Article
G protein-coupled receptor kinases (GRKs) orchestrate biased agonism at the β2-adrenergic receptor.
Science signaling - 21 Aug 2018
Choi Minjung, Staus Dean P, Wingler Laura M, Ahn Seungkirl, Pani Biswaranjan, Capel William D, Lefkowitz Robert J
Abstract excerpt
Biased agonists of G protein-coupled receptors (GPCRs), which selectively activate either G protein- or β-arrestin-mediated signaling pathways, are of major therapeutic interest because they have the potential to show improved efficacy and specificity as drugs. Efforts to understand the mechanistic basis of this phenomenon have focused on the hypothesis that G proteins and β-arrestins preferentially couple to...
Topics
- Cell Line, Tumor
- Extracellular Signal-Regulated MAP Kinases
- G-Protein-Coupled Receptor Kinases
- GTP-Binding Proteins
- HEK293 Cells
- Humans
- Mutation
- Phosphorylation
- Receptors, Adrenergic, beta-2
- Receptors, G-Protein-Coupled
- Signal Transduction
- beta-Arrestins
