Biased Signaling of the G-Protein-Coupled Receptor β 2 AR Is Governed by Conformational Exchange Kinetics
Structure, ISSN: 0969-2126, Vol: 28, Issue: 3, Page: 371-377.e3
2020
- 37Citations
- 89Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations37
- Citation Indexes37
- 37
- CrossRef12
- Captures89
- Readers89
- 89
Article Description
G-protein-coupled receptors (GPCRs) mediate a wide range of human physiological functions by transducing extracellular ligand binding events into intracellular responses. GPCRs can activate parallel, independent signaling pathways mediated by G proteins or β-arrestins. Whereas “balanced” agonists activate both pathways equally, “biased” agonists dominantly activate one pathway, which is of interest for designing GPCR-targeting drugs because it may mitigate undesirable side effects. Previous studies demonstrated that β-arrestin activation is associated with transmembrane helix VII (TM VII) of GPCRs. Here, single-molecule fluorescence spectroscopy with the β 2 -adrenergic receptor (β 2 AR) in the ligand-free state showed that TM VII spontaneously fluctuates between one inactive and one active-like conformation. The presence of the β-arrestin-biased agonist isoetharine prolongs the dwell time of TM VII in the active-like conformation compared with the balanced agonist formoterol, suggesting that ligands can induce signaling bias by modulating the kinetics of receptor conformational exchange.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0969212620300010; http://dx.doi.org/10.1016/j.str.2020.01.001; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85079892907&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/31978323; https://linkinghub.elsevier.com/retrieve/pii/S0969212620300010; https://dx.doi.org/10.1016/j.str.2020.01.001
Elsevier BV
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