Literature summary for 2.7.10.1 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.

Search for more literature for 2.7.10.1

Cloned(Commentary)

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

Protein Variants

Protein Variants	Comment	Organism
Y740F/Y751F	site-directed mutagenesis, reduced activity with GRK2 compared to the wild-type enzyme, the mutant cannot recruit phosphoinositide 3-kinase	Homo sapiens
Y857F	site-directed mutagenesis, mutant shows reduced sensitivity to GRK2 inhibitory phosphorylation compared to the wild-type PDGFRbeta	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
G protein-coupled receptor kinase-2	platelet-derived growth factor-dependent GRK2 phosphorylation desensitizes the PDGF receptor-beta	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + G protein-coupled receptor kinase-2	Homo sapiens	GRK2 activation also increases GRK2 degradation and downregulation, independent of Gbetagamma subunits and phosphoinositide 3-kinase	ADP + phosphorylated G protein-coupled receptor kinase-2	-	?
additional information	Homo sapiens	PDGFRbeta wild-type and mutant Y857F activate c-Src kinase	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
phosphoprotein	PDGFRbeta is phosphorylated by GRK2, and autophosphorylated	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + G protein-coupled receptor kinase-2	GRK2 activation also increases GRK2 degradation and downregulation, independent of Gbetagamma subunits and phosphoinositide 3-kinase	Homo sapiens	ADP + phosphorylated G protein-coupled receptor kinase-2	-	?
ATP + G protein-coupled receptor kinase-2	activates GRK2 by tyrosine phosphorylation at Y13, Y86, and Y92, the wild-type PDGFRbeta is 60fold more active with GRK2 than PDGFRbeta mutant Y857F, independent of Gbetagamma subunits and phosphoinositide 3-kinase	Homo sapiens	ADP + phosphorylated G protein-coupled receptor kinase-2	-	?
additional information	PDGFRbeta wild-type and mutant Y857F activate c-Src kinase	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
PDGFRbeta	-	Homo sapiens
platelet-derived growth factor receptor-beta	-	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

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Release 2023.1 (January 2023)