Design and synthesis of an ER-specific fluorescent probe based on carboxylesterase activity with quinone methide cleavage process

被引：37

作者：

Hakamata, Wataru ^{[1
]}

Machida, Aki ^{[1
]}

Oku, Tadatake ^{[1
]}

Nishio, Toshiyuki ^{[1
]}

机构：

[1] Nihon Univ, Coll Bioresource Sci, Dept Chem & Life Sci, Fujisawa, Kanagawa 2520880, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 11期

关键词：

Carboxylesterase; Fluorescent probe; Quinone methide cleavage; Resorufin; CATALYTIC-PROPERTIES; PRODRUGS;

D O I：

10.1016/j.bmcl.2011.04.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

CEs are important enzymes that catalyze the hydrolysis of prodrugs. In this Letter, we present a new mechanistic ER-specific fluorescent probe 1 based on CE activity. Permeation of 1 into cells and subsequent hydrolytic activation by CEs causes spontaneously quinone methide cleavage, resulting in bright red fluorescence in ER with high specificity. Probe 1 was developed for CE activity imaging and inhibitor screening at the cellular level. (C) 2011 Elsevier Ltd. All rights reserved.

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页码：3206 / 3209

页数：4

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