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J-GLOBAL ID：202002254911555452   整理番号：20A1175769

脂質-二分子層界面におけるヒトプロスタグランジンE受容体EP_4へのリガンド結合【JST・京大機械翻訳】

Ligand binding to human prostaglandin E receptor EP₄ at the lipid-bilayer interface

著者 (52件)： Toyoda Yosuke (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Toyoda Yosuke (School of Medicine, Tsinghua University, Beijing, China) ,  Morimoto Kazushi (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Suno Ryoji (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Horita Shoichiro (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Yamashita Keitaro (RIKEN SPring-8 Center, Sayo-cho, Sayo-gun, Hyogo, Japan) ,  Hirata Kunio (RIKEN SPring-8 Center, Sayo-cho, Sayo-gun, Hyogo, Japan) ,  Sekiguchi Yusuke (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Yasuda Satoshi (Department of Chemistry, Graduate School of Science, Chiba University, Inage, Chiba, Japan) ,  Yasuda Satoshi (Institute of Advanced Energy, Kyoto University, Uji, Kyoto, Japan) ,  Shiroishi Mitsunori (Graduate School of Pharmaceutical Sciences, Kyushu University, Higashi-ku, Fukuoka, Japan) ,  Shiroishi Mitsunori (Japan Science and Technology Agency (JST), Platform for Drug Discovery, Informatics, and Structural Life Science, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Shimizu Tomoko (NB Health Laboratory Co. Ltd., Kita Ward Sapporo City, Hokkaido, Japan) ,  Urushibata Yuji (NB Health Laboratory Co. Ltd., Kita Ward Sapporo City, Hokkaido, Japan) ,  Kajiwara Yuta (Graduate School of Energy Science, Kyoto University, Uji, Kyoto, Japan) ,  Kajiwara Yuta (Molecular Profiling Research Center for Drug Discovery (MOLPROF), National Institute of Advanced Industrial Science and Technology (AIST), Tokyo, Japan) ,  Inazumi Tomoaki (Department of Pharmaceutical Biochemistry, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-Honmachi, Kumamoto, Japan) ,  Hotta Yunhon (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Asada Hidetsugu (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Asada Hidetsugu (JST, the Strategic Basic Research Program, Membrane Protein Crystallography Project, Kyoto, Japan) ,  Nakane Takanori (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Shiimura Yuki (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Shiimura Yuki (JST, the Strategic Basic Research Program, Membrane Protein Crystallography Project, Kyoto, Japan) ,  Nakagita Tomoya (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Tsuge Kyoshiro (Department of Pharmaceutical Biochemistry, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-Honmachi, Kumamoto, Japan) ,  Yoshida Suguru (Laboratory of Chemical Bioscience, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo, Japan) ,  Kuribara Tomoko (Laboratory of Chemical Bioscience, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo, Japan) ,  Hosoya Takamitsu (Japan Science and Technology Agency (JST), Platform for Drug Discovery, Informatics, and Structural Life Science, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Hosoya Takamitsu (Laboratory of Chemical Bioscience, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo, Japan) ,  Sugimoto Yukihiko (Department of Pharmaceutical Biochemistry, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-Honmachi, Kumamoto, Japan) ,  Sugimoto Yukihiko (Japan Agency for Medical Research and Development (AMED), Core Research for Evolutional Science and Technology (CREST), Chiyoda-ku, Tokyo, Japan) ,  Nomura Norimichi (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Nomura Norimichi (JST, the Strategic Basic Research Program, Membrane Protein Crystallography Project, Kyoto, Japan) ,  Sato Miwa (Biomedical Department, Mitsui Knowledge Industry Co., Minato-ku, Tokyo, Japan) ,  Hirokawa Takatsugu (Japan Science and Technology Agency (JST), Platform for Drug Discovery, Informatics, and Structural Life Science, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Hirokawa Takatsugu (Molecular Profiling Research Center for Drug Discovery (MOLPROF), National Institute of Advanced Industrial Science and Technology (AIST), Tokyo, Japan) ,  Hirokawa Takatsugu (Division of Biomedical Science, Faculty of Medicine, University of Tsukuba, Tsukuba, Japan) ,  Kinoshita Masahiro (Institute of Advanced Energy, Kyoto University, Uji, Kyoto, Japan) ,  Murata Takeshi (Department of Chemistry, Graduate School of Science, Chiba University, Inage, Chiba, Japan) ,  Murata Takeshi (Japan Science and Technology Agency (JST), Platform for Drug Discovery, Informatics, and Structural Life Science, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Takayama Kiyoshi (NB Health Laboratory Co. Ltd., Kita Ward Sapporo City, Hokkaido, Japan) ,  Yamamoto Masaki (RIKEN SPring-8 Center, Sayo-cho, Sayo-gun, Hyogo, Japan) ,  Yamamoto Masaki (Japan Science and Technology Agency (JST), Platform for Drug Discovery, Informatics, and Structural Life Science, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Narumiya Shuh (Japan Agency for Medical Research and Development (AMED), Core Research for Evolutional Science and Technology (CREST), Chiyoda-ku, Tokyo, Japan) ,  Narumiya Shuh (Medical Innovation Center, Kyoto University Graduate School of Medicine, Sakyo-ku, Kyoto, Japan) ,  Iwata So (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Iwata So (RIKEN SPring-8 Center, Sayo-cho, Sayo-gun, Hyogo, Japan) ,  Iwata So (JST, the Strategic Basic Research Program, Membrane Protein Crystallography Project, Kyoto, Japan) ,  Kobayashi Takuya (Department of Medical Chemistry and Cell Biology, Kyoto University Graduate School of Medicine, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Kobayashi Takuya (Japan Science and Technology Agency (JST), Platform for Drug Discovery, Informatics, and Structural Life Science, Konoe-cho, Yoshida, Sakyo-ku, Kyoto, Japan) ,  Kobayashi Takuya (JST, the Strategic Basic Research Program, Membrane Protein Crystallography Project, Kyoto, Japan) ,  Kobayashi Takuya (Japan Agency for Medical Research and Development (AMED), Core Research for Evolutional Science and Technology (CREST), Chiyoda-ku, Tokyo, Japan)
資料名： Nature Chemical Biology  (Nature Chemical Biology)
巻： 15  号： 1  ページ： 18-26  発行年： 2019年 
JST資料番号： W2213A  ISSN： 1552-4450  資料種別： 逐次刊行物 (A)
記事区分： 原著論文  発行国： ドイツ (DEU)  言語： 英語 (EN)

