活性位点导向的PAL-CC-ABPP探针分子的设计、合成及其应用

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	活性位点导向的PAL-CC-ABPP探针分子的设计、合成及其应用
	仇文卫; 徐杰; 李静雅; 李佳; 南发俊
	2006-07-01
关键词	探针分子非共价作用小分子 PAL-CC-ABPP 功能蛋白质组学 ABPP CC
页码	2
英文摘要	Activity-based protein labeling by affinity chemical probes allows for a proteomic assessment of biochemical interactions, thereby providing comparative indices valuable for research and therapeutics. The utility of a chemical probe, including both specificity and affinity, largely relies on detail knowledge of targeted proteins and ability to synthesize ligands that are covalently active. Hence the challenge to satisfy these two concurrent requirements within one functional moiety often limits the scope of its general applicability. We rationalize that a modular separation of functional groups would be of advantageous. Here we report chemical strategy to synthesize a tri-modular photoaffinity labeling-CC probe (PAL-CC-ABP) with three functional groups for target recognition, proximal target cross-linking and distal reporter tag attachment. By testing a series of these probes for either recombinant or native methionine aminopeptidase and comparing with a conventional strategy, we demonstrate specificity, sensitivity, and the potential of general application of this tri-module strategy in both activity-based protein profiling and target identification of bioactive compounds.
会议录	中国化学会第二十五届学术年会论文摘要集（上册）
文献子类	Article
语种	中文
内容类型	会议论文
源URL	[http://119.78.100.183/handle/2S10ELR8/267556]
专题	国家新药筛选中心
作者单位	中国科学院上海药物研究所,国家新药筛选中心,上海 201203, 中国.
推荐引用方式 GB/T 7714	仇文卫,徐杰,李静雅,等. 活性位点导向的PAL-CC-ABPP探针分子的设计、合成及其应用[C]. 见:.