Synthesis of 'clickable' acylhomoserine lactone quorum sensing probes: Unanticipated effects on mammalian cell activation
Synthesis of 'clickable' acylhomoserine lactone quorum sensing probes: Unanticipated effects on mammalian cell activation
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DOI：
10.1016/j.bmcl.2010.11.122
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发表时间：
2011-05-01
影响因子：
2.7
通讯作者：
Janda, Kim D.
中科院分区：
文献类型：
--
作者：
Garner, Amanda L.;Yu, Jing;Janda, Kim D.
已合成了炔基-和叠氮基-标记的3-氧代-C-12-酰基高丝氨酸内酯探针，以检查它们作为用于发现铜绿假单胞菌自诱导物3-氧代-C-12-酰基高丝氨酸内酯的哺乳动物蛋白质靶标的探针的潜在效用。虽然这样的取代通常被认为是相当保守的，但从这些研究中，我们已经发现了炔基修饰的化合物和叠氮基修饰的化合物之间的活性的巨大差异，并提供了这样的结构修饰已被证明远低于保守的实例。(C)2010爱思唯尔有限公司版权所有。
Alkynyl- and azido-tagged 3-oxo-C-12-acylhomoserine lactone probes have been synthesized to examine their potential utility as probes for discovering the mammalian protein target of the Pseudomonas aeruginosa autoinducer, 3-oxo-C-12-acylhomoserine lactone. Although such substitutions are commonly believed to be quite conservative, from these studies, we have uncovered a drastic difference in activity between the alkynyl- and azido-modified compounds, and provide an example where such structural modification has proved to be much less than conservative. (C) 2010 Elsevier Ltd. All rights reserved.