Structurally refined beta-lactones as potent inhibitors of devastating bacterial virulence factors.
Disarmed forces: Inhibition of the central virulence regulator ClpP by structurally refined beta-lactones resulted in dramatically reduced production of devastating virulence factors, including pyrogenic toxin superantigens derived from pathogenic multiresistant Staphylococcus aureus strains. Targeting of this virulence regulator could present an attractive strategy for neutralizing the harmful effects of bacterial pathogens, and help the host immune response to eliminate the disarmed bacteria.
Böttcher
Thomas
T
Center for Integrated Protein Science Munich (CiPSM), Department of Chemistry and Biochemistry, Ludwig-Maximilians-Universität München, Butenandtstrasse 5-13, Munich, Germany.
Sieber
Stephan A
SA
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D000942:Antigens, Bacterial / Q000032:analysis; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors*; D005110:Extracellular Space / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D007118:Immunoassay; D007783:Lactones / Q000737:chemistry* / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000166:cytology / Q000187:drug effects* / Q000276:immunology / Q000378:metabolism; D013237:Stereoisomerism; D037521:Virulence Factors / Q000037:antagonists & inhibitors*
D000900:Anti-Bacterial Agents; D000942:Antigens, Bacterial; D001426:Bacterial Proteins; D007783:Lactones; D037521:Virulence Factors