Molecular insights into the biased signaling mechanism of the μ-opioid receptor

GPCR functional selectivity opens new opportunities for the design of safer drugs. Ligands orchestrate GPCR signaling cascades by modulating the receptor conformational landscape. Our study provides insights into the dynamic mechanism enabling opioid ligands to preferentially activate the G protein...

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Veröffentlicht in:	Molecular cell 2021-10, Vol.81 (20), p.4165-4175.e6
Hauptverfasser:	Cong, Xiaojing, Maurel, Damien, Déméné, Hélène, Vasiliauskaité-Brooks, Ieva, Hagelberger, Joanna, Peysson, Fanny, Saint-Paul, Julie, Golebiowski, Jérôme, Granier, Sébastien, Sounier, Rémy
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics, Opioid - chemistry Analgesics, Opioid - pharmacology Animals beta-Arrestins - genetics beta-Arrestins - metabolism biased agonism Binding Sites Biochemistry, Molecular Biology Computer-Aided Design Drug Design Drug Partial Agonism GPCR HEK293 Cells Humans Life Sciences Ligands Magnetic Resonance Spectroscopy Mice molecular dynamics Molecular Dynamics Simulation Neurobiology Neurons and Cognition NMR opioid Protein Binding Protein Interaction Domains and Motifs Protein Stability Receptors, Opioid, mu - agonists Receptors, Opioid, mu - genetics Receptors, Opioid, mu - metabolism Sf9 Cells Signal Transduction - drug effects Structural Biology Structure-Activity Relationship
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