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

Design and synthesis of rhodamine 110 derivative and caspase-3 substrate for enzyme and cell-based fluorescent assay
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DOI:
10.1016/s0960-894x(00)00590-4
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发表时间:
2001-01-08
影响因子:
2.7
通讯作者:
Weber, E
Weber, E
中科院分区:
医学4区
文献类型:
--
作者:
Cai, SX;Zhang, HZ;Weber, E

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由罗丹明 110 制备的 N-辛氧基羰基-R110 (1) 具有增强的细胞渗透和保留特性。制备了四肽底物 N-Ac-DEVD-N'-辛氧基羰基-R110 (3),并显示可被人重组 caspase-3 和凋亡的 HL-60 细胞有效裂解。该底物应可用于细胞凋亡诱导剂和抑制剂的细胞测定。 (C) 2000 Elsevier Science Ltd. 保留所有权利。
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.