ArticleAngewandte Chemie (International ed. in English)2021
Selective Bacterial Targeting and Infection-Triggered Release of Antibiotic Colistin Conjugates.
Article in Angewandte Chemie (International ed. in English), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 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
9 citing papers in PubMed.
- Scaffold Simplification Yields Potent Antibacterial Agents That Target Bacterial Topoisomerases.Molecules (Basel, Switzerland) · 2026Article
- Overcoming multidrug resistance: antimicrobial peptides as a next-generation therapeutic strategy.Frontiers in cellular and infection microbiology · 2026Review
- Antimicrobial Peptides for Skin Wound Healing.Biomolecules · 2025Review
- Infection-responsive long-term antibacterial bone plates for open fracture therapy.Bioactive materials · 2023Article
- Release of immunomodulatory peptides at bacterial membrane interfaces as a novel strategy to fight microorganisms.The Journal of biological chemistry · 2023Article
- Lectin-Targeted Prodrugs Activated byJournal of medicinal chemistry · 2022Article
- Statistic Copolymers Working as Growth Factor-Binding Mimics of Fibronectin.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Article
- Selective Bacterial Targeting and Infection-Triggered Release of Antibiotic Colistin Conjugates.Angewandte Chemie (International ed. in English) · 2021Article
- Smart Polymeric Delivery System for Antitumor and Antimicrobial Photodynamic Therapy.Frontiers in bioengineering and biotechnology · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In order to render potent, but toxic antibiotics more selective, we have explored a novel conjugation strategy that includes drug accumulation followed by infection-triggered release of the drug. Bacterial targeting was achieved using a modified fragment of the human antimicrobial peptide ubiquicidin, as demonstrated by fluorophore-tagged variants. To limit the release of the effector colistin only to infection-related situations, we introduced a linker that was cleaved by neutrophil elastase (NE), an enzyme secreted by neutrophil granulocytes at infection sites. The linker carried an optimized sequence of amino acids that was required to assure sufficient cleavage efficiency. The antibacterial activity of five regioisomeric conjugates prepared by total synthesis was masked, but was released upon exposure to recombinant NE when the linker was attached to amino acids at the 1- or the 3-position of colistin. A proof-of-concept was achieved in co-cultures of primary human neutrophils and Escherichia coli that induced the secretion of NE, the release of free colistin, and an antibacterial efficacy that was equal to that of free colistin.
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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.