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合成并评价一种对多巴胺具有选择性的荧光探针衍生检测试剂(Pup 试剂),多巴胺是结核分枝杆菌的一个潜在药物靶点。

Synthesis and evaluation of a selective fluorogenic Pup derived assay reagent for Dop, a potential drug target in Mycobacterium tuberculosis.

机构信息

Division of Cell Biology, Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands.

出版信息

Chembiochem. 2012 Sep 24;13(14):2056-60. doi: 10.1002/cbic.201200460. Epub 2012 Aug 24.

Abstract

A litter of pups: The synthesis and in vitro evaluation of new Pup-based fluorogenic substrates for Dop, the mycobacterial depupylase, are described. A full-length Pup-amidomethylcoumarin conjugate as well as an amino-terminus-truncated analogue exhibited high sensitivity and specificity towards hydrolysis by Dop. The substrates developed here might find application as high-throughput screening assay reagents for the identification of Dop inhibitors.

摘要

一窝幼崽

描述了新的基于 Pup 的荧光底物的合成和体外评估,用于 Dop,即分枝杆菌脱 pupylase。全长 Pup-氨甲基香豆素缀合物以及氨基末端截断类似物对 Dop 水解表现出高灵敏度和特异性。这里开发的底物可能会作为高通量筛选测定试剂,用于鉴定 Dop 抑制剂。

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