Novel 15-lipoxygenase-1 inhibitor protects cells from RSL3-induced cell death

被引：0
|
作者：
Zhang, Jianqiu [1 ]
van der Wouden, Petra E. [1 ]
Dekker, Frank J. [1 ]
机构：
[1] Univ Groningen, Groningen Res Inst Pharm GRIP, Dept Chem & Pharmaceut Biol, Antonius Deusinglaan 1, NL-9713 AV Groningen, Netherlands
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2025年 / 290卷
关键词：
Indole; Lipid peroxides; Lipid peroxidation; Cell death; 15-lipoxygenase-1 (15-LOX-1); POLYUNSATURATED FATTY-ACIDS; FERROPTOSIS; INACTIVATION;
D O I：
10.1016/j.ejmech.2025.117517
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Ferroptosis is a form of regulated cell death characterized by the accumulation of lipid peroxides. The enzyme 15-lipoxygenase-1 (15-LOX-1) plays a key role in catalyzing the formation of lipid peroxides. Therefore, inhibition of 15-LOX-1 enzyme activity holds promise to decrease the levels of lipid peroxidation. In this study, a novel potent 15-LOX-1 inhibitor, 5i, was developed and structure-activity relationships were explored. In vitro, this inhibitor inhibited lipid peroxidation and protected cells from RSL3-induced cell death. Thus, we report a potent 15-LOX-1 inhibitor, which can be used as a tool to investigate the role of 15-LOX-1.
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页数：11
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