ArticleScientific reports2015
Mechanistic analysis of a synthetic inhibitor of the Pseudomonas aeruginosa LasI quorum-sensing signal synthase.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 33 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
33 citing papers in PubMed, 72 citations in OpenAlex.
- Quorum sensing inhibition strategies for the control of Pseudomonas aeruginosa infections.World journal of microbiology & biotechnology · 2026Review
- Novel Pyridine-Based Thiazolyl-Hydrazone as a Promising Attenuator ofInternational journal of molecular sciences · 2026Article
- Updates on therapeutic targeting of diguanylate cyclase for addressing bacterial infections: A comprehensive review.World journal of microbiology & biotechnology · 2025Review
- In silico analysis of quorum sensing modulators: Insights into molecular docking and dynamics and potential therapeutic applications.PloS one · 2025Article
- Molecular simulation-based investigation of thiazole derivatives as potential LasR inhibitors of Pseudomonas aeruginosa.PloS one · 2025Article
- Article
- Beyond Antibiotics: What the Future Holds.Antibiotics (Basel, Switzerland) · 2024Review
- Quorum Quenching Approaches against Bacterial-Biofilm-Induced Antibiotic Resistance.Antibiotics (Basel, Switzerland) · 2024Review
- Lipid Nanocarriers-Enabled Delivery of Antibiotics and Antimicrobial Adjuvants to Overcome Bacterial Biofilms.Pharmaceutics · 2024Review
- Thiazolidin-4-Ones as a Promising Scaffold in the Development of Antibiofilm Agents-A Review.International journal of molecular sciences · 2023Review
- Article
- The Anti-Virulence Activities of the Antihypertensive Drug Propranolol in Light of Its Anti-Quorum Sensing Effects againstBiomedicines · 2023Article
- A clash of quorum sensing vs quorum sensing inhibitors: an overview and risk of resistance.Archives of microbiology · 2023Review
- Antibiofilm properties of cathelicidin LL-37: an in-depth review.World journal of microbiology & biotechnology · 2023Review
- Anti-quorum sensing potential of selenium nanoparticles against LasI/R, RhlI/R, and PQS/MvfR inFrontiers in molecular biosciences · 2023Article
- Hiring of the Anti-Quorum Sensing Activities of Hypoglycemic Agent Linagliptin to Alleviate theMicroorganisms · 2022Article
- Targeting the Holy Triangle of Quorum Sensing, Biofilm Formation, and Antibiotic Resistance in Pathogenic Bacteria.Microorganisms · 2022Review
- Repurposing phytochemicals as anti-virulent agents to attenuate quorum sensing-regulated virulence factors and biofilm formation in Pseudomonas aeruginosa.Microbial biotechnology · 2022Review
- Anti-Quorum Sensing Activities of Gliptins againstBiomedicines · 2022Article
- The role of bacterial signaling networks in antibiotics response and resistance regulation.Marine life science & technology · 2022Review
Corrections and comments
- Erratum issued
Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
Pseudomonas aeruginosa is an opportunistic Gram-negative pathogen responsible for many human infections. LasI is an acyl-homoserine lactone synthase that produces a quorum-sensing (QS) signal that positively regulates numerous P. aeruginosa virulence determinants. The inhibition of the LasI protein is therefore an attractive drug target. In this study, a novel in silico to in vitro complementation was applied to screen thiazolidinedione-type compounds for their ability to inhibit biofilm formation at concentrations not affecting bacterial growth. The compound (z)-5-octylidenethiazolidine-2, 4-dione (TZD-C8) was a strong inhibitor of biofilm formation and chosen for further study. Structural exploration of in silico docking predicted that the compound had high affinity for the LasI activity pocket. The TZD-C8 compound was also predicted to create hydrogen bonds with residues Arg30 and Ile107. Site-directed mutagenesis (SDM) of these two sites demonstrated that TZD-C8 inhibition was abolished in the lasI double mutant PAO-R30D, I107S. In addition, in vitro swarming motility and quorum sensing signal production were affected by TZD-C 8, confirming this compound alters the cell to cell signalling circuitry. Overall, this novel inhibitor of P. aeruginosa quorum sensing shows great promise and validates our mechanistic approach to discovering inhibitors of LuxI-type acyl-homoserine lactone synthases.
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What OpenQuestion holds
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.