Development of a novel series of non-natural triaryl agonists and antagonists of the Pseudomonas aeruginosa LasR quorum sensing receptor
Development of a novel series of non-natural triaryl agonists and antagonists of the Pseudomonas aeruginosa LasR quorum sensing receptor
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DOI：
10.1016/j.bmc.2016.10.021
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发表时间：
2017-01-01
影响因子：
3.5
通讯作者：
Perez, Lark J.
中科院分区：
文献类型：
--
作者：
Capilato, Joseph N.;Philippi, Shane V.;Perez, Lark J.
细菌通过一种称为群体感应（QS）的过程进行化学交流，在许多细菌病原体的感染中起着核心作用。铜绿假单胞菌的群体感应采用一系列小分子受体，包括主QS调节器LasR。在本研究中，我们使用结构活性关系研究和计算模型相结合的方法研究了非天然三芳基系列激光激光配体。这些研究已经确定了配体结合的关键结构要求，并揭示了诱导治疗相关的LasR拮抗的新策略。(C) 2016 Elsevier Ltd.版权所有。
Bacterial chemical communication, through a process called quorum sensing (QS), plays a central role in infection in numerous bacterial pathogens. Quorum sensing in Pseudomonas aeruginosa employs a series of small molecule receptors including the master QS regulator, LasR. In this study we investigate a nonnatural triaryl series of LasR ligands using a combination of structure activity relationship studies and computational modeling. These studies have enabled the identification of key structural requirements for ligand binding and have revealed a new strategy for inducing the therapeutically relevant antagonism of LasR. (C) 2016 Elsevier Ltd. All rights reserved.