Results 11 to 20 of about 60,395 (277)

Encapsulation and Enhanced Delivery of Topoisomerase I Inhibitors in Functionalized Carbon Nanotubes [PDF]

open access: yesACS Omega, 2018
Sieun Chae   +10 more
doaj   +2 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

Unraveling topoisomerase IA gate dynamics in presence of PPEF and its preclinical evaluation against multidrug-resistant pathogens

open access: yesCommunications Biology, 2023
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

Inhibitors of ABCB1 and ABCG2 overcame resistance to topoisomerase inhibitors in small cell lung cancer

open access: yesThoracic Cancer, 2022
Background Small cell lung cancer (SCLC) is a highly aggressive disease with a poor prognosis. Although most patients initially respond to topoisomerase inhibitors, resistance rapidly emerges.
Miwako Omori   +8 more
doaj   +1 more source

Effects of camptothecin derivatives and topoisomerase dual inhibitors on Trypanosoma cruzi growth and ultrastructure [PDF]

open access: yes, 2014
BACKGROUND: Trypanosoma cruzi is the etiological agent of Chagas’ disease that is an endemic disease in Latin America and affects about 8 million people.
Aline Araujo Zuma   +4 more
core   +1 more source

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