Figure 5.

Effect of best hits on constitutive activity of the CysLT2R mutant L129Q. (a) Inhibition of IP1 accumulation in HEK293 cells transiently expressing the CysLT2R mutant L129Q. Curves correspond to normalized data: values from non-stimulated cells expressing the WT receptor were set as 0% IP1 production and those from non-stimulated cells expressing the L129Q mutant were set as 100% IP1 production. Data represent mean ± SEM of three independent experiments, tested in quadruplicate. WT = wild-type; NS = non-stimulated. (b) Docking of BRI-12359 to the L129Q mutant. Docking pose of BRI-12359 is shown with cyan carbon atoms representation in grey transparent binding pocket of CysLT2R receptor, and L129Q mutation shown with yellow carbon atoms in CPK presentation.