ArticleScientific reports2016
Design and characterization of a polyamine derivative inhibiting the expression of type III secretion system in Pseudomonas aeruginosa.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 14 citations in OpenAlex.
- Article
- Genetic and Environmental Investigation of a Novel Phenylamino Acetamide Inhibitor of the Pseudomonas aeruginosa Type III Secretion System.Applied and environmental microbiology · 2023Article
- Spermidine Is an Intercellular Signal Modulating T3SS Expression in Pseudomonas aeruginosa.Microbiology spectrum · 2022Article
- Possible drugs for the treatment of bacterial infections in the future: anti-virulence drugs.The Journal of antibiotics · 2021Review
- The Roles of Microbial Cell-Cell Chemical Communication Systems in the Modulation of Antimicrobial Resistance.Antibiotics (Basel, Switzerland) · 2020Review
- Immunological blocking of spermidine-mediated host-pathogen communication provides effective control against Pseudomonas aeruginosa infection.Microbial biotechnology · 2020Article
- On the road to structure-based development of anti-virulence therapeutics targeting the type III secretion system injectisome.MedChemComm · 2019Review
- Fitting Pieces into the Puzzle ofJournal of bacteriology · 2019Review
- ASC acts in a caspase-1-independent manner to worsen acute pneumonia caused by Pseudomonas aeruginosa.Journal of medical microbiology · 2018Article
- Human Salivary Protein Histatin 5 Has Potent Bactericidal Activity against ESKAPE Pathogens.Frontiers in cellular and infection microbiology · 2017Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The type III secretion system (TTSS) of Pseudomonas aeruginosa is a key virulence determinant for infection of eukaryotic hosts. Based on the findings that spermidine-mediated host-pathogen signalling is important for activation of type III secretion systems (TTSS), in this study, we designed, synthesized and evaluated a series of polyamine derivatives for their potentials in inhibiting the expression TTSS in P. aeruginosa. In vitro assay of 15 compounds synthesized in this study unveiled stringent structural requirements for TTSS-inhibitory activity. Among them, R101SPM, a conjugate between rhodamine 101 and spermine, showed a potent activity in inhibition of the TTSS gene expression and in attenuation of the TTSS-mediated cytotoxicity on human cells. In vivo analysis demonstrated that R101SPM could rescue mice from the lethal infection by P. aeruginosa. Moreover, genetic analysis showed that the full TTSS-inhibitory activity of R101SPM required a functional spermidine transporter. Taken together, our results present a new class of lead molecules for developing anti-virulence drugs and demonstrate that the spermidine transporter SpuDEGHF of P. aeruginosa is a promising drug target.
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