Results 1 to 10 of about 263 (116)
Topoisomerase I Inhibitors [PDF]
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).
Reginald B. Ewesuedo, Mark J. Ratain
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Prospects of Topoisomerase Inhibitors as Promising Anti-Cancer Agents
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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Inhibition of Zn(II) binding type IA topoisomerases by organomercury compounds and Hg(II). [PDF]
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
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
doaj +1 more source
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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Antimicrobial resistance is a global issue, and the investigation of alternative therapies that are not traditional antibiotics are warranted. Novel bacterial type II topoisomerase inhibitors (NBTIs) have recently emerged as a novel class of antibiotics ...
Adam O. Whelan +11 more
doaj +1 more source
Identification of anziaic acid, a lichen depside from Hypotrachyna sp., as a new topoisomerase poison inhibitor. [PDF]
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
doaj +1 more source
The Potential of Topoisomerase Inhibitor-Based Antibody–Drug Conjugates
DNA topoisomerases are essential enzymes that stabilize DNA supercoiling and resolve entanglements. Topoisomerase inhibitors have been widely used as anti-cancer drugs for the past 20 years.
Seungmin Han +6 more
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Topoisomerase I inhibitors and drug resistance [PDF]
DNA topoisomerase I is a nuclear enzyme which catalyzes the conversion of the DNA topology by introducing single-strand breaks into the DNA molecule. This enzyme represents a novel and distinct molecule target for cancer therapy by antitopoisomerase drugs belonging to the campthotecin series of antineoplastics.
R. E. Parchment, A. Pessina
openaire +3 more sources
Two potent inhibitors PPEF and BPVF of bacterial TopoIA enzymes function by impairing DNA binding and thus DNA cleavage and relaxation activities of bacterial topoisomerase I enzymes.
Vikas Maurya +9 more
doaj +1 more source

