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. 2017 Jun 5;6(4):501–505. doi: 10.1002/open.201700062

Figure 2.

Figure 2

Prearranged PAMs potently enhance GLP‐1R signaling. a) Allosteric enhancement of GLP‐1(9–36)NH2 (“9–36”) cAMP responses (30 min incubation; n=4) (4‐parameter logistic fit shown). b) As for (a), but with exendin(9–39) (ex9‐39) (n=5). c) Allosteric enhancement of 10 μμ GLP‐1(9–36)NH2‐induced β‐arrestin2 (βarr2) recruitment (30 min incubation; n=5). d) cAMP responses to indicated PAM or prearranged PAM concentration in the absence of orthosteric ligand (30 min incubation; n=3). e) Cytosolic Ca2+ responses in Calcium 6 dye‐loaded cells, expressed relative to baseline fluorescent signal (60 min incubation; n=7). f) Area under curve (AUC) determined from (e). *P<0.05, **P<0.01, ***P<0.001; one‐ or two‐way randomized block ANOVA followed by either Sidak's or Tukey's post‐hoc test. Values represent the mean + or ± SEM. Except where indicated, PAMs or prearranged PAMs were applied at 10 μμ.