Fig. 6: β-arrestin2 recruitment to D3R mono- and D3R-NTSR1 coexpressing HEK293 cells indicates a specific effect of the bivalent ligands. | Communications Biology

Fig. 6: β-arrestin2 recruitment to D3R mono- and D3R-NTSR1 coexpressing HEK293 cells indicates a specific effect of the bivalent ligands.

From: Bivalent ligands promote endosomal trafficking of the dopamine D3 receptor-neurotensin receptor 1 heterodimer

Fig. 6: β-arrestin2 recruitment to D3R mono- and D3R-NTSR1 coexpressing HEK293 cells indicates a specific effect of the bivalent ligands.

The DiscoverX enzyme fragment complementation assay allows detection of β-arrestin2 recruitment to a GPCR that is C-terminally tagged with the ProLink fragment. a No β-arrestin2 recruitment to D3R-ProLink was detected after stimulation with quinpirole or compounds 1a-d (individual data points, n = 2 independent experiments). b Coexpression of wild-type NTSR1 does not alter β-arrestin2 recruitment to D3R-Prolink upon stimulation with quinpirole (n = 3). NT(8-13) induces a concentration dependent response (EC50 1.5 ± 0.4 nM, n = 8). c, d Stimulation with type 1 and 2 bivalent ligands results in bell-shaped concentration-response curves in D3R-ProLink-NTSR1 coexpressing cells (n = 4 for 1a-c, 2b and n = 3 for 1d, 2a,c,d). b Prevention of the bivalent binding mode by high concentrations of haloperidol (1 µM, 30 min preincubation, n = 3) reduces β-arrestin2 recruitment close to the level of NT(8-13) alone. Error bars denote s.e.m. of n independent experiments.

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