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. 2024 Jul 3;7:802. doi: 10.1038/s42003-024-06490-1

Fig. 4. bARK-CT reduces β-arrestin2 recruitment to the muscarinic M5 acetylcholine receptor (M5R).

Fig. 4

a Schematic representation of the bARK-CT-mediated mechanism as an inhibitor of GRK2/3 recruitment to the M5R. The bARK-CT fragment of GRK2 includes the GRK2-Gβγ interaction site (R587) and therefore competes with GRK2/3 for the binding. b Halo-Tag-β-arrestin2 recruitment to M5R-NLuc was measured in CRISPR/Cas9 HEK293 control cells, expressing all GRKs at endogenous levels, in absence (empty vector (EV)-transfected) or presence of different co-transfected amounts of bARK-CT (as indicated). Normalized Δ net BRET change (%) upon stimulation with the indicated concentrations of Acetylcholine (ACh) is shown of n = 4 (except 0.5 µg bARK-CT which is n = 3) independent experiments ± SEM, normalized to EV. Statistical differences were tested using one-way ANOVA, followed by a Tukey’s test (ns not significant; *p < 0.05; **p < 0.01). Detailed statistical results are provided in Supplementary Table 13. Comparison of basal and stimulated values can be found in Supplementary Fig. 8.