A Small Molecule That Inhibits the Quorum Sensing Receptor AgrC in Staphylococcus aureus
Thomas J. Polaske, Troy D. Vulpis, Alexandra E. Nelson, Ke Zhao, Helen E. Blackwell
TL;DR
Researchers developed a small molecule, CP-20, that effectively inhibits a key receptor in Staphylococcus aureus, which could help reduce its virulence.
Contribution
The discovery of a synthetically tractable small molecule that completely inhibits quorum sensing in Staphylococcus aureus.
Findings
CP-20 derivative inhibits quorum sensing with mid-nanomolar potency.
CP-20 binds AgrC and competitively inhibits its activity in vitro.
CP-20 is a versatile probe for studying Staphylococcal virulence.
Abstract
We report the synthesis and characterization of a small molecule, CP-20, capable of inhibiting the key quorum sensing receptor AgrC in Staphylococcus aureus. Structural alterations enabled the discovery of a CP-20 derivative that is capable of complete quorum sensing inhibition with mid-nanomolar potency. In vitro biochemical investigations support CP-20 binding AgrC and competitively inhibiting its activity. CP-20 represents a versatile and synthetically tractable small molecule probe for investigating Staphylococcal virulence via quorum sensing modulation.
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Taxonomy
TopicsAntimicrobial Resistance in Staphylococcus · Bacterial biofilms and quorum sensing · Biochemical and Structural Characterization