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. 2022 Nov 17;13:7033. doi: 10.1038/s41467-022-34696-6

Fig. 3. Agonist interactions in GPR119 ligand-binding pocket.

Fig. 3

a–f Ligand-receptor interactions in stacking gate (a, d) between GPR119 and AR231453 (a) or MBX- 2982 (d), in extracellular cavity (b, e) between GPR119 and AR231453 (b) or MBX-2982 (e), and in activation cavity (c, f) between GPR119 and AR231453 (c) or MBX-2982 (f). g Superimposition of OEA with AR231453 and MBX-2982 in GPR119 ligand-binding pocket. h, i Ligand-receptor interactions in extracellular cavity and stacking gate between GPR119 and OEA of the docking model (h) and in activation cavity (i). j cAMP accumulation of GPR119 induced by agonist AR231453, MBX-2982 and OEA. (EC50 ratio = EC50 of mutant/EC50 of wild type) and maximal agonist response (span for cAMP accumulation) for each mutant relative to the wild-type receptor are shown according to the extent of effect. Data are from at least three independent experiments performed in technical triplicate. For AR231453/MBX-2982-induced cAMP accumulation, WT were repeated 18 times. For OEA-induced cAMP accumulation, WT were repeated 6 times. Other mutants were all repeated 3 times. *P < 0.01; ***P < 0.0001 by one-way ANOVA followed by Dunnett’s post-test, compared with the response of the WT. ND (not determined) refers to data where a robust concentration response curve could not be established within the concentration range tested). A detailed statistical evaluation is provided in Supplementary Tables 2 and 4. Source data are available as a Source Data file.