Figure 1: Screen for inhibitors of the interaction between β2-adaptin and β-arrestin. | Nature Communications

Figure 1: Screen for inhibitors of the interaction between β2-adaptin and β-arrestin.

From: A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling

Figure 1

(a) Flowchart outlining the steps of the virtual screening and the selection of candidate molecules to be tested. (b) Schematic representation and dynamic range of the BRET-based assay used to test the compounds selected from the virtual screen that monitors the β2-adaptin/β-arrestin1 interaction. HEK293T cells were transfected with β2-adaptin-YFP, β-arrestin1-RlucII and myc-V2R. BRET was measured following V2R stimulation with 100 nM AVP for 45 min. Data are the mean±s.e.m. of three independent experiments. Statistical analysis was performed using a paired Student’s test (***P<0.001). (c) β2-adaptin/β-arrestin1 interaction was assessed as described in (b) with AVP-stimulation following pre-incubation with the indicated compounds (100 μM) for 25 min. Data are the mean±s.e.m. of three independent experiments. One-way ANOVA followed by Tuckey’s post-hoc tests were used to assess the statistical significance of the compound-induced BRET modulation compared to DMSO (***P<0.001).

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