Fig. 1: Cryo-EM structure of MRGPRX1-Gi1/Gq complexes.
From: Ligand recognition and G protein coupling of the human itch receptor MRGPRX1
a Cryo-EM density map of the BAM8-22-MRGPRX1-Gi1/Gq complexes and CNF-Tx2-MRGPRX1-Gi1 complex. b EM density maps of BAM8-22 in MRGPRX1-Gi1/Gq complexes and CNF-Tx2 in MRGPRX1-Gi1 complex. BAM8-22 in MRGPRX1-Gi1/Gq complexes, hot pink/cyan; CNF-Tx2, light pink; MRGPRX1, cornflower blue, salmon, and medium aquamarine from left to right; Gαi, dark orange; Gαq, yellow; Gβ, wheat; Gγ, light blue; scFv16 (single-chain variable fragment), gray. c Cut-away view of the ligand-binding pocket in the BAM8-22-MRGPRX1-Gi1/Gq, CNF-Tx2-MRGPRX1-Gi1, PAMP-12-MRGPRX2-Gi1 and KCA-CB1-Gi1 complexes. d The binding modes of the peptide agonists of MRGPRX1 compared with MRGPRX2. e The selectivity of different ligands for MRGPRX1 and MRGPRX2 was evaluated using Gαi-Gγ dissociation assay. Data are mean ± SEM of three independent experiments (n = 3). ΔBRET indicates the difference between the BRET signal recorded from cells treated with ligand and that from cells treated with vehicle.
