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Title: Structure–ATPase Activity Relationship of Rhodamine Derivatives as Potent Inhibitors of P-Glycoprotein CmABCB1
Authors: Miwa, Sorachi
Takikawa, Hiroshi
Takeuchi, Rina
Mizunuma, Ryo
Matsuoka, Keita
Ogawa, Haruo  kyouindb  KAKEN_id  orcid (unconfirmed)
Kato, Hiroaki
Takasu, Kiyosei
Author's alias: 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
Keywords: Multidrug resistance
ATP-Binding cassette transporter
Structure−activity relationship
Issue Date: 8-Feb-2024
Publisher: American Chemical Society (ACS)
Journal title: ACS Medicinal Chemistry Letters
Volume: 15
Issue: 2
Start page: 287
End page: 293
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.
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
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。
DOI(Published Version): 10.1021/acsmedchemlett.3c00526
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