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. 2023 Apr 10;14:2005. doi: 10.1038/s41467-023-37233-1

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Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Fig. 3 — a A schematic model outlines the ligand efficacy-dependent influence on the dynamics of TM6. A hallmark of GPCR activation by different agonists is an outward movement of TM6. Gs coupling requires disruption of interactions between the CT and the cytoplasmic core of the β₂AR. b Ligand efficacy-dependent influence on the smFRET efficiency distribution of 148C-378C. All experiments were done in the presence of 10 μM Gs^GDP, and saturating concentrations of ligands. The stabilization of the low-FRET state correlates with agonist efficacy. c The positive correlation between low-FRET occupancy and ligand efficacy (measured by a GTP turnover assay). The statistics of GTP turnover results are mean±s.d. of 3 independent experiments, and the statistics of low-FRET occupancy are mean±s.d. of 2 independent experiments. d The concentration titration experiments to evaluate the coupling of Gs^GDP to the agonist-occupied receptor in the absence or presence of the PAM (cmpd-6). The dashed rectangular box indicates the control condition without Gs^GDP. e The concentration titration experiments to evaluate the coupling ability of Gs^GDP to the agonist-occupied receptor in the absence or presence of the NAM (cmpd-15). Bars and error bars in (d) and (e) represent mean±s.e.m. of 3 independent samples.