ArticleAntimicrobial agents and chemotherapy2011
Novel inhibitors of the Pseudomonas aeruginosa virulence factor LasB: a potential therapeutic approach for the attenuation of virulence mechanisms in pseudomonal infection.
Article in Antimicrobial agents and chemotherapy, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 56 papers.
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Who cites it
56 citing papers in PubMed, 111 citations in OpenAlex.
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- Synchronous natural infection of Nile tilapia (Oreochromis niloticus) by drug-resistant Pseudomonas aeruginosa and Saprolegnia parasitica: insights into water quality, phenotypic traits, and genotypic profiles.Veterinary research communications · 2025Article
- Sulfur starvation induces an Fe-replete response and attenuates virulence pathways in Pseudomonas aeruginosa PAO1.BMC microbiology · 2025Article
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- Dipeptidic Phosphonates: Potent Inhibitors of Pseudomonas aeruginosa Elastase B Showing Efficacy in a Murine Keratitis Model.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Exploring Proteases as Alternative Molecular Targets to Tackle Inflammation in Cystic Fibrosis Respiratory Infections.International journal of molecular sciences · 2025Review
- Uncovering antibiotic resistance: extended-spectrum beta-lactamase-producingFrontiers in microbiology · 2025Article
- Exiguolysin, a Novel Thermolysin (M4) Peptidase fromMicroorganisms · 2024Article
- Does Every Strain ofPathogens (Basel, Switzerland) · 2024Article
- Optimized preparation pipeline for emergency phage therapy against Pseudomonas aeruginosa at Yale University.Scientific reports · 2024Article
- Insights into Kinases of ESKAPE Pathogens for Therapeutic Interventions.Cardiovascular & hematological agents in medicinal chemistry · 2024Review
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- Inhibitors of the Elastase LasB for the Treatment ofACS central science · 2023Article
- Cold atmospheric pressure plasma-antibiotic synergy inBiofilm · 2023Article
- Biosurfactant derived from probiotic Lactobacillus acidophilus exhibits broad-spectrum antibiofilm activity and inhibits the quorum sensing-regulated virulence.Biomolecules & biomedicine · 2023Article
- Chemical Optimization of SelectiveACS infectious diseases · 2023Article
- In Vivo Role of Two-Component Regulatory Systems in Models of Urinary Tract Infections.Pathogens (Basel, Switzerland) · 2023Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pseudomonas elastase (LasB), a metalloprotease virulence factor, is known to play a pivotal role in pseudomonal infection. LasB is secreted at the site of infection, where it exerts a proteolytic action that spans from broad tissue destruction to subtle action on components of the host immune system. The former enhances invasiveness by liberating nutrients for continued growth, while the latter exerts an immunomodulatory effect, manipulating the normal immune response. In addition to the extracellular effects of secreted LasB, it also acts within the bacterial cell to trigger the intracellular pathway that initiates growth as a bacterial biofilm. The key role of LasB in pseudomonal virulence makes it a potential target for the development of an inhibitor as an antimicrobial agent. The concept of inhibition of virulence is a recently established antimicrobial strategy, and such agents have been termed "second-generation" antibiotics. This approach holds promise in that it seeks to attenuate virulence processes without bactericidal action and, hence, without selection pressure for the emergence of resistant strains. A potent inhibitor of LasB, N-mercaptoacetyl-Phe-Tyr-amide (K(i) = 41 nM) has been developed, and its ability to block these virulence processes has been assessed. It has been demonstrated that thes compound can completely block the action of LasB on protein targets that are instrumental in biofilm formation and immunomodulation. The novel LasB inhibitor has also been employed in bacterial-cell-based assays, to reduce the growth of pseudomonal biofilms, and to eradicate biofilm completely when used in combination with conventional antibiotics.
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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.