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Literature summary for 2.7.11.15 extracted from

  • Wu, J.H.; Goswami, R.; Kim, L.K.; Miller, W.E.; Peppel, K.; Freedman, N.J.
    The platelet-derived growth factor receptor-beta phosphorylates and activates G protein-coupled receptor kinase-2. A mechanism for feedback inhibition (2005), J. Biol. Chem., 280, 31027-31035.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
platelet-derived growth factor receptor-beta activates the enzyme by tyrosine phosphorylation at Y13, Y86, and Y92, required, the wild-type PDGFRbeta is 60fold more active with GRK2 than PDGFRbeta mutant Y857F, GRK2 activation also increases GRK2 degradation and downregulation, independent of Gbetagamma subunits and phosphoinositide 3-kinase Bos taurus

Cloned(Commentary)

Cloned (Comment) Organism
expression of HA-tagged GRK2 wild-type and mutants and of FLAG-tagged platelet-derived growth factor receptor-beta wild-type and mutants in HEK-293 cells Bos taurus

Protein Variants

Protein Variants Comment Organism
Y13F site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is reduced with the mutant GRK2, reduced activity compared to the wild-type Bos taurus
Y13F/Y86F/Y92F site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is eliminated with the mutant GRK2, reduced activity compared to the wild-type Bos taurus
Y86F site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is reduced with the mutant GRK2, reduced activity compared to the wild-type Bos taurus
Y86F/Y92F site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is highly reduced with the mutant GRK2, reduced activity compared to the wild-type Bos taurus
Y92F site-directed mutagenesis, required activating tyrosine phosphorylation by platelet-derived growth factor receptor-beta kinase activity is reduced with the mutant GRK2, reduced activity compared to the wild-type Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
additional information platelet-derived growth factor receptor-beta activates the enzyme by tyrosine phosphorylation, the wild-type PDGFRbeta is 60fold more active with GRK2 than PDGFRbeta mutant Y857F, GRK2 activation also increases GRK2 degradation and downregulation Bos taurus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + platelet-derived growth factor receptor-beta Bos taurus feedback inhibition mechanism, overview ADP + phosphorylated platelet-derived growth factor receptor-beta
-
?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein
-
Bos taurus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + platelet-derived growth factor receptor-beta feedback inhibition mechanism, overview Bos taurus ADP + phosphorylated platelet-derived growth factor receptor-beta
-
?
ATP + platelet-derived growth factor receptor-beta active with the wild-type and mutant Y740F/Y751F PDGFRbeta, GRK2 phosphorylation desensitizes the PDGF receptor-beta, feedback inhibition mechanism, overview Bos taurus ADP + phosphorylated platelet-derived growth factor receptor-beta
-
?

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
ATP
-
Bos taurus