抄録/ポイント： G蛋白質共役受容体であるプロスタグランジンE受容体EP4は,癌や自己免疫疾患などの疾患に関与する。ここでは,アンタゴニストONO-AE3-208および3.2Å解像度での阻害抗体との複合体におけるヒトEP4の結晶構造を報告する。構造は細胞外表面が細胞外ループにより閉塞され,拮抗剤が7番目の膜貫通ドメインにおいて高度に保存されたArg316残基に近い脂質二分子層との界面に存在することを明らかにした。機能的及びドッキング研究により,天然アゴニストPGE2は類似様式で結合することを示した。この構造情報は,膜二分子層からEP4結合ポケットへのリガンド侵入経路への洞察も提供する。さらに,構造は,抗体がEP4のリガンド結合に立体的に影響することを明らかにした。これらの結果は,この受容体ファミリーにおけるオルト立体およびアロステリック部位の両方を標的とする新しい治療薬の設計を容易にするはずである。アンタゴニストONO-AE3-208および機能性抗体との複合体におけるヒトプロスタグランジンE受容体EP4の構造は,GPCRsの間でユニークな脂質二重層の界面にリガンド結合部位を明らかにする。Copyright Springer Nature America, Inc. 2018 Translated from English into Japanese by JST.【JST・京大機械翻訳】

シソーラス用語： *界面 ,  結晶構造 ,  ドッキング ,  抗体 ,  *脂質 ,  *受容体 ,  ヒト ,  結合部位 ,  複合体 ,  アロステリック部位 ,  *リガンド結合 ,  リガンド結合ドメイン
準シソーラス用語： アゴニスト ,  アンタゴニスト ,  残基 , 【Automatic Indexing@JST】

分類 (2件)： 細胞膜の受容体  (EF04030C) ,  分子構造  (EB03020Y)

タイトルに関連する用語 (6件)： 脂質 ,  二分子層 ,  界面 ,  ヒト ,  プロスタグランジンE受容体 ,  リガンド結合