Results 11 to 20 of about 32,790 (255)

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   +4 more sources

Topoisomerase I inhibitors: camptothecins and beyond [PDF]

open access: yesNature Reviews Cancer, 2006
Nuclear DNA topoisomerase I (TOP1) is an essential human enzyme. It is the only known target of the alkaloid camptothecin, from which the potent anticancer agents irinotecan and topotecan are derived. As camptothecins bind at the interface of the TOP1-DNA complex, they represent a paradigm for interfacial inhibitors that reversibly trap macromolecular ...
Pommier, Yves, Yves Pommier
openaire   +3 more sources

PROSPECTS FOR SEARCHING MULTITARGET TOPOISOMERASE INHIBITORS WITH ANTITUMOR PROPERTIES

open access: yesСибирский онкологический журнал, 2019
Purpose of research: to identify the prospects of search for new antitumor non-camptothecin inhibitors of topoisomerase I/II among the various chemical compounds based on the analysis of side effects.Material and Methods.
M. I. Treshchalin   +2 more
doaj   +3 more sources

Benzoxazines as new human topoisomerase I inhibitors and potential poisons. [PDF]

open access: yesDaru, 2020
Background The numbers of topoisomerase I targeted drugs on the market are very limited although they are used clinically for treatment of solid tumors.
Foto E   +7 more
europepmc   +2 more sources

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

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   +1 more source

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

MRE11 facilitates the removal of human topoisomerase II complexes from genomic DNA [PDF]

open access: yes, 2012
Topoisomerase II creates a double-strand break intermediate with topoisomerase covalently coupled to the DNA via a 5'-phosphotyrosyl bond. These intermediate complexes can become cytotoxic protein-DNA adducts and DSB repair at these lesions requires ...
Caroline A. Austin   +32 more
core   +1 more source

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