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DCフィールド | 値 | 言語 |
---|---|---|
dc.contributor.author | Miwa, Sorachi | en |
dc.contributor.author | Takikawa, Hiroshi | en |
dc.contributor.author | Takeuchi, Rina | en |
dc.contributor.author | Mizunuma, Ryo | en |
dc.contributor.author | Matsuoka, Keita | en |
dc.contributor.author | Ogawa, Haruo | en |
dc.contributor.author | Kato, Hiroaki | en |
dc.contributor.author | Takasu, Kiyosei | en |
dc.contributor.alternative | 三和, 空知 | ja |
dc.contributor.alternative | 瀧川, 紘 | ja |
dc.contributor.alternative | 水沼, 諒 | ja |
dc.contributor.alternative | 松岡, 敬太 | ja |
dc.contributor.alternative | 小川, 治夫 | ja |
dc.contributor.alternative | 加藤, 博章 | ja |
dc.contributor.alternative | 高須, 清誠 | ja |
dc.date.accessioned | 2024-02-09T01:56:28Z | - |
dc.date.available | 2024-02-09T01:56:28Z | - |
dc.date.issued | 2024-02-08 | - |
dc.identifier.uri | http://hdl.handle.net/2433/286959 | - |
dc.description.abstract | Understanding the transport and inhibition mechanisms of substrates by P-glycoprotein (P-gp) is one of the important approaches in addressing multidrug resistance (MDR). In this study, we evaluated a variety of rhodamine derivatives as potential P-gp inhibitors targeting CmABCB1, a P-gp homologue, with a focus on their ATPase activity. Notably, a Q-rhodamine derivative with an o, o′-dimethoxybenzyl ester moiety (RhQ-DMB) demonstrated superior affinity and inhibitory activity, which was further confirmed by a drug susceptibility assay in yeast strains expressing CmABCB1. Results from a tryptophan fluorescence quenching experiment using a CmABCB1 mutant suggested that RhQ-DMB effectively enters and binds to the inner chamber of CmABCB1. These findings underscore the promising potential of RhQ-DMB as a tool for future studies aimed at elucidating the substrate-bound state of CmABCB1. | en |
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 Medicinal Chemistry Letters], copyright © [2024 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/acsmedchemlett.3c00526 | en |
dc.rights | The full-text file will be made open to the public on 19 January 2025 in accordance with publisher's 'Terms and Conditions for Self-Archiving'. | en |
dc.rights | This is not the published version. Please cite only the published version. 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。 | en |
dc.subject | Multidrug resistance | en |
dc.subject | ATP-Binding cassette transporter | en |
dc.subject | Rhodamine | en |
dc.subject | Inhibitor | en |
dc.subject | Structure−activity relationship | en |
dc.title | Structure–ATPase Activity Relationship of Rhodamine Derivatives as Potent Inhibitors of P-Glycoprotein CmABCB1 | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.jtitle | ACS Medicinal Chemistry Letters | en |
dc.identifier.volume | 15 | - |
dc.identifier.issue | 2 | - |
dc.identifier.spage | 287 | - |
dc.identifier.epage | 293 | - |
dc.relation.doi | 10.1021/acsmedchemlett.3c00526 | - |
dc.textversion | author | - |
dcterms.accessRights | embargoed access | - |
datacite.date.available | 2025-01-19 | - |
datacite.awardNumber | 21H02068 | - |
datacite.awardNumber | 21H05211 | - |
datacite.awardNumber | 23H02664 | - |
datacite.awardNumber | 20H03222 | - |
datacite.awardNumber.uri | https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-21H02068/ | - |
datacite.awardNumber.uri | https://kaken.nii.ac.jp/grant/KAKENHI-PLANNED-21H05211/ | - |
datacite.awardNumber.uri | https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-23H02664/ | - |
datacite.awardNumber.uri | https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-20H03222/ | - |
dc.identifier.eissn | 1948-5875 | - |
jpcoar.funderName | 日本学術振興会 | ja |
jpcoar.funderName | 日本学術振興会 | ja |
jpcoar.funderName | 日本学術振興会 | ja |
jpcoar.funderName | 日本学術振興会 | ja |
jpcoar.awardTitle | 複合構造を有する中分子天然物を基盤とした生物活性分子の創製 | ja |
jpcoar.awardTitle | 多成分連続反応のデジタル精密制御 | ja |
jpcoar.awardTitle | X線1分子動態計測による膜蛋白質マルチセンシング機構の動的解明 | ja |
jpcoar.awardTitle | 膜脂質中のABC多剤排出ポンプの交互アクセス機構の立体構造基盤 | ja |
出現コレクション: | 学術雑誌掲載論文等 |
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