ArticleBiochemistry2019
Bimodal Actions of a Naphthyridone/Aminopiperidine-Based Antibacterial That Targets Gyrase and Topoisomerase IV.
Article in Biochemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Mechanism of Action of Gepotidacin: Well-Balanced Dual-Targeting againstACS infectious diseases · 2025Article
- Kinetoplast DNA Decatenation Assay with Eukaryotic Topoisomerase II.Methods in molecular biology (Clifton, N.J.) · 2025Article
- Interactions between Gepotidacin andACS infectious diseases · 2024Article
- Gyrase and Topoisomerase IV: Recycling Old Targets for New Antibacterials to Combat Fluoroquinolone Resistance.ACS infectious diseases · 2024Review
- Novel bacterial topoisomerase inhibitors: unique targeting activities of amide enzyme-binding motifs for tricyclic analogs.Antimicrobial agents and chemotherapy · 2023Article
- Actions of a Novel Bacterial Topoisomerase Inhibitor againstInternational journal of molecular sciences · 2023Article
- Nybomycin inhibits both types ofAntimicrobial agents and chemotherapy · 2023Article
- A Series of Spiropyrimidinetriones that Enhances DNA Cleavage Mediated byACS infectious diseases · 2023Article
- A 2.8 Å Structure of Zoliflodacin in a DNA Cleavage Complex withInternational journal of molecular sciences · 2023Article
- 1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.ACS medicinal chemistry letters · 2022Article
- The Structural Features of Novel Bacterial Topoisomerase Inhibitors That Define Their Activity on Topoisomerase IV.Journal of medicinal chemistry · 2022Review
- HowFrontiers in cellular and infection microbiology · 2022Review
- Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-PositiveACS medicinal chemistry letters · 2020Article
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Authors and funding
6 authors.
Funding
Abstract
Gyrase and topoisomerase IV are the targets of fluoroquinolone antibacterials. However, the rise in antimicrobial resistance has undermined the clinical use of this important drug class. Therefore, it is critical to identify new agents that maintain activity against fluoroquinolone-resistant strains. One approach is to develop non-fluoroquinolone drugs that also target gyrase and topoisomerase IV but interact differently with the enzymes. This has led to the development of the "novel bacterial topoisomerase inhibitor" (NBTI) class of antibacterials. Despite the clinical potential of NBTIs, there is a relative paucity of data describing their mechanism of action against bacterial type II topoisomerases. Consequently, we characterized the activity of GSK126, a naphthyridone/aminopiperidine-based NBTI, against a variety of Gram-positive and Gram-negative bacterial type II topoisomerases, including gyrase from
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