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- W4309263586 abstract "Abstract Agonists selectively targeting cannabinoid receptor-like G-protein-coupled receptor (GPCR) GPR119 hold promise for treating metabolic disorders while avoiding unwanted side effects. Here we present the cryo-electron microscopy (cryo-EM) structures of the human GPR119-G s signaling complexes bound to AR231453 and MBX-2982, two representative agonists reported for GPR119. The structures reveal a one-amino acid shift of the conserved proline residue of TM5 that forms an outward bulge, opening up a hydrophobic cavity between TM4 and TM5 at the middle of the membrane for its endogenous ligands-monounsaturated lipid metabolites. In addition, we observed a salt bridge between ICL1 of GPR119 and Gβ s . Disruption of the salt bridge eliminates the cAMP production of GPR119, indicating an important role of Gβ s in GPR119-mediated signaling. Our structures, together with mutagenesis studies, illustrate the conserved binding mode of the chemically different agonists, and provide insights into the conformational changes in receptor activation and G protein coupling." @default.
- W4309263586 created "2022-11-25" @default.
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- W4309263586 date "2022-11-17" @default.
- W4309263586 modified "2023-10-05" @default.
- W4309263586 title "Activation and signaling mechanism revealed by GPR119-Gs complex structures" @default.
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- W4309263586 doi "https://doi.org/10.1038/s41467-022-34696-6" @default.
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