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タイトル: | Structure–ATPase Activity Relationship of Rhodamine Derivatives as Potent Inhibitors of P-Glycoprotein CmABCB1 |
著者: | Miwa, Sorachi Takikawa, Hiroshi https://orcid.org/0000-0002-4414-2129 (unconfirmed) Takeuchi, Rina Mizunuma, Ryo Matsuoka, Keita Ogawa, Haruo https://orcid.org/0000-0001-5515-1533 (unconfirmed) Kato, Hiroaki https://orcid.org/0000-0002-5993-4532 (unconfirmed) Takasu, Kiyosei https://orcid.org/0000-0002-1798-7919 (unconfirmed) |
著者名の別形: | 三和, 空知 瀧川, 紘 水沼, 諒 松岡, 敬太 小川, 治夫 加藤, 博章 高須, 清誠 |
キーワード: | Multidrug resistance ATP-Binding cassette transporter Rhodamine Inhibitor Structure−activity relationship |
発行日: | 8-Feb-2024 |
出版者: | American Chemical Society (ACS) |
誌名: | ACS Medicinal Chemistry Letters |
巻: | 15 |
号: | 2 |
開始ページ: | 287 |
終了ページ: | 293 |
抄録: | 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. |
著作権等: | 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 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'. 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。 |
URI: | http://hdl.handle.net/2433/286959 |
DOI(出版社版): | 10.1021/acsmedchemlett.3c00526 |
出現コレクション: | 学術雑誌掲載論文等 |
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