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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Topoisomerase I Inhibitors [PDF]
Oncologist, 1997 The helical structure of DNA was proposed in 1953 by Watson and Crick (1). Twelve years later, Vinograd and collaborators (2–4) found that the helix axis can also be coiled in circular DNA. This structure was called supercoiling. This finding was extended to linear DNA by Pettijohn and others (5–8).
Mark J Ratain, Ratain Mark J
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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
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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
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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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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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Encapsulation and Enhanced Delivery of Topoisomerase I Inhibitors in Functionalized Carbon Nanotubes [PDF]
ACS Omega, 2018 Sieun Chae +10 more
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Inhibition of Zn(II) binding type IA topoisomerases by organomercury compounds and Hg(II). [PDF]
PLoS ONE, 2015 Type IA topoisomerase activities are essential for resolving DNA topological barriers via an enzyme-mediated transient single strand DNA break. Accumulation of topoisomerase DNA cleavage product can lead to cell death or genomic rearrangement.
Bokun Cheng +4 more
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Topoisomerase II as a Novel Antiviral Target against Panarenaviral Diseases
Viruses, 2022 Although many arenaviruses cause severe diseases with high fatality rates each year, treatment options are limited to off-label use of ribavirin, and a Food and Drug Administration (FDA)-approved vaccine is not available.
Tosin Oladipo Afowowe +4 more
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Nature Communications, 2021 CX-5461 recently progressed through phase I clinical trial as a first-inhuman inhibitor of RNA-POL I. Here, the authors demonstrate that CX-5461 synergizes with topoisomerase I inhibitors to inhibit neuroblastoma cells and that its primary target in this
Min Pan +29 more
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