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Discovery of quorum quenchers targeting the membrane-embedded sensor domain of the<i>Staphylococcus aureus</i>receptor histidine kinase, AgrC

Qian Xie, Mareike M. Wiedmann, Aishan Zhao, Ivelisse Rodriguez Pagan, Richard P. Novick, Hiroaki Suga, Tom W. Muir

2020Chemical Communications27 citationsDOIOpen Access PDF

Abstract

We combined mRNA display technology with lipid-nanodisc based selections and identified high-affinity ligands targeting the integral membrane sensor domain of the histidine kinase AgrC as potent inhibitors of Staphylococcus aureus quorum sensing-modulated virulence. Our study highlights the potential of this integrated approach for identifying functional modulators of integral membrane proteins.

Topics & Concepts

Histidine kinaseQuorum sensingStaphylococcus aureusChemistryHistidineKinaseBiochemistryBiophysicsCombinatorial chemistryBiologyBacteriaEnzymeGeneticsGeneVirulenceAntimicrobial Resistance in StaphylococcusBiochemical and Structural CharacterizationBacterial biofilms and quorum sensing
Discovery of quorum quenchers targeting the membrane-embedded sensor domain of the<i>Staphylococcus aureus</i>receptor histidine kinase, AgrC | Litcius