Article
Mapping the putative G protein-coupled receptor (GPCR) docking site on GPCR kinase 2: insights from intact cell phosphorylation and recruitment assays.
The Journal of biological chemistry - 5 Sept 2014
Beautrait Alexandre, Michalski Kevin R, Lopez Thomas S, Mannix Katelynn M, McDonald Devin J, Cutter Amber R, Medina Christopher B, Hebert Aaron M, Francis Charnelle J, Bouvier Michel, Tesmer John J G, Sterne-Marr Rachel
Abstract excerpt
G protein-coupled receptor kinases (GRKs) phosphorylate agonist-occupied receptors initiating the processes of desensitization and β-arrestin-dependent signaling. Interaction of GRKs with activated receptors serves to stimulate their kinase activity. The extreme N-terminal helix (αN), the kinase small lobe, and the active site tether (AST) of the AGC kinase domain have previously been implicated in mediating the...
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