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- W615125544 abstract "G protein-coupled receptor (GPCR) kinases (GRKs) desensitize GPCRs by phosphorylating agonist-occupied receptors. GRK kinase activity is stimulated by interaction with activated receptors. The GRK 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 allosteric activation. Expanded mutagenesis of the αN and AST allowed us to further assess the role of these regions in kinase activation and receptor phosphorylation, in vitro and in intact cells. We also developed a bioluminescence resonance energy transfer (BRET)-based assay to monitor the recruitment of GRK2 to activated α2A-adrenergic receptors (α2A-ARs) in living cells. The BRET assay allowed us to distinguish GRK2 recruitment to Gβγ versus α2A-AR. We suggest that one surface of GRK2 αN directly interacts with receptors, whereas the opposite face and three AST residues are more important for kinase domain closure and activation. Taken together with data on GRK1 and GRK6, our data suggests that all three GRK subfamilies make conserved interactions with GPCRs, but there may be unique interactions that influence selectivity. Funding: NSF (RSM), NIH (JT), Canadian Institute for Health Research (MB), and FRSQ & Groupe de Recherche Universitaire sur le Médicament (AB)." @default.
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- W615125544 date "2015-04-01" @default.
- W615125544 modified "2023-10-01" @default.
- W615125544 title "Mapping G Protein‐coupled Receptor (GPCR) Docking Site on GPCR Kinase 2: New Insights from Intact Cell Studies" @default.
- W615125544 doi "https://doi.org/10.1096/fasebj.29.1_supplement.893.2" @default.
- W615125544 hasPublicationYear "2015" @default.
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