五元环过氧化物选择性地引发癌细胞中的铁死亡。
Five-Membered Ring Peroxide Selectively Initiates Ferroptosis in Cancer Cells.
作者信息
Abrams Rachel P, Carroll William L, Woerpel K A
机构信息
Department of Chemistry, New York University , 100 Washington Square East, New York, New York 10003, United States.
Laura and Isaac Perlmutter Cancer Center, New York University Langone Medical Center , 522 First Avenue, New York, New York 10016, United States.
出版信息
ACS Chem Biol. 2016 May 20;11(5):1305-12. doi: 10.1021/acschembio.5b00900. Epub 2016 Mar 1.
Abstract
A 1,2-dioxolane (FINO2) was identified as a lead compound from a screen of organic peroxides. FINO2 does not induce apoptosis, but instead initiates ferroptosis, an iron-dependent, oxidative cell death pathway. Few compounds are known to induce primarily ferroptosis. In contrast to the perceived instability of peroxides, FINO2 was found to be thermally stable to at least 150 °C. FINO2 was more potent in cancer cells than nonmalignant cells of the same type. One of the enantiomers was found to be more responsible for the observed activity.
摘要
1,2 - 二氧戊环（FINO2）是从有机过氧化物筛选中鉴定出的先导化合物。FINO2不会诱导细胞凋亡，而是引发铁死亡，这是一种铁依赖性的氧化细胞死亡途径。已知很少有化合物主要诱导铁死亡。与过氧化物被认为的不稳定性相反，发现FINO2在至少150℃下热稳定。FINO2在癌细胞中比相同类型的非恶性细胞更有效。发现其中一种对映体对观察到的活性贡献更大。
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