ArticleNature chemical biology2020
Discovery of an antivirulence compound that reverses β-lactam resistance in MRSA.
Article in Nature chemical biology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 87 citations in OpenAlex.
- Elucidating the Staphylococcus aureus TSST-1 Regulatory Network as a Response to Vaginal pH.Molecular microbiology · 2026Article
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- Gastrodin Inhibits Bacterial Biofilm Formation, Thereby Activating the Antibacterial Activity of Antibiotics.Molecules (Basel, Switzerland) · 2026Article
- Photochemical modification of two fluorene-based molecules with DNA intercalating and anti-methicillin resistant Staphylococcus aureus activity.The Journal of biological chemistry · 2026Article
- Inhibition of Candida albicans yeast-to-hypha transition and virulence by cyclic dipeptides derived from probiotic Aeromonas veronii V03.Scientific reports · 2026Article
- Chemical-mediated alteration of antibiotic susceptibility: mechanisms and potential new targets for antibiotic adjuvant discovery.Journal of bacteriology · 2026Review
- YZ462 exhibits potent antibacterial activity against methicillin-resistant Staphylococcus aureus through bacterial membrane disruption.BMC microbiology · 2025Article
- ThemBio · 2025Article
- Salmonella stress response systems as targets for anti-virulence strategies.BMC microbiology · 2025Article
- Synergistic interaction of amphotericin B and betulinic acid against clinically important fungi: evidence fromMicrobiology spectrum · 2025Article
- Structure-activity relationship study of benserazide derivatives as PilB inhibitors.RSC advances · 2025Article
- The Next Frontier: Unveiling Novel Approaches for Combating Multidrug-Resistant Bacteria.Pharmaceutical research · 2025Review
- The inhibitory effect of the methanolic extract and the essence ofIranian journal of microbiology · 2025Article
- Mechanistic insights into the multitarget synergistic efficacy of farrerol and β-lactam antibiotics in combating methicillin-resistantAntimicrobial agents and chemotherapy · 2025Article
- A screen for cell envelope stress uncovers an inhibitor of prolipoprotein diacylglyceryl transferase, Lgt, iniScience · 2024Article
- Guarding the walls: the multifaceted roles of Bce modules in cell envelope stress sensing and antimicrobial resistance.Journal of bacteriology · 2024Review
- Discovery of an antivirulence compound that targets the Staphylococcus aureus SaeRS two-component system to inhibit toxic shock syndrome toxin-1 production.The Journal of biological chemistry · 2024Article
- Pyrrole-based inhibitors of RND-type efflux pumps reverse antibiotic resistance and display anti-virulence potential.PLoS pathogens · 2024Article
- Sensitizing methicillin-resistantAntimicrobial agents and chemotherapy · 2024Article
- Recent Advances in Strategies to Combat Bacterial Drug Resistance: Antimicrobial Materials and Drug Delivery Systems.Pharmaceutics · 2023Review
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Authors and funding
13 authors at 5 institutions in 2 countries.
Funding
Abstract
Staphylococcus aureus is the leading cause of infections worldwide, and methicillin-resistant strains (MRSA) are emerging. New strategies are urgently needed to overcome this threat. Using a cell-based screen of ~45,000 diverse synthetic compounds, we discovered a potent bioactive, MAC-545496, that reverses β-lactam resistance in the community-acquired MRSA USA300 strain. MAC-545496 could also serve as an antivirulence agent alone; it attenuates MRSA virulence in Galleria mellonella larvae. MAC-545496 inhibits biofilm formation and abrogates intracellular survival in macrophages. Mechanistic characterization revealed MAC-545496 to be a nanomolar inhibitor of GraR, a regulator that responds to cell-envelope stress and is an important virulence factor and determinant of antibiotic resistance. The small molecule discovered herein is an inhibitor of GraR function. MAC-545496 has value as a research tool to probe the GraXRS regulatory system and as an antibacterial lead series of a mechanism to combat drug-resistant Staphylococcal infections.
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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.