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TitleActivation and signaling mechanism revealed by GPR119-G complex structures.
Journal, issue, pagesNat Commun, Vol. 13, Issue 1, Page 7033, Year 2022
Publish dateNov 17, 2022
AuthorsYuxia Qian / Jiening Wang / Linlin Yang / Yanru Liu / Lina Wang / Wei Liu / Yun Lin / Hong Yang / Lixin Ma / Sheng Ye / Shan Wu / Anna Qiao /
PubMed AbstractAgonists 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 ...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 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. Disruption of the salt bridge eliminates the cAMP production of GPR119, indicating an important role of Gβ 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.
External linksNat Commun / PubMed:36396650 / PubMed Central
MethodsEM (single particle)
Resolution2.33 - 2.87 Å
Structure data

32424

7wcm

EMDB-32424, PDB-7wcm:
Cryo-EM structure of GPR119-Gs Complex with small molecule agonist MBX-2982
Method: EM (single particle) / Resolution: 2.33 Å

32425

7wcn

EMDB-32425, PDB-7wcn:
Cryo-EM structure of GPR119-Gs Complex with small molecule agonist AR231453
Method: EM (single particle) / Resolution: 2.87 Å

Chemicals

ChemComp-8VP:
2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(1,2,3,4-tetrazol-1-yl)phenoxy]methyl]-1,3-thiazole

ChemComp-8WL:
N-(2-fluoranyl-4-methylsulfonyl-phenyl)-5-nitro-6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]pyrimidin-4-amine / agonist*YM

Source
  • homo sapiens (human)
  • lama glama (llama)
KeywordsSIGNALING PROTEIN / GPCR

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