Feedback inhibition of G protein-coupled receptor kinase 2 (GRK2) activity by extracellular signal-regulated kinases
JA Pitcher, JJG Tesmer, JLR Freeman… - Journal of Biological …, 1999 - ASBMB
G protein-coupled receptor kinase (GRK)-mediated receptor phosphorylation and β-arrestin
binding uncouple G protein-coupled receptors (GPCRs) from their respective G proteins and
initiates the process of receptor internalization. In the case of the β 2-adrenergic receptor
and lysophosphatidic acid receptor, these processes can lead to ERK activation. Here we
identify a novel mechanism whereby the activity of GRK2 is regulated by feedback inhibition.
GRK2 is demonstrated to be a phosphoprotein in cells. Mass spectrometry and mutational …
binding uncouple G protein-coupled receptors (GPCRs) from their respective G proteins and
initiates the process of receptor internalization. In the case of the β 2-adrenergic receptor
and lysophosphatidic acid receptor, these processes can lead to ERK activation. Here we
identify a novel mechanism whereby the activity of GRK2 is regulated by feedback inhibition.
GRK2 is demonstrated to be a phosphoprotein in cells. Mass spectrometry and mutational …
