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

Figure 3.

Figure 3

Prearranged PAMs modify GLP‐1 binding kinetics. a) GLP‐1‐FITC residence time (=1/ dissociation rate constant k off) at surface SNAP‐GLP‐1R after pre‐incubation with PAM or prearranged PAM, determined by non‐linear regression of GLP‐1‐FITC binding data15 (n=7). b) As for (a), but association rate constant (k on). c) Effect of PAMs and prearranged PAMs on affinity constants (K d) for GLP‐1‐FITC (n=7). d) Schematic showing the endosomal binding protocol. e) Representative images demonstrating complete internalization of surface‐labeled SNAP‐GLP‐1R by, and co‐localization with, 100 nμ GLP‐1‐FITC (n=2) (scale bars; 8 μm). f) Effect of PAMs and prearranged PAMs on endosomal GLP‐1‐FITC dissociation after complete SNAP‐GLP‐1R internalization, agonist washout, and compound application in the presence of exendin(9–39) (n=5). g) AUC from (f) relative to zero baseline. *P<0.05; one‐way randomized block ANOVA followed by Sidak's post‐hoc test. Values represent the mean + or ± SEM. PAMs or prearranged PAMs were applied at 10 μμ.