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The discovery of a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1) for ischemic heart: synthesis, activity and target identification 期刊论文

编号：

9a731a96-bc09-4e13-b1a3-0ecde2b9d670
作者：

Wang, Ying^[1];Cao, Yang^[2];Zhu, Qing^[3];Gu, Xianfeng(古险峰)*^[2]Zhu, Yi Zhun(朱依谆)*^[1,4]
语种：

English
期刊：

SCIENTIFIC REPORTS ISSN：2045-2322 2016 年 6 卷 ; JUL 22
收录：
摘要：

Apaf-1 is a central component in the apoptosis regulatory network for the treatment of apoptosis related diseases. Excessive Apaf-1 activity induced by myocardial ischemia causes cell injury. No drug targeted to Apaf-1 for treating myocardial ischemia has been reported to the best of our knowledge. In the present work, we synthesized a novel compound, ZYZ-488, which exhibited significant cardioprotective property in significantly increasing the viability of hypoxia-induced H9c2 cardiomyocytes and reducing CK and LDH leakage. Further study suggested the protective activity of ZYZ-488 dependent on its anti-apoptosis effect. This anti-apoptotic effect is most probably related to its disturbing the interaction between Apaf-1 and procaspase-9 as the target fishing and molecular docking indicated. The suppression on the activation of procaspase-9 and procaspase-3 with ZYZ-488 strongly suggested that compound ZYZ-488 could be a novel inhibitor of Apaf-1. In conclusion, ZYZ-488 as a novel small molecule competitive inhibitor of Apaf-1, with the great potential for treating cardiac ischemia.
推荐引用方式
GB/T 7714：

Wang Ying,Cao Yang,Zhu Qing, et al. The discovery of a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1) for ischemic heart: synthesis, activity and target identification [J].SCIENTIFIC REPORTS,2016,6.
APA：

Wang Ying,Cao Yang,Zhu Qing,Gu Xianfeng,&Zhu Yi Zhun.(2016).The discovery of a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1) for ischemic heart: synthesis, activity and target identification .SCIENTIFIC REPORTS,6.
MLA：

Wang Ying, et al. "The discovery of a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1) for ischemic heart: synthesis, activity and target identification" .SCIENTIFIC REPORTS 6(2016).

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