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-Structure paper
タイトル | Structural basis for strychnine activation of human bitter taste receptor TAS2R46. |
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ジャーナル・号・ページ | Science, Vol. 377, Issue 6612, Page 1298-1304, Year 2022 |
掲載日 | 2022年9月16日 |
著者 | Weixiu Xu / Lijie Wu / Shenhui Liu / Xiao Liu / Xiaoling Cao / Cui Zhou / Jinyi Zhang / You Fu / Yu Guo / Yiran Wu / Qiwen Tan / Ling Wang / Junlin Liu / Longquan Jiang / Zhongbo Fan / Yuan Pei / Jingyi Yu / Jianjun Cheng / Suwen Zhao / Xiaojiang Hao / Zhi-Jie Liu / Tian Hua / |
PubMed 要旨 | Taste sensing is a sophisticated chemosensory process, and bitter taste perception is mediated by type 2 taste receptors (TAS2Rs), or class T G protein-coupled receptors. Understanding the detailed ...Taste sensing is a sophisticated chemosensory process, and bitter taste perception is mediated by type 2 taste receptors (TAS2Rs), or class T G protein-coupled receptors. Understanding the detailed molecular mechanisms behind taste sensation is hindered by a lack of experimental receptor structures. Here, we report the cryo-electron microscopy structures of human TAS2R46 complexed with chimeric mini-G protein gustducin, in both strychnine-bound and apo forms. Several features of TAS2R46 are disclosed, including distinct receptor structures that compare with known GPCRs, a new "toggle switch," activation-related motifs, and precoupling with mini-G protein gustducin. Furthermore, the dynamic extracellular and more-static intracellular parts of TAS2R46 suggest possible diverse ligand-recognition and activation processes. This study provides a basis for further exploration of other bitter taste receptors and their therapeutic applications. |
リンク | Science / PubMed:36108005 |
手法 | EM (単粒子) |
解像度 | 3.01 - 3.08 Å |
構造データ | EMDB-33364, PDB-7xp4: EMDB-33365, PDB-7xp5: EMDB-33366, PDB-7xp6: |
化合物 | ChemComp-SY9: |
由来 |
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キーワード | MEMBRANE PROTEIN / G protein-coupled receptor / taste type 2 receptors / cryo-electron microscopy structure |