2018年3月8日
Indolylmaleimide Derivative IM-17 Shows Cardioprotective Effects in Ischemia-Reperfusion Injury.
ACS medicinal chemistry letters
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- 巻
- 9
- 号
- 3
- 開始ページ
- 182
- 終了ページ
- 187
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1021/acsmedchemlett.7b00454
We previously developed IM-54 as a novel type of inhibitor of hydrogen-peroxide-induced necrotic cell death. Here, we examined its cell death inhibition profile. IM-54 was found to selectively inhibit oxidative stress-induced necrosis, but it did not inhibit apoptosis induced by various anticancer drugs or Fas ligand, or necroptosis. IM-17, an IM derivative having improved water-solubility and metabolic stability, was developed and confirmed to retain necrosis-inhibitory activity. IM-17 showed cardioprotective effects in an isolated rat heart model and an in vivo arrhythmia model, suggesting that IM derivatives may have therapeutic potential.
- リンク情報
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- DOI
- https://doi.org/10.1021/acsmedchemlett.7b00454
- PubMed
- https://www.ncbi.nlm.nih.gov/pubmed/29541357
- PubMed Central
- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5846036
- Web of Science
- https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000427331200003&DestApp=WOS_CPL
- ID情報
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- DOI : 10.1021/acsmedchemlett.7b00454
- ISSN : 1948-5875
- PubMed ID : 29541357
- PubMed Central 記事ID : PMC5846036
- Web of Science ID : WOS:000427331200003