ArticleChembiochem : a European journal of chemical biology2021
PEGylated Oligothioetheramide Prodrugs Activated by Host Serum Proteases.
Article in Chembiochem : a European journal of chemical biology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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
1 citing paper in PubMed, 6 citations in OpenAlex.
- Antibacterial Prodrugs to Overcome Bacterial Antimicrobial Resistance.Pharmaceuticals (Basel, Switzerland) · 2024Review
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Due to the increasing prominence of antibiotic resistance, novel drug discovery and delivery approaches targeting bacteria are essential. In this work we evaluate a prodrug design to improve the cytotoxic profile of polycationic oligothioetheramides (oligoTEAs), which are promising antimicrobials. Herein we chemically modify the oligoTEA, PDT-4G, with a polyethylene glycol (PEG) and show that 1, 2, and 5 kDa PEGs mitigate cytotoxicity. As PEGylation reduces antibacterial activity, we evaluate two peptide linkers which, unlike oligoTEAs, are susceptible to proteolytic cleavage in serum. To gain insight into the prodrug reactivation, two linkers were tested, the 5-residue peptide sequence LMPTG, and the dipeptide sequence VC-PABC. In the presence of 20 % serum, prodrugs made with the VC-PABC linker successfully inhibited bacterial growth. Overall, we observed reactivation of oligoTEAs facilitated by serum protease cleavage of the peptide linkers. This work opens the door to the future design of antimicrobial prodrugs with tunable release profiles.
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Registered trials
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