Extended Data Fig. 6: Quantitative analysis of ibutamoren and AwFw-LL properties on the ghrelin receptor.
From: The structure and function of the ghrelin receptor coding for drug actions
(a-f) Quantitative characterization of the response induced by ibutamoren (a-c) and AwFw-LL (d-f) compared to ghrelin using the in cellulo GEF assay. (a) Normalized BRET responses to the maximum amplitude induced by ghrelin are shown. (b and c) The maximum amplitude (b) and activation rates (c) induced by ibutamoren, presented as fold change in comparison to the ghrelin-induce response, are shown as bar graphs. (d) Normalized BRET responses to the maximum amplitude induced by ghrelin are shown. (e and f) The maximum amplitude (e) and activation rates (f) induced by AwFw-LL, presented as fold change in comparison to the ghrelin-induced response, are shown as bar graphs. The traces represent the mean values of five independent experiments (a and d). Mean ± SEM of five independent experiments are shown (b-c and e-f). ‘N.D.’ indicates not detected (e). Statistical significance was determined by One-Way ANOVA followed by Dunnett multiple comparison test (b and c) and Two-Way ANOVA with Šídák multiple comparison test (e and f), with significance indicated by asterisks (*P < 0.05, **P < 0.01, ***P < 0.001, ****P < 0.0001). Adjusted P values are as follows: 0.0003 for Gq vs. GoA, 0.0290 for Gq vs. G15, and 0.0307 for Gq vs. G13 in panel b; 0.0463 for Gq vs. GoA, 0.0002 for Gq vs. G15, and 0.9907 for Gq vs. G13 in panel c; <0.0001 for GoA, G15, and G13, and 0.0055 for Gq in panel e; 0.0002 for GoA, 0.0034 for Gq, <0.0001 for G15, and 0.0009 for G13 in panel f. "N.D." indicates that the response was not determined (f) due to small responses that could not be accurately quantified for activation rates.
