Extended Data Fig. 9: Impact of N3057.35K mutations on drug actions.
From: The structure and function of the ghrelin receptor coding for drug actions
(a) Assay design to examine the antagonist/inverse agonist action of the N3057.35K mutant compared to the wild-type ghrelin receptor. (b-i) Effects of JMV 2959, PF-05190457, YIL 781, or CDP21 on wild-type ghrelin receptor (b, d, f, and h) and N3057.35K mutant (c, e, g, and i). Transfected cells were pre-incubated with 100 μM JMV 2959, 10 μM PF-05190457, 10 μM YIL 781, or 32 μM CPD21 for 1 min and then stimulated with 10 μM anamorelin. The traces represent the mean values of three independent experiments. Mean ± SEM are presented as bar graphs. Statistical significance was determined by unpaired two-tailed t test, with significance indicated by asterisks (*P < 0.05, **P < 0.01, ***P < 0.001, ****P < 0.0001). Adjusted P values are as follows: 0.0004 (b), 0.0005 (c), <0.0001 (d), 0.0009 (e), <0.0001 (f), 0.1809 (g), and <0.0001 (h). (j) Comparison of the chemical structures of YIL 781 and CPD21. (k) Binding modes of N3057.35 and CPD21 or PF-05190457.
