Fig. 6: Arrestin-3 recruitment to inactive β2-adrenergic receptor (β2AR).
From: A small molecule enhances arrestin-3 binding to the β2-adrenergic receptor

HEK293 arrestin2/3 KO cells were co-transfected with plasmids encoding arrestin-3 (A–D) or arrestin-2 (E–H), both with N-terminal SmBiT and β2AR (A, C, E, and G) or M2R (B, D, F, and H) with C-terminal LgBiT. The cells were treated with 100 mM LSH3 or DMSO (vehicle control) for 30 min prior to the addition of luciferase substrate (time point 0). Agonist (10 mM isoproterenol (ISO) for β2AR or 10 mM carbachol for M2R) was added at 30 min. A Arrestin-3 recruitment to β2AR. B Arrestin-3 recruitment to M2R. C Arrestin-3 recruitment to inactive β2AR (no agonist). D Arrestin-3 recruitment to inactive M2R. E Arrestin-2 recruitment to β2AR. F Arrestin-2 recruitment to M2R. G Arrestin-2 recruitment to inactive β2AR. H Arrestin-2 recruitment to inactive M2R. Data are presented as means ± SEM (N = 6). Statistical significance was determined by two-way repeat measures ANOVA followed by Fisher’s LSD post hoc test and indicated, as follows: *, p < 0.05.