ArticleAntimicrobial agents and chemotherapy2010
Discovery and characterization of inhibitors of Pseudomonas aeruginosa type III secretion.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 72 papers.
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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
72 citing papers in PubMed, 127 citations in OpenAlex.
- Topical formulation of repurposed FDA-approved compounds inhibits Pseudomonas aeruginosa ExoU and improves corneal infection outcomes.PLoS pathogens · 2026Article
- Anti-infective compounds forSustainable microbiology · 2026Review
- Discovery of synthetic small molecules targeting the central regulator ofScience advances · 2025Article
- Modeling Host-Pathogen Interactions inInternational journal of molecular sciences · 2024Review
- The transcriptional regulators of virulence forGenes & diseases · 2023Review
- Genetic and Environmental Investigation of a Novel Phenylamino Acetamide Inhibitor of the Pseudomonas aeruginosa Type III Secretion System.Applied and environmental microbiology · 2023Article
- Using next generation antimicrobials to target the mechanisms of infection.npj antimicrobials and resistance · 2023Review
- Research Progress on Small Molecular Inhibitors of the Type 3 Secretion System.Molecules (Basel, Switzerland) · 2022Review
- Union Is Strength: Target-Based and Whole-Cell High-Throughput Screens in Antibacterial Discovery.Journal of bacteriology · 2022Review
- Harmine, an inhibitor of the type III secretion system ofFrontiers in cellular and infection microbiology · 2022Article
- Five Plant Natural Products Are Potential Type III Secretion System Inhibitors to Effectively Control Soft-Rot Disease Caused byFrontiers in microbiology · 2022Article
- Identification of Translocation Inhibitors Targeting the Type III Secretion System of Enteropathogenic Escherichia coli.Antimicrobial agents and chemotherapy · 2021Article
- Foundational concepts in the biology of bacterial keratitis.Experimental eye research · 2021Review
- Developing Cyclic Peptomers as Broad-Spectrum Type III Secretion System Inhibitors in Gram-Negative Bacteria.Antimicrobial agents and chemotherapy · 2021Article
- Review
- Baicalin Represses Type Three Secretion System ofMolecules (Basel, Switzerland) · 2021Article
- Molecular Targets and Strategies for Inhibition of the Bacterial Type III Secretion System (T3SS); Inhibitors Directly Binding to T3SS Components.Biomolecules · 2021Review
- Identification of Small Molecules Blocking theBiomolecules · 2021Article
- Prevalence of ExoY Activity inFrontiers in microbiology · 2021Article
- An In Vitro Cell Culture Model for Pyoverdine-Mediated Virulence.Pathogens (Basel, Switzerland) · 2020Article
12 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
The type III secretion system (T3SS) is a clinically important virulence mechanism in Pseudomonas aeruginosa that secretes and translocates up to four protein toxin effectors into human cells, facilitating the establishment and dissemination of infections. To discover inhibitors of this important virulence mechanism, we developed two cellular reporter assays and applied them to a library of 80,000 compounds. The primary screen was based on the dependence of the transcription of T3SS operons on the T3SS-mediated secretion of a negative regulator and consisted of a transcriptional fusion of the Photorhabdus luminescens luxCDABE operon to the P. aeruginosa exoT effector gene. Secondary assays included direct measurements of the T3SS-mediated secretion of a P. aeruginosa ExoS effector-beta-lactamase fusion protein as well as the detection of the secretion of native ExoS by the sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) analysis of culture supernatants. Five inhibitors in three chemical classes were demonstrated to inhibit type III secretion selectively with minimal cytotoxicity and with no effects on bacterial growth or on the type II-mediated secretion of elastase. These inhibitors also block the T3SS-mediated secretion of a YopE effector-beta-lactamase fusion protein from an attenuated Yersinia pestis strain. The most promising of the inhibitors is a phenoxyacetamide that also blocks the T3SS-mediated translocation of effectors into mammalian cells in culture. Preliminary studies of structure-activity relationships in this phenoxyacetamide series demonstrated a strict requirement for the R-enantiomer at its stereocenter and indicated tolerance for a variety of substituents on one of its two aromatic rings.
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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.