Discovery of tumor-specific irreversible inhibitors of stearoyl CoA desaturase

Panayotis C Theodoropoulos, Stephen S Gonzales,Sarah E Winterton,Carlos Rodriguez-Navas, John S McKnight,Lorraine K Morlock,Jordan M Hanson,Bethany Cross, Amy E Owen,Yingli Duan,Jose R Moreno,Andrew Lemoff,Hamid Mirzaei,Bruce A Posner,Noelle S Williams,Joseph M Ready,Deepak Nijhawan

Nature Chemical Biology（2016）

引用 55|浏览7

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摘要

Two chemical series, oxalamides and benozothiazoles, produced toxicity in particular lung cancer cells. These compounds were metabolized in these sensitive cells by the cytochrome P450 enzyme CYP4F11 into potent inhibitors of stearoyl CoA desaturase.

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关键词

Cancer therapy,Mechanism of action,Small molecules,Target identification,Chemistry/Food Science,general,Biochemical Engineering,Biochemistry,Cell Biology,Bioorganic Chemistry

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