ArticleACS infectious diseases2022
Polymyxin Stereochemistry and Its Role in Antibacterial Activity and Outer Membrane Disruption.
Article in ACS infectious diseases, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 44 citations in OpenAlex.
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- A generalizable assay for intracellular accumulation to profile cytosolic drug delivery in mammalian cells.Communications chemistry · 2026Article
- Genome-Driven Discovery of Anti-MDR Bacterial Heptapeptides from a Cold-Seep-DerivedMolecules (Basel, Switzerland) · 2026Article
- Breaking the outer membrane barrier: structure, targets, and antimicrobial strategies for Gram-negative bacteria.Frontiers in microbiology · 2026Review
- Comparative Effectiveness of Colistin Sodium versus Polymyxin B Sulfate Against CR-GNB: A Retrospective Cohort Study.Infection and drug resistance · 2026Article
- Nanozymes modulate probiotic tryptophan metabolism to prevent Salmonella infection in mammalian models.Nature microbiology · 2025Article
- Revolutionizing antibiotic therapy: Polymyxin B and FeJournal of pharmaceutical analysis · 2025Article
- An Rcs Stress-Based High-Throughput Screen Reveals Novel Gyrase Inhibitors as Indirect Inducers of Cell Envelope Stress in Gram-Negative Bacteria.ACS infectious diseases · 2025Article
- Interactions between Lipopolysaccharide and Peptide Bacteriocin BacSp222 Influence Their Biological Activities.ACS infectious diseases · 2025Article
- Design, Synthesis, and Antibacterial Evaluation of Rifampicin-Siderophore Conjugates.ACS infectious diseases · 2025Article
- Development of Broad-Spectrum Antimicrobial Peptides through the Conjugation of FtsZ-Binding and Cell-Penetrating Peptides.ACS infectious diseases · 2025Article
- Specific labeling of outer membrane vesicles with antibiotic-conjugated probe reveals early bacterial infections in blood.Nature communications · 2025Article
- Total Synthesis, Structure Elucidation, and Bioactivity Evaluation of the Cyclic Lipopeptide Natural Product Paenilipoheptin A.Organic letters · 2025Article
- Total Synthesis and Structural Reassignment of the Antitubercular Natural Product Evybactin.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Phytochemical Analysis and Antimicrobial Activity ofMicroorganisms · 2024Article
- Stereorandomized Oncocins with Preserved Ribosome Binding and Antibacterial Activity.Journal of medicinal chemistry · 2024Article
- Activity of polymyxin B combined with cefepime-avibactam against the biofilms of polymyxin B-resistant Pseudomonas aeruginosa and Klebsiella pneumoniae in in vitro and in vivo models.BMC microbiology · 2024Article
- Recent Advances in the Development of Polymyxin Antibiotics: 2010-2023.ACS infectious diseases · 2024Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
With increasing rates of resistance toward commonly used antibiotics, especially among Gram-negative bacteria, there is renewed interested in polymyxins. Polymyxins are lipopeptide antibiotics with potent anti-Gram-negative activity and are generally believed to target lipid A, the lipopolysaccharide (LPS) anchor found in the outer membrane of Gram-negative bacteria. To characterize the stereochemical aspects of their mechanism(s) of action, we synthesized the full enantiomers of polymyxin B and the polymyxin B nonapeptide (PMBN). Both compounds were compared with the natural compounds in biological and biophysical assays, revealing strongly reduced antibacterial activity for the enantiomeric species. The enantiomeric compounds also exhibit reduced LPS binding, lower outer membrane (OM) permeabilization, and loss of synergetic potential. These findings provide new insights into the stereochemical requirements underlying the mechanisms of action of polymyxin B and PMBN.
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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.