論文

査読有り
2009年11月

Revisiting AI-2 Quorum Sensing Inhibitors: Direct Comparison of Alkyl-DPD Analogues and a Natural Product Fimbrolide

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
  • Colin A. Lowery
  • ,
  • Takumi Abe
  • ,
  • Junguk Park
  • ,
  • Lisa M. Eubanks
  • ,
  • Daisuke Sawada
  • ,
  • Gunnar F. Kaufmann
  • ,
  • Kim D. Janda

131
43
開始ページ
15584
終了ページ
+
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1021/ja9066783
出版者・発行元
AMER CHEMICAL SOC

Quorum sensing (QS) systems have been discovered in a wide variety of bacteria, and mediate both intra- and interspecies communication. The AI-2-based QS system represents the most studied of these proposed interspecies systems and has been shown to regulate diverse functions such as bioluminescence, expression of virulence factors, and biofilm formation. As such, the development of modulatory compounds, both agonists and antagonists, is of great interest for the study of unknown AI-2-based QS systems and the potential treatment of bacterial infections. The fimbrolide class of natural products has exhibited excellent inhibitory activity against AI-2-based QS and as such may be considered the "gold standard" of AI-2 inhibitors. Thus, we sought to include a fimbrolide as a control compound for our recently developed alkyl-DPD panel of AI-2 modulators. Herein, we present a revised synthesis of a commonly studied fimbrolide as well as a direct comparison between the fimbrolide and alkyl-DPD analogues. We demonstrate that our alkyl-DPD analogues are more potent inhibitors of QS in both Vibrio harveyi and Salmonella typhimurium, the two organisms with defined AI-2 QS systems, and in doing so call into question the widely accepted use of fimbrolide-derived compounds as the "gold standard" of AI-2 inhibition.

リンク情報
DOI
https://doi.org/10.1021/ja9066783
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/19824634
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000271513600009&DestApp=WOS_CPL
Scopus
https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=70350633944&origin=inward
Scopus Citedby
https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=70350633944&origin=inward
ID情報
  • DOI : 10.1021/ja9066783
  • ISSN : 0002-7863
  • eISSN : 1520-5126
  • PubMed ID : 19824634
  • SCOPUS ID : 70350633944
  • Web of Science ID : WOS:000271513600009

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