ArticleAdvanced science (Weinheim, Baden-Wurttemberg, Germany)2021
A New PqsR Inverse Agonist Potentiates Tobramycin Efficacy to Eradicate Pseudomonas aeruginosa Biofilms.
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In one paragraph
Article in Advanced science (Weinheim, Baden-Wurttemberg, Germany), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers, 1 of them a synthesis that pooled it.
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32citing papers in PubMed, 1 pooled it
3.2field-weighted citation impact, top 7% of its field
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Who cites it
32 citing papers in PubMed, 1 synthesis or guideline pooled it, 56 citations in OpenAlex.
- A bibliometric analysis on discovering anti-quorum sensing agents against clinically relevant pathogens: current status, development, and future directions.Frontiers in microbiology · 2023Pooled it
- Coumarins Disrupt Cell-Cell Communication and Virulence in Priority Pathogens: Targeting the PQS Signalling System in Pseudomonas aeruginosa.Microbial biotechnology · 2026Article
- Quorum Sensing and Quorum Quenching in Pseudomonas aeruginosa and Staphylococcus aureus Infections: Therapeutic Potential, Limitations and Clinical Challenges.Antibiotics (Basel, Switzerland) · 2026Review
- Antibacterial and anti-virulence effects ofMicrobiology spectrum · 2026Article
- Chemical-mediated alteration of antibiotic susceptibility: mechanisms and potential new targets for antibiotic adjuvant discovery.Journal of bacteriology · 2026Review
- Exploiting Pharmacokinetic/Pharmacodynamic Methods for Optimizing and Accelerating Drug Development of Innovative Anti-Infectives.ChemMedChem · 2026Review
- Identification of ferredoxin PA1551 as an antibacterial synergistic target for biofilm inhibitors against Pseudomonas aeruginosa.NPJ biofilms and microbiomes · 2025Article
- 1,2,3-Triazolo-Bridged Click Coupling of Pinane-Based Azidodiol Enantiomers with Pyrimidine- and Purine-Based Building Blocks: Synthesis, Antiproliferative, and Antimicrobial Evaluation.International journal of molecular sciences · 2025Article
- Anti-QS Strategies AgainstMicroorganisms · 2025Review
- Inhibitors of the PqsR Quorum-Sensing Receptor Reveal Differential Roles for PqsE and RhlI in Control of Phenazine Production.ACS chemical biology · 2025Article
- Domain adaptable language modeling of chemical compounds identifies potent pathoblockers for Pseudomonas aeruginosa.Communications chemistry · 2025Article
- From Bones to Bugs: Structure-Based Development of Raloxifene-Derived Pathoblockers That Inhibit Pyocyanin Production inJournal of medicinal chemistry · 2025Article
- Targeting AI-2 quorum sensing: harnessing natural products against Streptococcus suis biofilm infection.Veterinary research · 2025Article
- Nanomaterials Regulate Bacterial Quorum Sensing: Applications, Mechanisms, and Optimization Strategies.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Review
- Multidimensional Criteria for Virtual Screening of PqsR Inhibitors Based on Pharmacophore, Docking, and Molecular Dynamics.International journal of molecular sciences · 2024Article
- Design, Synthesis, and Evaluation of New 1Journal of medicinal chemistry · 2024Article
- New Antimicrobial Strategies to Treat Multi-Drug Resistant Infections Caused by Gram-Negatives in Cystic Fibrosis.Antibiotics (Basel, Switzerland) · 2024Review
- Enzyme-Linked Lipid Nanocarriers for Coping Pseudomonal Pulmonary Infection. Would Nanocarriers Complement Biofilm Disruption or Pave Its Road?International journal of nanomedicine · 2024Article
- Periodically disturbing biofilms reduces expression of quorum sensing-regulated virulence factors iniScience · 2023Article
- Towards Translation of PqsR Inverse Agonists: From In Vitro Efficacy Optimization to In Vivo Proof-of-Principle.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2023Article
Corrections and comments
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Authors and funding
26 authors at 6 institutions in 4 countries.
Christian SchützHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.
Duy-Khiet HoHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0002-7327-6775
Mostafa Mohamed HamedHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.
Ahmed Saad AbdelsamieHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.
Teresa RöhrigHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.
Christian HerrDepartment of Internal Medicine V - Pulmonology, Allergology and Critical Care Medicine, Saarland University, Building 41, Homburg, 66421, Germany.ORCID 0000-0001-9422-6569
Andreas Martin KanyHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0001-7580-3658
Katharina RoxGerman Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.ORCID 0000-0002-8020-1384
Stefan SchmelzGerman Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.ORCID 0000-0002-2511-7593
Lorenz SiebenbürgerPharmBioTec GmbH, Science Park 1, Saarbrücken, 66123, Germany.ORCID 0000-0003-0461-1186
Marius WirthPharmBioTec GmbH, Science Park 1, Saarbrücken, 66123, Germany.
Carsten BörgerPharmBioTec GmbH, Science Park 1, Saarbrücken, 66123, Germany.ORCID 0000-0001-8590-3054
Samir YahiaouiHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.
Robert BalsDepartment of Internal Medicine V - Pulmonology, Allergology and Critical Care Medicine, Saarland University, Building 41, Homburg, 66421, Germany.ORCID 0000-0002-1472-9535
Andrea ScrimaGerman Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.ORCID 0000-0003-2760-611X
Wulf BlankenfeldtGerman Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.ORCID 0000-0001-9886-9668
Justus Constantin HorstmannHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0002-0341-3631
Rebekka ChristmannHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0003-1775-2113
Xabier MurgiaHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0002-6370-9047
Marcus KochLeibniz Institute for New Materials, Campus D2.2, Saarbrücken, 66123, Germany.
Aylin BerwangerHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0002-5921-8181
Brigitta LoretzHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0003-0057-5181
Anna Katharina Herta HirschHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0001-8734-4663
Rolf Wolfgang HartmannHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0002-5871-5231
Claus-Michael LehrHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0002-5864-8462
Martin EmptingHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.ORCID 0000-0002-0503-5830
German Center for Infection Research · DEHelmholtz Centre for Infection Research · DESaarland University · DEGAIKER Technology Centre · ESLeibniz-Institute for New Materials · DEUniversity of Washington · US
Funding
Deutsches Zentrum für Infektionsforschung Flexible Fund TTU09.908H2020 Marie Skłodowska-Curie Actions Grant Agreement No. 642028Helmholtz Association Helmholtz-Validation Fonds HVF0054
Abstract
Pseudomonas aeruginosa (PA) infections can be notoriously difficult to treat and are often accompanied by the development of antimicrobial resistance (AMR). Quorum sensing inhibitors (QSI) acting on PqsR (MvfR) - a crucial transcriptional regulator serving major functions in PA virulence - can enhance antibiotic efficacy and eventually prevent the AMR. An integrated drug discovery campaign including design, medicinal chemistry-driven hit-to-lead optimization and in-depth biological profiling of a new QSI generation is reported. The QSI possess excellent activity in inhibiting pyocyanin production and PqsR reporter-gene with IC
Indexed as
AnimalsBiofilmsDisease Models, AnimalMicePseudomonas aeruginosaPseudomonas InfectionsQuinolonesQuorum SensingTobramycin2-heptyl-3-hydroxy-4-quinoloneQuinolonesTobramycinbiofilm inhibitionnanoparticlesPseudomonas aeruginosaquorum sensing
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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.