ReviewACS chemical biology2013
Drugging topoisomerases: lessons and challenges.
Review in ACS chemical biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 394 papers.
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Who cites it
394 citing papers in PubMed, 818 citations in OpenAlex.
- Cyano-modulated Zn(II)-Schiff base complexes for lysosome-targeted fluorescence imaging and pH-responsive camptothecin delivery.International journal of pharmaceutics: X · 2026Article
- Topotecan Synergizes with SP141 in the Management of Uveal Melanoma.bioRxiv : the preprint server for biology · 2026Article
- A multispecies toolkit ofProceedings of the National Academy of Sciences of the United States of America · 2026Article
- Molecular Determinants of Response and Rational Drug Combinations for Antibody-Drug Conjugates (ADCs) with Topoisomerase I (TOP1) Inhibitor Payloads.Journal of molecular biology · 2026Review
- Characterization of beddomeilactone amide as bacterial DNA gyrase inhibitor: in vitro evaluation and computational insights.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- Phase I Study of Telisotuzumab Adizutecan (Temab-A, ABBV-400), a Novel c-Met Antibody-Drug Conjugate, in Patients With Late-Line Colorectal Cancer and Advanced Solid Tumors.Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2026Article
- Benzofuran-Annulated Naphthalimides Trigger Replication Stress, DNA Damage, and p53-Dependent Cell Cycle Arrest.Pharmaceutics · 2026Article
- Natural Products as Promising Pharmacological Agents Against Cancer: A Holistic Overview of Their Anti-Cancer Mechanisms of Action of the Last Five Years.Pharmaceuticals (Basel, Switzerland) · 2026Review
- A high-throughput fluorescent DNA cleavage assay for discovering bacterial DNA gyrase poisons.Nucleic acids research · 2026Article
- Antibody-drug conjugates in colorectal cancer: molecular design, preclinical advances, and translational challenges.Cancer chemotherapy and pharmacology · 2026Review
- Complex mechanisms of topoisomerase II poisons revealed by whole-genome analysis.Communications biology · 2026Article
- Design and Multi-Level Biological Evaluation of Naphthyridine-Based Derivatives as Topoisomerase I/II-Targeted Anticancer Agents with Anti-Fowlpox Virus Activity Supported by In Silico Analysis.International journal of molecular sciences · 2026Article
- Topoisomerase inhibitors in cervical cancer: mechanistic insights and therapeutic strategies.Molecular medicine (Cambridge, Mass.) · 2026Review
- Search for Specific Inhibitors Targeting Type IA Topoisomerases.Journal of molecular biology · 2026Review
- Targeted CRISPR knockout screening identifies known and novel chemogenomic interactions between DNA damaging agents and DNA repair genes.NAR cancer · 2026Article
- MYC modulates TOP2A diffusion to promote substrate detection and activity.Nature communications · 2026Article
- The Roles of Topoisomerases in Transcriptional Regulation.International journal of molecular sciences · 2026Review
- Gyrase and Topoisomerase IV as Antibacterial Targets for Gepotidacin and Zoliflodacin: Teaching Old Enzymes New Tricks.International journal of molecular sciences · 2026Review
- Repurposing fluoroquinolones as cancer chemosensitizers: a way to overcome cancer therapeutic bottleneck.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- Synthesis of functionalized, 13-alkyl-substituted coralyne derivatives and investigation of their interactions with duplex and abasic site-containing DNA.Beilstein journal of organic chemistry · 2026Article
334 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
1 author at 1 institution in 1 country.
Funding
Abstract
Topoisomerases are ubiquitous enzymes that control DNA supercoiling and entanglements. They are essential during transcription and replication, and topoisomerase inhibitors are among the most effective and most commonly used anticancer and antibacterial drugs. This review consists of two parts. In the first part ("Lessons"), it gives background information on the catalytic mechanisms of the different enzyme families (6 different genes in humans and 4 in most bacteria), describes the "interfacial inhibition" by which topoisomerase-targeted drugs act as topoisomerase poisons, and describes clinically relevant topoisomerase inhibitors. It generalizes the interfacial inhibition principle, which was discovered from the mechanism of action of topoisomerase inhibitors, and discusses how topoisomerase inhibitors kill cells by trapping topoisomerases on DNA rather than by classical enzymatic inhibition. Trapping protein-DNA complexes extends to a novel mechanism of action of PARP inhibitors and could be applied to the targeting of transcription factors. The second part of the review focuses on the challenges for discovery and precise use of topoisomerase inhibitors, including targeting topoisomerase inhibitors using chemical coupling and encapsulation for selective tumor delivery, use of pharmacodynamic biomarkers to follow drug activity, complexity of the response determinants for anticancer activity and patient selection, prospects of rational combinations with DNA repair inhibitors targeting tyrosyl-DNA-phosphodiesterases 1 and 2 (TDP1 and TDP2) and PARP, and the unmet need to develop inhibitors for type IA enzymes.
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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.