors, covalent attachment by fatty acids to the C-terminus, e.g. palmitoylated GRK4 and GRK6, or by electrostatic interactions with phospholipids, e.g. for GRK5 Mus musculus 5886
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + beta-adrenergic receptor Mus musculus desensitization of the receptor by GRK4, GRK5, and GRK6 ADP + phosphorylated beta-adrenergic receptor
-
 ?
ATP + G protein-coupled receptor Mus musculus phosphorylation has a regulatory role ADP + phosphorylated G protein-coupled receptor
-
 ?
additional information Mus musculus G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview ?
-
 ?

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
lipoprotein GRK4-6 are permanently modulated by fatty acids and/or phospholipids Mus musculus
phosphoprotein regulation of GRK5 by phosphorylation through PKC, GRK5 is activated by autophosphorylation, autophosphorylation is stimulated by phospholipids, such as phosphatidylinositol-4,5-bisphosphate, overview Mus musculus

Purification (Commentary)

Purification (Comment) Organism
GRK2 by gel filtration from Sf9 cells Mus musculus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + beta-adrenergic receptor desensitization of the receptor by GRK4, GRK5, and GRK6 Mus musculus ADP + phosphorylated beta-adrenergic receptor
-
 ?
ATP + G protein-coupled receptor phosphorylation has a regulatory role Mus musculus ADP + phosphorylated G protein-coupled receptor
-
 ?
ATP + G protein-coupled receptor the GPCRs possess multiple phosphorylation sites for serine/threonine kinases Mus musculus ADP + phosphorylated G protein-coupled receptor
-
 ?
additional information G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview Mus musculus ?
-
 ?
additional information the GRKs are specific for GPCRs and arrestins, overview Mus musculus ?
-
 ?

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 4
-
 Mus musculus
G protein-coupled receptor kinase 5
-
 Mus musculus
GRK4
-
 Mus musculus
GRK5
-
 Mus musculus

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004 0.00005 inhibit GRK5 with an IC50 of 40-50 nM, inhibition mechanism via inducing inhibitory autophosphorylation and blocking of membrane association Mus musculus Ca2+/calmodulin