文献

J-GLOBAL ID：201902258332875596   整理番号：19A2352492

ピペラジニルアゼチジン骨格における”尾部スイッチング”戦略を用いた可逆的および不可逆的モノアシルグリセロールリパーゼ陽電子放出断層撮影(PET)トレーサの設計,合成および評価【JST・京大機械翻訳】

Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine Skeleton

著者 (35件)： Chen Zhen (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Chen Zhen (Department of Chemistry, School of Science, Tianjin University, China) ,  Mori Wakana (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Deng Xiaoyun (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Cheng Ran (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Ogasawara Daisuke (The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, California, United States) ,  Zhang Genwei (Department of Chemistry and Biochemistry, University of Oklahoma, Oklahoma, United States) ,  Schafroth Michael A. (The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, California, United States) ,  Dahl Kenneth (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Fu Hualong (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Hatori Akiko (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Shao Tuo (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Zhang Yiding (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Yamasaki Tomoteru (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Zhang Xiaofei (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Rong Jian (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Yu Qingzhen (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Hu Kuan (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Fujinaga Masayuki (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Xie Lin (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Kumata Katsushi (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Gou Yuancheng (ChemShuttle, Inc., Jiangsu, China) ,  Chen Jingjin (ChemShuttle, Inc., Jiangsu, China) ,  Gu Shuyin (ChemShuttle, Inc., Jiangsu, China) ,  Bao Liang (ChemShuttle, Inc., Jiangsu, China) ,  Wang Lu (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Collier Thomas Lee (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Vasdev Neil (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Shao Yihan (Department of Chemistry and Biochemistry, University of Oklahoma, Oklahoma, United States) ,  Ma Jun-An (Department of Chemistry, School of Science, Tianjin University, China) ,  Cravatt Benjamin F. (The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, California, United States) ,  Fowler Christopher (Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden) ,  Josephson Lee (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States) ,  Zhang Ming-Rong (Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Japan) ,  Liang Steven H. (Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Massachusetts, United States)
資料名： Journal of Medicinal Chemistry  (Journal of Medicinal Chemistry)
巻： 62  号： 7  ページ： 3336-3353  発行年： 2019年 
JST資料番号： D0102A  ISSN： 0022-2623  CODEN： JMCMAR  資料種別： 逐次刊行物 (A)
記事区分： 原著論文  発行国： アメリカ合衆国 (USA)  言語： 英語 (EN)

抄録/ポイント： モノアシルグリセロールリパーゼ(MAGL)は,エンドカンナビノイド系(eCB)において2-アラキドノイルグリセロール(2-AG)を分解するセリンヒドロラーゼである。MAGLの選択的阻害は,慢性疼痛,炎症,癌および神経変性を含む多様な病理学的条件の治療のための潜在的治療アプローチとして出現した。ここでは,ピペラジニルアゼチジン足場上での「テールスイッチング」により可逆的で不可逆的なMAGL阻害剤の新しいアレイを明らかにした。著者らは,11Cまたは18Fによる放射性標識化に適した,鉛不可逆結合MAGL阻害剤8および可逆結合化合物17および37を開発した。[11C]8([11C]-MAGL-2-11)は,MAGLに対する脳で高い脳取り込みと優れた結合特異性を示した。可逆的放射性リガンド[11C]17([11C]-PAD)と[18F]37([18F]-MAGL-4-11)は,末梢器官におけるMAGLに対する優れたin vivo結合特異性を示した。本研究は,可逆的で不可逆的な結合機構における調整可能性を有するMAGL標的陽電子放出断層撮影トレーサーの開発の道を開く可能性がある。Copyright 2019 American Chemical Society All rights reserved. Translated from English into Japanese by JST.【JST・京大機械翻訳】

シソーラス用語： 炎症 ,  ヒト ,  *不可逆性 ,  *スイッチング ,  *PET【トモグラフィー】 ,  治療法
準シソーラス用語： 器官 ,  放射性リガンド ,  結合特異性 ,  阻害剤 ,  神経変性 ,  慢性疼痛 ,  セリンヒドロラーゼ ,  内因性カンナビノイド ,  *モノアシルグリセロールリパーゼ , 【Automatic Indexing@JST】

分類 (2件)： 酵素製剤・酵素阻害剤の基礎研究  (GW21010W) ,  薬物学一般  (GV01010J)

タイトルに関連する用語 (10件)： 骨格 ,  尾部 ,  スイッチング ,  戦略 ,  モノアシルグリセロールリパーゼ ,  陽電子放出断層撮影 ,  PET ,  トレーサ ,  設計 ,  評価