ArticleNature protocols2008
DNA cleavage assay for the identification of topoisomerase I inhibitors.
Article in Nature protocols, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 66 papers.
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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
66 citing papers in PubMed, 105 citations in OpenAlex.
- Novel Camptothecin-Based Lipid Conjugated with Steroids and Triterpene Acids: Enhanced Cellular Uptake and Topoismerase I Inhibition.Pharmaceutics · 2026Article
- Unveiling the Mechanism of Action of Palmitic Acid, a Human Topoisomerase 1B Inhibitor from the Antarctic SpongeInternational journal of molecular sciences · 2025Article
- Understanding Cancer's Defense against Topoisomerase-Active Drugs: A Comprehensive Review.Cancers · 2024Review
- Article
- Alkyne Activation in the Diversity Oriented Synthesis of spChemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic spongeJournal of enzyme inhibition and medicinal chemistry · 2022Article
- 2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Structural and biochemical basis for DNA and RNA catalysis by human Topoisomerase 3β.Nature communications · 2022Article
- TOP1-DNA Trapping by Exatecan and Combination Therapy with ATR Inhibitor.Molecular cancer therapeutics · 2022Article
- Synthesis of 11-aminoalkoxy substituted benzophenanthridine derivatives as tyrosyl-DNA phosphodiesterase 1 inhibitors and their anticancer activity.Bioorganic chemistry · 2022Article
- Topoisomerase I (TOP1) dynamics: conformational transition from open to closed states.Nature communications · 2022Article
- PARylation prevents the proteasomal degradation of topoisomerase I DNA-protein crosslinks and induces their deubiquitylation.Nature communications · 2021Article
- Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.Journal of medicinal chemistry · 2021Article
- The synthesis of furoquinolinedione and isoxazoloquinolinedione derivatives as selective Tyrosyl-DNA phosphodiesterase 2 (TDP2) inhibitors.Bioorganic chemistry · 2021Article
- Discovery of 4-alkoxy-2-aryl-6,7-dimethoxyquinolines as a new class of topoisomerase I inhibitors endowed with potent in vitro anticancer activity.European journal of medicinal chemistry · 2021Article
- Topoisomerase I-driven repair of UV-induced damage in NER-deficient cells.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Synthesis and biological evaluation of 5-aminoethyl benzophenanthridone derivatives as DNA topoisomerase IB inhibitors.European journal of medicinal chemistry · 2019Article
- Discovery, Synthesis, and Evaluation of Oxynitidine Derivatives as Dual Inhibitors of DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1), and Potential Antitumor Agents.Journal of medicinal chemistry · 2018Article
- Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors.Molecular cancer therapeutics · 2018Article
- Distribution bias and biochemical characterization of TOP1MT single nucleotide variants.Scientific reports · 2017Article
6 more citing papers are in PubMed but not listed here.
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
Abstract
The inhibition of DNA topoisomerase I (Top1) has proven to be a successful approach in the design of anticancer agents. However, despite the clinical successes of the camptothecin derivatives, a significant need for less toxic and more chemically stable Top1 inhibitors still persists. Here, we describe one of the most frequently used protocols to identify novel Top1 inhibitors. These methods use uniquely 3'-radiolabeled DNA substrates and denaturing polyacrylamide gel electrophoresis to provide evidence for the Top1-mediated DNA cleaving activity of potential Top1 inhibitors. These assays allow comparison of the effectiveness of different drugs in stabilizing the Top1-DNA intermediate or cleavage (cleavable) complex. A variation on these assays is also presented, which provides a suitable system for determining whether the inhibitor blocks the forward cleavage or religation reactions by measuring the reversibility of the drug-induced Top1-DNA cleavage complexes. This entire protocol can be completed in approximately 2 d.
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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.