ArticleNature communications2020
Discovery of gramicidin A analogues with altered activities by multidimensional screening of a one-bead-one-compound library.
Article in Nature communications, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 49 citations in OpenAlex.
- Discovery of leucine analogues of tyrocidines and tryptocidines fromSynthetic and systems biotechnology · 2027Article
- Gramicidin D as a Multi-Target Antimicrobial Against Staphylococcus aureus: Biofilm Disruption, Virulence Attenuation, Antibiotic Potentiation, and Protein-Peptide Docking Insight.Probiotics and antimicrobial proteins · 2026Article
- Liposomal nanoprobes actuated by engineered water channels for sensitive detection of molecular targets by MRI.Nature biomedical engineering · 2026Article
- Overlooked Complications and Opportunities in the Development of Drugs Based upon Macrobicyclic Peptides: The "Homeomorphic Switch".Journal of the American Chemical Society · 2026Review
- Antifungal Biocontrol in Sustainable Crop Protection: Microbial Lipopeptides, Polyketides, and Plant-Derived Agents.Journal of fungi (Basel, Switzerland) · 2025Review
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- Bacterial Extracellular Vesicles and Antimicrobial Peptides: A Synergistic Approach to Overcome Antimicrobial Resistance.Antibiotics (Basel, Switzerland) · 2025Review
- Recent exploration of γ-AApeptide based antimicrobial peptide mimics as potential therapeutics towards drug-resistant bacteria.Exploration of drug science · 2025Article
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- Antibiotics: From Mechanism of Action to Resistance and Beyond.Indian journal of microbiology · 2024Review
- Costunolide Inhibits Chronic Kidney Disease Development by Attenuating IKKβ/NF-κB Pathway.Drug design, development and therapy · 2024Article
- Microbial- and Plant-Derived Bioactive Peptides and Their Applications against Foodborne Pathogens: Current Status and Future Prospects.International journal of microbiology · 2024Review
- Genomic Based Analysis of the Biocontrol SpeciesJournal of fungi (Basel, Switzerland) · 2023Article
- High-Throughput Screening of Natural Product and Synthetic Molecule Libraries for Antibacterial Drug Discovery.Metabolites · 2023Review
- Antibiotic Susceptibility Testing with Raman Biosensing.Antibiotics (Basel, Switzerland) · 2022Review
- Advancements in antimicrobial nanoscale materials and self-assembling systems.Chemical Society reviews · 2022Review
- Article
- Gramicidin A accumulates in mitochondria, reduces ATP levels, induces mitophagy, and inhibits cancer cell growth.Chemical science · 2022Article
- Ion Channels and Transporters as Therapeutic Agents: From Biomolecules to Supramolecular Medicinal Chemistry.Biomedicines · 2022Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Gramicidin A (1) is a peptide antibiotic that disrupts the transmembrane ion concentration gradient by forming an ion channel in a lipid bilayer. Although long used clinically, it is limited to topical application because of its strong hemolytic activity and mammalian cytotoxicity, likely arising from the common ion transport mechanism. Here we report an integrated high-throughput strategy for discovering analogues of 1 with altered biological activity profiles. The 4096 analogue structures are designed to maintain the charge-neutral, hydrophobic, and channel forming properties of 1. Synthesis of the analogues, tandem mass spectrometry sequencing, and 3 microscale screenings enable us to identify 10 representative analogues. Re-synthesis and detailed functional evaluations find that all 10 analogues share a similar ion channel function, but have different cytotoxic, hemolytic, and antibacterial activities. Our large-scale structure-activity relationship studies reveal the feasibility of developing analogues of 1 that selectively induce toxicity toward target organisms.
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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.