部分
化学发光
体内
化学
醌
对苯二酚
连接器
体外
二氧乙烷
NAD+激酶
癌细胞
组合化学
癌症
生物化学
生物物理学
癌症研究
立体化学
生物
酶
有机化学
生物技术
操作系统
遗传学
计算机科学
作者
Subin Son,Miae Won,Ori Green,Nir Hananya,Amit Sharma,Yukyoung Jeon,Jong Hwan Kwak,Jonathan L. Sessler,Doron Shabat,Jong Seung Kim
标识
DOI:10.1002/anie.201813032
摘要
Abstract Activatable (turn‐on) probes that permit the rapid, sensitive, selective, and accurate identification of cancer‐associated biomarkers can help drive advances in cancer research. Herein, a NAD(P)H:quinone oxidoreductase‐1 (NQO1)‐specific chemiluminescent probe 1 is reported that allows the differentiation between cancer subtypes. Probe 1 incorporates an NQO1‐specific trimethyl‐locked quinone trigger moiety covalently tethered to a phenoxy‐dioxetane moiety through a para ‐aminobenzyl alcohol linker. Bio‐reduction of the quinone to the corresponding hydroquinone results in a chemiluminescent signal. As inferred from a combination of in vitro cell culture analyses and in vivo mice studies, the probe is safe, cell permeable, and capable of producing a “turn‐on” luminescence response in an NQO1‐positive A549 lung cancer model. On this basis, probe 1 can be used to identify cancerous cells and tissues characterized by elevated NQO1 levels.
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