FIGURE 1.

Effect of LMW allosteric compounds of FSHR to activate cAMP signaling (A) Chemical structures of compounds used in this study: the benzamide B3 and the thiazolidinone derivates T1 and T2. (B) Intracellular cAMP levels measured in cells transiently transfected with the cAMP BRET sensor CAMYEL and FSHR stimulated with increasing concentrations of FSH, B3 or T1. For each concentration considered, the area under the curve (AUC) was extrapolated from the signal recorded following 20 min stimulation and plotted as concentration/activity curves. Concentrations of FSH were −12.5 to −6.5 log M while B3 and T1 were −10 to −4 log M, at half-log dilutions. Data were normalized considering FSH maximal response as 100%. n = 6 independent experiments. (C) Intracellular levels of cAMP measured via HTRF in cells expressing FLAG-FSHR and stimulation with either DMSO, FSH (10 nM), B3, T1 or T2 (10 μM) for 5 min. n = 4 independent experiments; One-way ANOVA: **p < 0.01, ***p < 0.001.