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DCフィールド | 値 | 言語 |
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dc.contributor.author | Furuta, Tomoyuki | en |
dc.contributor.author | Mizukami, Yuya | en |
dc.contributor.author | Asano, Lisa | en |
dc.contributor.author | Kotake, Kenjiro | en |
dc.contributor.author | Ziegler, Slava | en |
dc.contributor.author | Yoshida, Hiroki | en |
dc.contributor.author | Watanabe, Mizuki | en |
dc.contributor.author | Sato, Shin-ichi | en |
dc.contributor.author | Waldmann, Herbert | en |
dc.contributor.author | Nishikawa, Makiya | en |
dc.contributor.author | Uesugi, Motonari | en |
dc.contributor.alternative | 西川, 元也 | ja |
dc.contributor.alternative | 上杉, 志成 | ja |
dc.date.accessioned | 2019-11-27T05:10:15Z | - |
dc.date.available | 2019-11-27T05:10:15Z | - |
dc.date.issued | 2019-9-20 | - |
dc.identifier.issn | 1554-8929 | - |
dc.identifier.issn | 1554-8937 | - |
dc.identifier.uri | http://hdl.handle.net/2433/244838 | - |
dc.description.abstract | Covalent conjugates of multiple nutrients often exhibit greater biological activities than each individual nutrient and more predictable safety profiles than completely unnatural chemical entities. Here, we report the construction and application of a focused chemical library of 308 covalent conjugates of a variety of small-molecule nutrients. Screening of the library with a reporter gene of sterol regulatory element-binding protein (SREBP), a master regulator of mammalian lipogenesis, led to the discovery of a conjugate of docosahexaenoic acid (DHA), glucosamine, and amino acids as an inhibitor of SREBP (molecule 1, DHG). Mechanistic analyses indicate that molecule 1 impairs the SREBP activity by inhibiting glucose transporters and thereby activating AMP-activated protein kinase (AMPK). Oral administration of molecule 1 suppressed the intestinal absorption of glucose in mice. These results suggest that such synthetic libraries of nutrient conjugates serve as a source of novel chemical tools and pharmaceutical seeds that modulate energy metabolism. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society (ACS) | en |
dc.rights | This document is the Accepted Manuscript version of a Published Work that appeared in final form in 'ACS Chemical Biology', copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://doi.org/10.1021/acschembio.9b00444. | en |
dc.rights | The full-text file will be made open to the public on 22 August 2020 in accordance with publisher's 'Terms and Conditions for Self-Archiving'. | en |
dc.rights | この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。 | ja |
dc.rights | This is not the published version. Please cite only the published version. | en |
dc.subject | Molecular Medicine | en |
dc.subject | Biochemistry | en |
dc.subject | General Medicine | en |
dc.title | Nutrient-Based Chemical Library as a Source of Energy Metabolism Modulators | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.jtitle | ACS Chemical Biology | - |
dc.identifier.volume | 14 | - |
dc.identifier.issue | 9 | - |
dc.identifier.spage | 1860 | - |
dc.identifier.epage | 1865 | - |
dc.relation.doi | 10.1021/acschembio.9b00444 | - |
dc.textversion | author | - |
dc.identifier.pmid | 31436407 | - |
dcterms.accessRights | open access | - |
datacite.date.available | 2020-08-22 | - |
datacite.awardNumber | 17H06408 | - |
datacite.awardNumber | 26220206 | - |
jpcoar.funderName | 日本学術振興会 | ja |
jpcoar.funderName | 日本学術振興会 | ja |
jpcoar.funderName.alternative | Japan Society for the Promotion of Science (JSPS) | en |
jpcoar.funderName.alternative | Japan Society for the Promotion of Science (JSPS) | en |
出現コレクション: | 学術雑誌掲載論文等 |
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