ArticleNature2010
Type IIA topoisomerase inhibition by a new class of antibacterial agents.
Article in Nature, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 325 papers, 1 of them a synthesis that pooled it.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
325 citing papers in PubMed, 1 synthesis or guideline pooled it, 819 citations in OpenAlex.
- Efficacy and safety of Gepotidacin for urogenital infections: a systematic review and meta-analysis of randomized controlled trials.Infection · 2026Pooled it
- Gepotidacin and Early Symptom Improvement in Uncomplicated Urinary Tract Infection: A Nonrandomized Clinical Trial.JAMA network open · 2026Trial
- Efficacy andAntimicrobial agents and chemotherapy · 2025Trial
- Efficacy andAntimicrobial agents and chemotherapy · 2025Trial
- BWC0977, a broad-spectrum antibacterial clinical candidate to treat multidrug resistant infections.Nature communications · 2024Trial
- Pharmacokinetics, safety, and tolerability of gepotidacin administered as single or repeat ascending doses, in healthy adults and elderly subjects.Clinical and translational science · 2022Trial
- Pharmacokinetics of Oral Formulations of Gepotidacin (GSK2140944), a Triazaacenaphthylene Bacterial Type II Topoisomerase Inhibitor, in Healthy Adult and Adolescent Participants.Antimicrobial agents and chemotherapy · 2022Trial
- Microbiome recovery in adult females with uncomplicated urinary tract infections in a randomised phase 2A trial of the novel antibiotic gepotidacin (GSK140944).BMC microbiology · 2021Trial
- Phase 2a Pharmacokinetic, Safety, and Exploratory Efficacy Evaluation of Oral Gepotidacin (GSK2140944) in Female Participants with Uncomplicated Urinary Tract Infection (Acute Uncomplicated Cystitis).Antimicrobial agents and chemotherapy · 2020Trial
- A comprehensive review of small molecule drugs approved by the FDA in 2025: advance and prospect.Journal of enzyme inhibition and medicinal chemistry · 2026Review
- Characterization of isolates from two phase 3 uncomplicated urinary tract infection trials (EAGLE-2 and EAGLE-3) that show an apparent ≥4-fold increase in gepotidacin MIC between baseline and post-baseline visits.JAC-antimicrobial resistance · 2026Article
- Novel Bacterial Topoisomerase Inhibitors: A New Front in an Old War.Journal of molecular biology · 2026Review
- Molecular Docking of Natural Products: Critical Appraisal of Current Methodology and Practical Guidelines.Molecules (Basel, Switzerland) · 2026Review
- Characterization of gepotidacin activity, includingMicrobiology spectrum · 2026Article
- Designing the DNA-Intercalating Moiety to Improve the Safety and Efficacy of Novel Bacterial Topoisomerase Inhibitors.Journal of medicinal chemistry · 2026Article
- Article
- Biotransformation of Coumarins: Mechanisms and Pharmaceutical Potential.Molecules (Basel, Switzerland) · 2026Review
- Integrated experimental and computational characterization of bioactive metabolites from Streptomyces paradoxus GH53 with antimicrobial, antioxidant, and antitumor activities.Scientific reports · 2026Article
- Oral Gepotidacin for the Treatment of Uncomplicated Urogenital Gonorrhea: Nucleic Acid Amplification Testing Outcomes in a Randomized, Multicenter Phase 3 Trial (EAGLE-1).Open forum infectious diseases · 2026Article
- AssessingbioRxiv : the preprint server for biology · 2026Article
265 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
25 authors at 4 institutions in 2 countries.
Funding
Abstract
Despite the success of genomics in identifying new essential bacterial genes, there is a lack of sustainable leads in antibacterial drug discovery to address increasing multidrug resistance. Type IIA topoisomerases cleave and religate DNA to regulate DNA topology and are a major class of antibacterial and anticancer drug targets, yet there is no well developed structural basis for understanding drug action. Here we report the 2.1 A crystal structure of a potent, new class, broad-spectrum antibacterial agent in complex with Staphylococcus aureus DNA gyrase and DNA, showing a new mode of inhibition that circumvents fluoroquinolone resistance in this clinically important drug target. The inhibitor 'bridges' the DNA and a transient non-catalytic pocket on the two-fold axis at the GyrA dimer interface, and is close to the active sites and fluoroquinolone binding sites. In the inhibitor complex the active site seems poised to cleave the DNA, with a single metal ion observed between the TOPRIM (topoisomerase/primase) domain and the scissile phosphate. This work provides new insights into the mechanism of topoisomerase action and a platform for structure-based drug design of a new class of antibacterial agents against a clinically proven, but conformationally flexible, enzyme class.
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What OpenQuestion holds
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.