Results 1 to 10 of about 61,437 (248)

Identification of anziaic acid, a lichen depside from Hypotrachyna sp., as a new topoisomerase poison inhibitor. [PDF]

open access: yesPLoS 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
doaj   +7 more sources

Topoisomerase I Inhibitors [PDF]

open access: yesThe 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
  +5 more sources

Prospects of Topoisomerase Inhibitors as Promising Anti-Cancer Agents

open access: yesPharmaceuticals, 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
doaj   +1 more source

DNA topoisomerases participate in fragility of the oncogene RET [PDF]

open access: yes, 2013
Fragile site breakage was previously shown to result in rearrangement of the RET oncogene, resembling the rearrangements found in thyroid cancer. Common fragile sites are specific regions of the genome with a high susceptibility to DNA breakage under ...
A Ganguly   +86 more
core   +9 more sources

Inhibition of Zn(II) binding type IA topoisomerases by organomercury compounds and Hg(II). [PDF]

open access: yesPLoS 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
doaj   +1 more source

Topoisomerase II as a Novel Antiviral Target against Panarenaviral Diseases

open access: yesViruses, 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
doaj   +1 more source

The chemotherapeutic CX-5461 primarily targets TOP2B and exhibits selective activity in high-risk neuroblastoma

open access: yesNature 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
doaj   +1 more source

In Vitro Activity of Novel Topoisomerase Inhibitors against Francisella tularensis and Burkholderia pseudomallei

open access: yesAntibiotics, 2023
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

The Potential of Topoisomerase Inhibitor-Based Antibody–Drug Conjugates

open access: yesPharmaceutics, 2022
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
doaj   +1 more source

Topoisomerase I inhibitors and drug resistance [PDF]

open access: yesCytotechnology, 1998
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

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