ArticleACS infectious diseases2019
Simplified Autoinducing Peptide Mimetics with Single-Nanomolar Activity Against the Staphylococcus aureus AgrC Quorum Sensing Receptor.
Article in ACS infectious diseases, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
24 citing papers in PubMed, 44 citations in OpenAlex.
- A secreted AIP-Like peptide fromVirulence · 2026Article
- Targeting Quorum Sensing to Combat Foodborne Pathogens: A Dual Strategy Against Spoilage and Pathogenesis.Foods (Basel, Switzerland) · 2026Review
- A Cyclic Pentapeptide Inhibits AgrC as a Quorum-Sensing Quenching Agent inAntibiotics (Basel, Switzerland) · 2026Article
- Research Progress on Antivirulence Agents Targeting the Accessory Gene Regulator (Agr) System ofInfection and drug resistance · 2026Review
- Article
- Molecular Mechanisms of Virulence Regulation inAccounts of chemical research · 2025Article
- Review
- Non-Membrane Active Peptide Resensitizes MRSA to β-Lactam Antibiotics and Inhibits S. aureus Virulence.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Structural characteristics, functions, and counteracting strategies of biofilms inComputational and structural biotechnology journal · 2025Review
- Beyond Antibiotics: What the Future Holds.Antibiotics (Basel, Switzerland) · 2024Review
- Native Peptide Cyclization, Sequential Chemoselective Amidation in Water.Journal of the American Chemical Society · 2023Article
- Characterization of an Autoinducing Peptide Signal Reveals Highly Efficacious Synthetic Inhibitors and Activators of Quorum Sensing and Biofilm Formation inBiochemistry · 2023Article
- Genomic and Phenotypic Characterization of Mastitis-Causing Staphylococci and Probiotic Lactic Acid Bacteria Isolated from Raw Sheep's Milk.International journal of molecular sciences · 2023Article
- Chemical and biomolecular insights into theIsrael journal of chemistry · 2023Article
- Potent pan-group quorum sensing inhibitors inChemical communications (Cambridge, England) · 2023Article
- The space between us: Modeling spatial heterogeneity in synthetic microbial consortia dynamics.Biophysical reports · 2022Article
- Mechanism of Action of Ribosomally Synthesized and Post-Translationally Modified Peptides.Chemical reviews · 2022Review
- Identification of small molecules that strongly inhibit bacterial quorum sensing using a high-throughput lipid vesicle lysis assay.Cell chemical biology · 2022Article
- Article
- Peptidomimetics as Potential Anti-Virulence Drugs Against Resistant Bacterial Pathogens.Frontiers in microbiology · 2022Review
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Staphylococcus aureus is a leading cause of hospital-acquired infections worldwide, and cases of community-acquired infections are becoming more prevalent. The production of numerous virulence factors in S. aureus is under the control of the accessory gene regulator (agr) quorum sensing (QS) system. S. aureus upregulates agr at high cell density by secreting a peptide pheromone, or autoinducing peptide (AIP), which is detected by its cognate transmembrane receptor, AgrC. The extracellular AIP binding site of AgrC represents an attractive target for inhibition of the agr system and, thereby, QS-controlled virulence in S. aureus. Nonnative peptides and, more recently, peptidomimetics have been reported to inhibit the AgrC receptor and represent useful chemical tools to study the role of QS in S. aureus infections. We seek to expand beyond peptide-like scaffolds to generate AgrC modulators with enhanced stability, solubility, and synthetic accessibility relative to these compounds, while maintaining their high potencies. Toward this goal, we report herein a study of the structure-activity relationships responsible for the activity of a recently reported simplified AIP mimetic and AgrC antagonist, n7OFF, and the discovery of a new AIP mimetic, Bnc3, which has low- to sub-nanomolar inhibitory activity in all four S. aureus agr specificity groups. NMR structural studies of Bnc3 revealed hydrophobic and hydrophilic faces that are likely critical for AgrC antagonism, in agreement with prior studies of peptide-derived inhibitors. Bnc3 represents an important transition compound toward the development of small-molecule AgrC antagonists.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.