ArticleScientific reports2022
Discovery of first-in-class nanomolar inhibitors of heptosyltransferase I reveals a new aminoglycoside target and potential alternative mechanism of action.
Article in Scientific reports, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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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.
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Who cites it
4 citing papers in PubMed, 9 citations in OpenAlex.
- Design, Synthesis, and Biological Evaluation of 6″-Modified Apramycin Derivatives to Overcome Aminoglycoside Resistance.Pharmaceutics · 2025Article
- Potentiating Activity of GmhA Inhibitors on Gram-Negative Bacteria.Journal of medicinal chemistry · 2024Article
- Making a chink in their armor: Current and next-generation antimicrobial strategies against the bacterial cell envelope.Advances in microbial physiology · 2023Article
- StandardisedFrontiers in pharmacology · 2022Article
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
A clinically relevant inhibitor for Heptosyltransferase I (HepI) has been sought after for many years because of its critical role in the biosynthesis of lipopolysaccharides on bacterial cell surfaces. While many labs have discovered or designed novel small molecule inhibitors, these compounds lacked the bioavailability and potency necessary for therapeutic use. Extensive characterization of the HepI protein has provided valuable insight into the dynamic motions necessary for catalysis that could be targeted for inhibition. Structural inspection of Kdo
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Registered trials
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