Design and synthesis of rhodamine 110 derivative and caspase-3 substrate for enzyme and cell-based fluorescent assay

被引：91

作者：

Cai, SX ^{[1
]}

Zhang, HZ ^{[1
]}

Guastella, J ^{[1
]}

Drewe, J ^{[1
]}

Yang, W ^{[1
]}

Weber, E ^{[1
]}

机构：

[1] Maxim Pharmaceut, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(00)00590-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

N-Octyloxycarbonyl-R110 (1), with enhanced cell penetration and retention properties, was prepared from rhodamine 110. The tetrapeptide substrate N-Ac-DEVD-N'-octyloxycarbonyl-R110 (3) was prepared and shown to be efficiently cleaved by human recombinant caspase-3 and by apoptotic HL-60 cells. This substrate should prove useful in cell-based assays for apoptosis inducers and inhibitors. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：39 / 42

页数：4

共 9 条

[1]

Mammalian caspases: Structure, activation, substrates, and functions during apoptosis [J].