Development of a novel series of non-natural triaryl agonists and antagonists of the Pseudomonas aeruginosa LasR quorum sensing receptor

Joseph N. Capilato, Shane V. Philippi, Thomas Reardon, Ashleigh McConnell, Dylan C. Oliver, Amy Warren, Jill S. Adams, Chun Wu, Lark J. Perez

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

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 non-natural 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.

Original languageEnglish (US)
Pages (from-to)153-165
Number of pages13
JournalBioorganic and Medicinal Chemistry
Volume25
Issue number1
DOIs
StatePublished - Jan 1 2017

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint

Dive into the research topics of 'Development of a novel series of non-natural triaryl agonists and antagonists of the Pseudomonas aeruginosa LasR quorum sensing receptor'. Together they form a unique fingerprint.

Cite this