Fig. 6. I-287 has no effect on βarrestin2 recruitment and PAR2 internalization.

a Impact of increasing concentrations of I-287 (15 min) on βarrestin2 recruitment at the plasma membrane induced by an EC₈₀ concentration of hTrypsin or SLIGKV-NH₂ (15 min) in HEK293 cells co-expressing hPAR2 and the ebBRET sensors βarrestin2–RlucII/rGFP-CAAX. Results are expressed as ΔBRET in % of the response induced by EC₈₀ of respective agonists in the absence of I-287 (mean ± SEM; n = 5). b Schematic representation of receptor internalization BRET-based biosensor using the hPAR2-RlucII and rGFP-CAAX sensors to monitor loss of hPAR2 from cell surface. c Impact of I-287 (1 µM, 15 min) on hPAR2 internalization kinetics induced by an EC₈₀ concentration of hTrypsin or SLIGKV-NH₂ in HEK293 cells expressing the hPAR2-RlucII/rGFP-CAAX sensors. Results are expressed as BRET² ratio of absolute values (mean ± SEM; n = 3).