Insights into divalent cation regulation and G₁₃-coupling of orphan receptor GPR35.

ABSTRACT: Endogenous ions play important roles in the function and pharmacology of G protein-coupled receptors (GPCRs) with limited atomic evidence. In addition, compared with G protein subtypes G_s, G_i/o, and G_q/11, insufficient structural evidence is accessible to understand the coupling mechanism of G_12/13 protein by GPCRs. Orphan receptor GPR35, which is predominantly expressed in the gastrointestinal tract and is closely related to inflammatory bowel diseases (IBDs), stands out as a prototypical receptor for investigating ionic modulation and G₁₃ coupling. Here we report a cryo-electron microscopy structure of G₁₃-coupled GPR35 bound to an anti-allergic drug, lodoxamide. This structure reveals a novel divalent cation coordination

SUBMITTER: Duan J 

PROVIDER: S-EPMC9772185 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature