Matches in SemOpenAlex for { <https://semopenalex.org/work/W4386732685> ?p ?o ?g. }
- W4386732685 abstract "Abstract GPR84 is a unique orphan G protein-coupled receptor (GPCR) that can be activated by endogenous medium-chain fatty acids (MCFAs). The signaling of GPR84 is largely pro-inflammatory, which can augment inflammatory response, and GPR84 also functions as a pro-phagocytic receptor to enhance phagocytic activities of macrophages. In this study, we show that the activation of GPR84 by the synthetic agonist 6-OAU can synergize with the blockade of CD47 on cancer cells to induce phagocytosis of cancer cells by macrophages. We also determine a high-resolution structure of the GPR84-G i signaling complex with 6-OAU. This structure reveals an occluded binding pocket for 6-OAU, the molecular basis of receptor activation involving non-conserved structural motifs of GPR84, and an unusual G i -coupling interface. Together with computational docking and simulations studies, this structure also suggests a mechanism for the high selectivity of GPR84 for MCFAs and a potential routes of ligand binding and dissociation. These results provide a framework for understanding GPR84 signaling and developing new drugs targeting GPR84." @default.
- W4386732685 created "2023-09-15" @default.
- W4386732685 creator A5000927614 @default.
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- W4386732685 creator A5090385327 @default.
- W4386732685 date "2023-09-14" @default.
- W4386732685 modified "2023-10-03" @default.
- W4386732685 title "Pro-phagocytic function and structural basis of GPR84 signaling" @default.
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