Item type |
文献 / Documents(1) |
公開日 |
2019-10-15 |
アクセス権 |
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アクセス権 |
open access |
資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
出版社版DOI |
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識別子タイプ |
DOI |
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関連識別子 |
https://doi.org/10.1111/cbdd.12594 |
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言語 |
ja |
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関連名称 |
10.1111/cbdd.12594 |
出版タイプ |
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出版タイプ |
AM |
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出版タイプResource |
http://purl.org/coar/version/c_ab4af688f83e57aa |
タイトル |
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タイトル |
Bongkrekic Acid Analogue, Lacking One of the Carboxylic Groups of its Parent Compound, Shows Moderate but pH‐insensitive Inhibitory Effects on the Mitochondrial ADP/ATP Carrier |
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言語 |
en |
タイトル別表記 |
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その他のタイトル |
pH-resistant Inhibitor of Mitochondrial ADP/ATP Carrier |
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言語 |
en |
著者 |
ヤマモト, アツシ
ハスイ, ケイスケ
マツオ, ヒロシ
オクダ, カツヒロ
アベ, マサト
マツモト, ケンジ
ハラダ, カズキ
ヨシムラ, ユウヤ
山本, 武範
大倉, 一人
新藤, 充
篠原, 康雄
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抄録 |
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内容記述タイプ |
Abstract |
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内容記述 |
Bongkrekic acid (BKA), isolated from Burkholderia cocovenenans, is known to specifically inhibit the mitochondrial ADP/ATP carrier. However, the manner of its interaction with the carrier remains elusive. In the present study, we tested the inhibitory effects of 17 bongkrekic acid analogues, derived from the intermediates obtained during its total synthesis, on the mitochondrial ATP/ATP carrier. Rough screening of these chemicals, done by measuring their inhibitory effects on the mitochondrial ATP synthesis, revealed that 4 of them, KH-1, 7, 16, and 17, had moderate inhibitory effects. Further characterization of the actions of these 4 analogues on mitochondrial function showed that KH-16 had moderate; KH-1 and KH-17, weak; and KH-7, negligible side effects of both permeabilization of the mitochondrial inner membrane and inhibition of the electron transport, indicating that only KH-7 had a specific inhibitory effect on the mitochondrial ADP/ATP carrier. Although the parental bongkrekic acid showed a strong pH dependency of its action, the inhibitory effect of KH-7 was almost insensitive to the pH of the reaction medium, indicating the importance of the 3 carboxyl groups of BKA for its pH- dependent action. A direct inhibitory effect of KH-7 on the mitochondrial ADP/ATP carrier was also clearly demonstrated. |
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言語 |
en |
キーワード |
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言語 |
en |
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主題Scheme |
Other |
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主題 |
ADP/ATP carrier |
キーワード |
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言語 |
en |
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主題Scheme |
Other |
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主題 |
bongkrekic acid(BKA) |
キーワード |
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言語 |
en |
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主題Scheme |
Other |
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主題 |
mitochondria |
キーワード |
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言語 |
en |
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主題Scheme |
Other |
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主題 |
mitochondrial solute carrier (SLC25a) |
書誌情報 |
en : Chemical Biology & Drug Design
巻 86,
号 5,
p. 1304-1322,
発行日 2015-05-29
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収録物ID |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
17470277 |
収録物ID |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
17470285 |
収録物ID |
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収録物識別子タイプ |
NCID |
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収録物識別子 |
AA12108214 |
収録物ID |
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収録物識別子タイプ |
NCID |
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収録物識別子 |
AA12571955 |
出版者 |
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出版者 |
John Wiley & Sons |
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言語 |
en |
権利情報 |
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言語 |
en |
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権利情報 |
This is the peer reviewed version of the following article: Yamamoto, A. , Hasui, K. , Matsuo, H. , Okuda, K. , Abe, M. , Matsumoto, K. , Harada, K. , Yoshimura, Y. , Yamamoto, T. , Ohkura, K. , Shindo, M. and Shinohara, Y. (2015), Bongkrekic Acid Analogue, Lacking One of the Carboxylic Groups of its Parent Compound, Shows Moderate but pH‐insensitive Inhibitory Effects on the Mitochondrial ADP/ATP Carrier. Chem Biol Drug Des, 86: 1304-1322, which has been published in final form at https://doi.org/10.1111/cbdd.12594. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions. |
EID |
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識別子 |
295256 |
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識別子タイプ |
URI |
言語 |
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言語 |
eng |