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Identification of Verapamil Binding Sites Within Human Kv1.5 Channel Using Mutagenesis and Docking Simulation.
http://hdl.handle.net/10422/00012492
http://hdl.handle.net/10422/00012492c1a182cc-0c44-4931-894e-137854882197
名前 / ファイル | ライセンス | アクション |
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000022 (3.0 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2019-04-08 | |||||
タイトル | ||||||
タイトル | Identification of Verapamil Binding Sites Within Human Kv1.5 Channel Using Mutagenesis and Docking Simulation. | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Amino Acid Substitution | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Animals | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Atrial Fibrillation | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Binding Sites | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | CHO Cells | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Cricetulus | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Humans | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Kv1.5 Potassium Channel | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Molecular Docking Simulation | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Point Mutation | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Potassium Channel Blockers | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Verapamil | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
林, 維光
× 林, 維光× Tano, Ayami× Mi, Xinya× 小嶋, 亜希子× SETO, Tomoyoshi× 松浦, 博 |
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著者別名 |
林, 維光
× 林, 維光× 田埜, 郁実× 小嶋, 亜希子× 瀬戸, 倫義× 松浦, 博 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | BACKGROUND/AIMS: The phenylalkylamine class of L-type Ca2+ channel antagonist verapamil prolongs the effective refractory period (ERP) of human atrium, which appears to contribute to the efficacy of verapamil in preventing reentrant-based atrial arrhythmias including atrial fibrillation. This study was designed to investigate the molecular and electrophysiological mechanism underlying the action of verapamil on human Kv1.5 (hKv1.5) channel that determines action potential duration and ERP in human atrium. |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | METHODS: Site-directed mutagenesis created 10 single-point mutations within pore region of hKv1.5 channel. Wholecell patch-clamp method investigated the effect of verapamil on wild-type and mutant hKv1.5 channels heterologously expressed in Chinese hamster ovary cells. Docking simulation was conducted using open-state homology model of hKv1.5 channel pore. |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | RESULTS: Verapamil preferentially blocked hKv1.5 channel in its open state with IC50 of 2.4±0.6 μM (n = 6). The blocking effect of verapamil was significantly attenuated in T479A, T480A, I502A, V505A, I508A, L510A, V512A and V516A mutants, compared with wild-type hKv1.5 channel. Computer docking simulation predicted that verapamil is positioned within central cavity of channel pore and has contact with Thr479, Thr480, Val505, Ile508, Ala509, Val512, Pro513 and Val516. |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | CONCLUSION: Verapamil acts as an open-channel blocker of hKv1.5 channel, presumably due to direct binding to specific amino acids within pore region of hKv1.5 channel, such as Thr479, Thr480, Val505, Ile508, Val512 and Val516. This blocking effect of verapamil on hKv1.5 channel appears to contribute at least partly to prolongation of atrial ERP and resultant antiarrhythmic action on atrial fibrillation in humans. |
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書誌情報 |
Cellular physiology and biochemistry : international journal of experimental cellular physiology 巻 52, 号 2, p. 302-314, 発行日 2019-02-28 |
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出版者 | ||||||
出版者 | Cell Physiol Biochem Press GmbH & Co KG | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 1421-9778 | |||||
PMID | ||||||
関連タイプ | isIdenticalTo | |||||
識別子タイプ | PMID | |||||
関連識別子 | 30816676 | |||||
DOI | ||||||
関連タイプ | isIdenticalTo | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.33594/000000022 | |||||
権利 | ||||||
権利情報 | © Copyright by the Author(s). Published by Cell Physiol Biochem Press. | |||||
著者版フラグ | ||||||
出版タイプ | VoR | |||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||
資源タイプ | ||||||
内容記述タイプ | Other | |||||
内容記述 | Journal Article |