A strategy for antagonizing quorum sensing. Author Guozhou Chen, Lee Swem, Danielle Swem, Devin Stauff, Colleen O'Loughlin, Philip Jeffrey, Bonnie Bassler, Frederick Hughson Publication Year 2011 Type Journal Article Abstract Quorum-sensing bacteria communicate via small molecules called autoinducers to coordinate collective behaviors. Because quorum sensing controls virulence factor expression in many clinically relevant pathogens, membrane-permeable quorum sensing antagonists that prevent population-wide expression of virulence genes offer a potential route to novel antibacterial therapeutics. Here, we report a strategy for inhibiting quorum-sensing receptors of the widespread LuxR family. Structure-function studies with natural and synthetic ligands demonstrate that the dimeric LuxR-type transcription factor CviR from Chromobacterium violaceum is potently antagonized by molecules that bind in place of the native acylated homoserine lactone autoinducer, provided that they stabilize a closed conformation. In such conformations, each of the two DNA-binding domains interacts with the ligand-binding domain of the opposing monomer. Consequently, the DNA-binding helices are held apart by ∼60 Å, twice the ∼30 Å separation required for operator binding. This approach may represent a general strategy for the inhibition of multidomain proteins. Keywords Quorum Sensing, Repressor Proteins, Trans-Activators, Biofilms, Anti-Bacterial Agents, Dose-Response Relationship, Drug, Molecular Structure, Structure-Activity Relationship, 4-Butyrolactone, Binding Sites, Lactones, Virulence, Mutation, Models, Molecular, Ligands, Chromobacterium, Crystallography, X-Ray, DNA, Protein Conformation Journal Mol Cell Volume 42 Issue 2 Pages 199-209 Date Published 2011 Apr 22 ISSN Number 1097-4164 DOI 10.1016/j.molcel.2011.04.003 Alternate Journal Mol Cell PMCID PMC3092643 PMID 21504831 PubMedPubMed CentralGoogle ScholarBibTeXEndNote X3 XML