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Small molecules that modulate quorum sensing and control virulence in Pseudomonas aeruginosa.调节铜绿假单胞菌群体感应并控制其毒力的小分子。
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Medicinal chemistry as a conduit for the modulation of quorum sensing.作为群体感应调节途径的药物化学
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Biochemical target isolation for novices: affinity-based strategies.新手的生化靶点分离：基于亲和力的策略。
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Synthesis and validation of a probe to identify quorum sensing receptors.合成并验证一种用于识别群体感应受体的探针。
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Click chemistry and bioorthogonal reactions: unprecedented selectivity in the labeling of biological molecules.点击化学与生物正交反应：生物分子标记中前所未有的选择性。
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Cu-catalyzed azide-alkyne cycloaddition.铜催化的叠氮化物-炔烃环加成反应
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Modulation of gene expression via disruption of NF-kappaB signaling by a bacterial small molecule.通过一种细菌小分子破坏核因子-κB信号传导来调节基因表达。
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The quorum quenching antibody RS2-1G9 protects macrophages from the cytotoxic effects of the Pseudomonas aeruginosa quorum sensing signalling molecule N-3-oxo-dodecanoyl-homoserine lactone.群体感应淬灭抗体RS2-1G9可保护巨噬细胞免受铜绿假单胞菌群体感应信号分子N-3-氧代十二烷酰高丝氨酸内酯的细胞毒性作用。
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Environmental regulation of Pseudomonas aeruginosa PAO1 Las and Rhl quorum-sensing systems.铜绿假单胞菌PAO1群体感应系统Las和Rhl的环境调控
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'点击化学'酰基高丝氨酸内酯群体感应探针的合成：对哺乳动物细胞激活的意外影响。

Synthesis of 'clickable' acylhomoserine lactone quorum sensing probes: unanticipated effects on mammalian cell activation.

机构信息

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

出版信息

Bioorg Med Chem Lett. 2011 May 1;21(9):2702-5. doi: 10.1016/j.bmcl.2010.11.122. Epub 2010 Dec 4.

DOI:10.1016/j.bmcl.2010.11.122
PMID:21190852
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3081916/
Abstract

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.

摘要

炔基-和叠氮基标记的 3-氧代-C(12)-酰基高丝氨酸内酯探针已被合成，以研究它们作为发现铜绿假单胞菌自动诱导物，3-氧代-C(12)-酰基高丝氨酸内酯的哺乳动物蛋白靶标的探针的潜在用途。尽管这种取代通常被认为是相当保守的，但通过这些研究，我们发现炔基-和叠氮基修饰化合物之间的活性有很大差异，并提供了一个例子，证明这种结构修饰远非保守。