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一种呋喃基丙烯共轭香豆素,作为一种有效的抑制剂和用于硫氧还蛋白还原酶共价标记的高选择性开启型荧光探针。

A furanyl acryl conjugated coumarin as an efficient inhibitor and a highly selective off-on fluorescent probe for covalent labelling of thioredoxin reductase.

作者信息

Huang Lei, Chen Yu, Liang Baoxia, Xing Bengang, Wen Gesi, Wang Shuni, Yue Xin, Zhu Cuige, Du Jun, Bu Xianzhang

机构信息

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, P. R. China.

出版信息

Chem Commun (Camb). 2014 Jul 7;50(53):6987-90. doi: 10.1039/c4cc02119c.

Abstract

A simple and novel furanyl acryl conjugated coumarin fluorophore was designed as an effective thioredoxin reductase (TrxR)-responding fluorescent probe by an activity-guided approach. Basically, the α,β-unsaturated ketone moiety in the probe structure could quench the fluorescence of the coumarin, but upon the covalent modification of TrxR, a significant fluorescence could be generated, which has been confirmed to be obviously selective over Trx, GSH, Cys and DTT.

摘要

通过活性导向法设计了一种简单新颖的呋喃基丙烯共轭香豆素荧光团,作为一种有效的硫氧还蛋白还原酶(TrxR)响应荧光探针。基本上,探针结构中的α,β-不饱和酮部分可以淬灭香豆素的荧光,但在TrxR进行共价修饰后,会产生显著的荧光,已证实其对Trx、谷胱甘肽(GSH)、半胱氨酸(Cys)和二硫苏糖醇(DTT)具有明显的选择性。

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