Identification of anziaic acid, a lichen depside from Hypotrachyna sp., as a new topoisomerase poison inhibitor. [PDF]
PLoS ONE, 2013 Topoisomerase inhibitors are effective for antibacterial and anticancer therapy because they can lead to the accumulation of the intermediate DNA cleavage complex formed by the topoisomerase enzymes, which trigger cell death.
Bokun Cheng +6 more
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Enhanced Stability and Bioactivity of Natural Anticancer Topoisomerase I Inhibitors through Cyclodextrin Complexation [PDF]
Pharmaceutics, 2021 The use of cyclodextrins as drug nano-carrier systems for drug delivery is gaining importance in the pharmaceutical industry due to the interesting pharmacokinetic properties of the resulting inclusion complexes.
Víctor González-Ruiz +9 more
doaj +2 more sources
Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors. [PDF]
Mol Cancer Ther, 2018 Abstract Contrary to other anticancer targets, topoisomerase I (TOP1) is targeted by only one chemical class of FDA-approved drugs: topotecan and irinotecan, the derivatives of the plant alkaloid, camptothecin. The indenoisoquinolines LMP400, LMP744, and LMP776 are novel noncamptothecin TOP1 inhibitors in clinical trial, which ...
Marzi L +10 more
europepmc +4 more sources
Topoisomerase inhibitors in cervical cancer: mechanistic insights and therapeutic strategies [PDF]
Molecular MedicineCervical cancer represents a critical global health burden, particularly among women in countries with limited healthcare infrastructure, where it accounts for a substantial proportion of cancer-related morbidity and mortality.
Yashaswini Reddy +6 more
doaj +2 more sources
Discovery of potent bisindole-based pyrazolopyridine derivatives as topoisomerase inhibitors: DNA damage induction and synergistic antileukemic activity [PDF]
Frontiers in PharmacologyIntroductionThe development of novel anticancer agents targeting DNA replication and repair mechanisms remains a priority in leukemia therapy. In this study, newly synthesized derivatives incorporating bis-indole and pyrazolo[3,4-b]pyridine scaffolds ...
Wagdy M. Eldehna +12 more
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Dual-acting histone deacetylase-topoisomerase I inhibitors. [PDF]
Bioorg Med Chem Lett, 2013 Current chemotherapy regimens are comprised mostly of single-target drugs which are often plagued by toxic side effects and resistance development. A pharmacological strategy for circumventing these drawbacks could involve designing multivalent ligands that can modulate multiple targets while avoiding the toxicity of a single-targeted agent.
Guerrant W +5 more
europepmc +4 more sources
Small DNA circles as bacterial topoisomerase I inhibitors. [PDF]
RSC Adv, 2019 It is demonstrated that small DNA circles showed high inhibitory effect on the activity of bacterial topoisomerase I and the single-stranded regions associated with bending deformation are believed to be the crucial factor for trapping the enzymes.
Li D, Wang Q, Zhou B, Zhuge Q, Lv B.
europepmc +4 more sources
Discovery of DNA Topoisomerase I Inhibitors with Low-Cytotoxicity Based on Virtual Screening from Natural Products [PDF]
Marine Drugs, 2017 Currently, DNA topoisomerase I (Topo I) inhibitors constitute a family of antitumor agents with demonstrated clinical effects on human malignancies. However, the clinical uses of these agents have been greatly limited due to their severe toxic effects ...
Lan-Ting Xin +10 more
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Topoisomerase I Inhibitors [PDF]
The Oncologist, 1997 Abstract Topoisomerase I inhibitors are a new class of anticancer agents with a mechanism of action aimed at interrupting DNA replication in cancer cells, the result of which is cell death. Most if not all Topoisomerase I inhibitors are derivatives of the plant extract camptothecin.
Reginald B. Ewesuedo, Mark J. Ratain
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Prospects of Topoisomerase Inhibitors as Promising Anti-Cancer Agents
Pharmaceuticals, 2023 Topoisomerases are very important enzymes that regulate DNA topology and are vital for biological actions like DNA replication, transcription, and repair. The emergence and spread of cancer has been intimately associated with topoisomerase dysregulation.
Prasanna Anjaneyulu Yakkala +3 more
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