Art

J-GLOBAL ID：201702248875830488   Reference number：17A1714303

Discovery of benzo[g]indoles as a novel class of non-covalent Keap1-Nrf2 protein-protein interaction inhibitor

新規クラスの非共有結合Keap1-Nrf2蛋白質-蛋白質相互作用阻害剤としてのベンゾ[g]インドールの発見【Powered by NICT】

Author (14)： Yasuda Daisuke (Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, Japan) ,  Yuasa Akihiro (Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, Japan) ,  Obata Rika (Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, Japan) ,  Nakajima Mao (Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, Japan) ,  Takahashi Kyoko (Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, Japan) ,  Ohe Tomoyuki (Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, Japan) ,  Ichimura Yoshinobu (Department of Biochemistry, Niigata University Graduate School of Medical and Dental Sciences, 1-757 Asahimachidori, Chuo-ku, Niigata-shi, Niigata, Japan) ,  Komatsu Masaaki (Department of Biochemistry, Niigata University Graduate School of Medical and Dental Sciences, 1-757 Asahimachidori, Chuo-ku, Niigata-shi, Niigata, Japan) ,  Yamamoto Masayuki (Department of Medical Biochemistry, Tohoku University School of Medicine, 2-1 Seiryo-machi, Aoba-ku, Sendai-shi, Miyagi, Japan) ,  Imamura Riyo (Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, Japan) ,  Kojima Hirotatsu (Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, Japan) ,  Okabe Takayoshi (Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, Japan) ,  Nagano Tetsuo (Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, Japan) ,  Mashino Tadahiko (Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, Japan)
Material： Bioorganic & Medicinal Chemistry Letters  (Bioorg Med Chem Lett)
Volume： 27  Issue： 22  Page： 5006-5009  Publication year： 2017 
JST Material Number： W0248A  ISSN： 0960-894X  Document type： Article
Article type： 原著論文  Country of issue： Netherlands (NLD)  Language： ENGLISH (EN)

Abstract/Point： The Keap1-Nrf2 system is an at...

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Thesaurus term： cytotoxicity ,  *covalent bond ,  Safety ,  clinical trial ,  *Proteins ,  metabolic stability ,  lead compound ,  Cell Line ,  inhibitory activity ,  activating agent ,  *NF-E2-Related Factor 2 ,  *Keap1 protein ,  *noncovalent binding ,  *protein-protein interaction
Semi thesaurus term： *阻害剤 , 【Automatic Indexing@JST】

Author keywords (5)： Nrf2 ,  Keap1 ,  Protein-protein interaction inhibitor ,  High-throughput screening ,  Metabolic stability

JST classification (1)： Synthesis of drugs  (GV01030F)

Terms in the title (8)： クラス ,  非共有結合 ,  Keap1 ,  NRF2 ,  蛋白質-蛋白質相互作用 ,  阻害剤 ,  インドール ,  発見