Fig. 1: Cryo-EM structures of GPR88-Gi1 in the apo and 2-PCCA-bound forms.
From: Activation and allosteric regulation of the orphan GPR88-Gi1 signaling complex
a The chemical structure of 2-PCCA. b NanoBiT G-protein dissociation assay. Concentration–response curves of the G-protein dissociation signals for the indicated G-protein members. Symbols and error bars represent mean and s.e.m. of 3 (Gs), 4 (Gq, G13), and 6 (Gi1) independent experiments, each performed in duplicate. c Coupling of apo-state GPR88 or 2-PCCA bound GPR88 with Gi1 measured by GTPase Glo assay using purified proteins in detergent micelles. Error bars denote mean and s.e.m. of five independent experiments with repeats in triplicate. Statistical analyses were performed using the ordinary one-way ANOVA. ***p < 0.001; ****p < 0.0001. d, e Cryo-EM maps and structural models of GPR88-Gi1 signaling complex in the absence (d) or presence (e) of 2-PCCA.
