Library screening for synthetic agonists and antagonists of a Pseudomonas aeruginosa autoinducer

Smith KM.; Bu YG.; Suga H.

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Library screening for synthetic agonists and antagonists of a Pseudomonas aeruginosa autoinducer

机译：文库筛选铜绿假单胞菌自动诱导剂的合成激动剂和拮抗剂

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The autoinducer (AI) that initiates the quorum sensing (QS) signaling cascade in Pseudomonas aeruginosa is an acyl-homoserine lactone (acyl-HSL). We initiated a study of the requirements for binding of the Al to its protein effector LasR by synthesizing a library of analogs with the HSL moiety replaced with different amines and alcohols. We tested each compound for both agonist and antagonist activity using a QS-controlled reporter gene assay and found several new agonists and antagonists. A representative antagonist was further tested for its ability to inhibit virulence factors. This data progresses our understanding of the LasR-AI interaction toward the rational design of therapeutic inhibitors of OS. [References: 30]

机译：在铜绿假单胞菌中引发群体感应（QS）信号级联的自动诱导剂（AI）是酰基高丝氨酸内酯（acyl-HSL）。我们通过合成HSL部分被不同的胺和醇取代的类似物文库，开始了对Al与其蛋白效应子LasR结合的要求的研究。我们使用QS控制的报告基因测试了每种化合物的激动剂和拮抗剂活性，并发现了几种新的激动剂和拮抗剂。进一步测试了代表性的拮抗剂抑制毒力因子的能力。这些数据使我们对LasR-AI相互作用的理解朝着OS治疗抑制剂的合理设计发展。 [参考：30]

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《Chemistry & biology》 |2003年第6期|共9页
作者
Smith KM.; Bu YG.; Suga H.;
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正文语种 eng
中图分类化学;
关键词
To-cell communication; Halogenated furanones; Delisea-pulchra; Vibrio-fischeri; Gene-expression; Virulence genes; Analogs; Signal; Inhibition; Bacteria;

机译：细胞间通讯;卤代呋喃酮;Delsea-pulchra;费氏弧菌;基因表达;毒力基因;类似物;信号;抑制;细菌;

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1. Library screening for synthetic agonists and antagonists of a Pseudomonas aeruginosa autoinducer [J] . Smith KM., Bu YG., Suga H. Chemistry & biology . 2003,第6期

机译：文库筛选铜绿假单胞菌自动诱导剂的合成激动剂和拮抗剂
2. Structural Basis for Native Agonist and Synthetic Inhibitor Recognition by the Pseudomonas aeruginosa Quorum Sensing Regulator PqsR (MvfR) [J] . Alex Truman, Aravindan Ilangovan, Christian Pustelny, PLoS Pathogens . 2013,第7期

机译：铜绿假单胞菌群体感应调节剂PqsR（MvfR）的天然激动剂和合成抑制剂识别的结构基础。
3. Potent and Selective Synthetic Modulators of a Quorum Sensing Repressor in Pseudomonas aeruginosa Identified from Second-Generation Libraries of N-Acylated L-Homoserine Lactones [J] . Mattmann M.E., Shipway P.M., Heth N.J., Chembiochem: A European journal of chemical biology . 2011,第6期

机译：从N-酰化的L-高丝氨酸内酯的第二代文库中鉴定出的铜绿假单胞菌群体感应阻遏物的有效和选择性合成调节剂
4. The Agonist/Antagonist Differential-docking Screening (AADS) Method for Exploration of the Estrogen Receptor-binding Chemicals [C] . Takeru Nose, Takatoshi Tokunaga, YasuyuM Shimohigashi Japanese peptide symposium . 2010

机译：激动剂/拮抗剂差动对接筛选（AADS）探索雌激素受体结合化学品的方法
5. Quorum sensing in Pseudomonas aeruginosa: Design, synthesis and analysis of autoinducer analogs as antagonists for the quorum sensing pathway. [D] . Jog, Geetanjali J. 2005

机译：铜绿假单胞菌的群体感应：设计，合成和分析自动诱导类似物作为群体感应途径的拮抗剂。
6. Potent and Selective Synthetic Modulators of a Quorum Sensing Repressor in Pseudomonas aeruginosa Identified from Second-Generation Libraries of N-Acylated l-Homoserine Lactones [O] . Margrith E. Mattmann, Patrick M. Shipway, Nicole J. Heth, -1

机译：铜绿假单胞菌的Quorum传感阻遏物的有效和选择性合成调节剂其从N-酰化L-型甲状甲虫的第二代文库中鉴定
7. Library Screening for Synthetic Agonists and Antagonists of a Pseudomonas aeruginosa Autoinducer [O] . Smith Kristina M., Bu Yigong, Suga Hiroaki 2003

机译：铜绿假单胞菌自动诱导剂的合成激动剂和拮抗剂的库筛选

Library screening for synthetic agonists and antagonists of a Pseudomonas aeruginosa autoinducer

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