HUSCAP logo Hokkaido Univ. logo

Hokkaido University Collection of Scholarly and Academic Papers >
Graduate School of Veterinary Medicine / Faculty of Veterinary Medicine >
Peer-reviewed Journal Articles, etc >

Cibacron blue 3G-A is a novel inhibitor of Otopetrin 1 (OTOP1), a proton channel

This item is licensed under:Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International

Files in This Item:
SYamaguchi For HUSCAP.pdf1.09 MBPDFView/Open
Please use this identifier to cite or link to this item:

Title: Cibacron blue 3G-A is a novel inhibitor of Otopetrin 1 (OTOP1), a proton channel
Authors: Islam, MD Mominul Browse this author
Sasaki, Omi Browse this author
Yano-Nashimoto, Saori Browse this author
Okamatsu-Ogura, Yuko Browse this author →KAKEN DB
Yamaguchi, Soichiro Browse this author →KAKEN DB
Keywords: Otopetrin1
Proton channel
Reactive blue 2
Cibacron blue 3G-A
Issue Date: 29-Apr-2023
Publisher: Elsevier
Journal Title: Biochemical and biophysical research communications
Volume: 665
Start Page: 64
End Page: 70
Publisher DOI: 10.1016/j.bbrc.2023.04.112
Abstract: Otopetrin 1 (OTOP1) is a proton (H+) channel which detects acidic stimuli in sour taste receptor cells and plays some sort of role in the formation of otoconia in the inner ear. Although it is known that zinc ion (Zn2+) inhibits OTOP1, Zn2+ requires high concentrations (mM order) to inhibit OTOP1 sufficiently, and no other inhibitors have been found. Therefore, to identify a novel inhibitor, we screened a chemical library (LOPAC1280) by whole-cell patch clamp recordings, measuring proton currents of heterologously-expressed mouse OTOP1. From the screening, we found that reactive blue 2 inhibited OTOP1 currents. Further evaluations of three analogues of reactive blue 2 revealed that cibacron blue 3G-A potently inhibited OTOP1 currents. Cibacron blue 3G-A inhibited OTOP1 currents in a concentration-dependent manner, and its 50% inhibitory concentration (IC50) and the Hill coefficient were 5.0 mM and 1.1, respectively. The inhibition of OTOP1 currents by cibacron blue 3G-A was less affected by extracellular anion compositions, membrane potentials, and low pH than the inhibition by Zn2+. These results suggest that the inhibition of OTOP1 by cibacron blue 3G-A is neither likely to be a pore-blocking inhibition nor a competitive inhibition. Furthermore, our findings revealed that cibacron blue 3G-A can be used as a novel inhibitor of OTOP1 especially under the conditions in which OTOP1 activity is evaluated such as low pH. (c) 2023 Elsevier Inc. All rights reserved.
Rights: © 2023. This manuscript version is made available under the CC-BY-NC-ND 4.0 license
Type: article (author version)
Appears in Collections:獣医学院・獣医学研究院 (Graduate School of Veterinary Medicine / Faculty of Veterinary Medicine) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 山口 聡一郎

Export metadata:

OAI-PMH ( junii2 , jpcoar_1.0 )

MathJax is now OFF:


 - Hokkaido University