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-Structure paper
タイトル | Structures of signaling complexes of lipid receptors S1PR1 and S1PR5 reveal mechanisms of activation and drug recognition. |
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ジャーナル・号・ページ | Cell Res, Vol. 31, Issue 12, Page 1263-1274, Year 2021 |
掲載日 | 2021年9月15日 |
著者 | Yuan Yuan / Guowen Jia / Chao Wu / Wei Wang / Lin Cheng / Qian Li / Ziyan Li / Kaidong Luo / Shengyong Yang / Wei Yan / Zhaoming Su / Zhenhua Shao / |
PubMed 要旨 | Sphingosine-1-phosphate (S1P) is an important bioactive lipid molecule in cell membrane metabolism and binds to G protein-coupled S1P receptors (S1PRs) to regulate embryonic development, ...Sphingosine-1-phosphate (S1P) is an important bioactive lipid molecule in cell membrane metabolism and binds to G protein-coupled S1P receptors (S1PRs) to regulate embryonic development, physiological homeostasis, and pathogenic processes in various organs. S1PRs are lipid-sensing receptors and are therapeutic targets for drug development, including potential treatment of COVID-19. Herein, we present five cryo-electron microscopy structures of S1PRs bound to diverse drug agonists and the heterotrimeric Gi protein. Our structural and functional assays demonstrate the different binding modes of chemically distinct agonists of S1PRs, reveal the mechanical switch that activates these receptors, and provide a framework for understanding ligand selectivity and G protein coupling. |
リンク | Cell Res / PubMed:34526663 / PubMed Central |
手法 | EM (単粒子) |
解像度 | 2.98 - 3.42 Å |
構造データ | EMDB-31341, PDB-7evy: EMDB-31342, PDB-7evz: EMDB-31343, PDB-7ew0: EMDB-31344, PDB-7ew1: EMDB-31349, PDB-7ew7: |
化合物 | ChemComp-J8C: ChemComp-NAG: ChemComp-JER: ChemComp-PLM: ChemComp-JEU: ChemComp-JEX: |
由来 |
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キーワード | MEMBRANE PROTEIN / Homo sapiens |