Topoisomerases, targets of inhibitors used in chemotherapy, induce DNA breaks accumulation leading to cancer cell death. A newly synthesized copper(II) indenoisoquinoline complex WN197 exhibits a cytotoxic effect below 0.5 µM, on MDA-MB-231, HeLa, and HT-
Caroline Molinaro +6 more
doaj +1 more source
DNA single-strand break repair and spinocerebellar ataxia with axonal neuropathy-1 [PDF]
DNA single-strand breaks (SSBs) are the commonest DNA lesions arising spontaneously in cells, and if not repaired may block transcription or may be converted into potentially lethal/clastogenic DNA double-strand breaks (DSBs).
Arnaudeau +82 more
core +1 more source
Evaluation of melanin-targeted radiotherapy in combination with radiosensitizing drugs for the treatment of melanoma [PDF]
The incidence of malignant melanoma is rising faster than that of any other cancer in the United States. An [131I]-labeled benzamide - [131I]MIP-1145 - selectively targets melanin, reduces melanoma tumor burden and increases survival in preclinical ...
Babich, John +5 more
core +1 more source
TDP1 deficiency sensitizes human cells to base damage via distinct topoisomerase I and PARP mechanisms with potential applications for cancer therapy [PDF]
Base damage and topoisomerase I (Top1)-linked DNA breaks are abundant forms of endogenous DNA breakage, contributing to hereditary ataxia and underlying the cytotoxicity of a wide range of anti-cancer agents.
Alagoz +50 more
core +1 more source
Relationship between protein biomarkers of chemotherapy response and microsatellite status, tumor mutational burden and PD-L1 expression in cancer patients. [PDF]
Chemotherapy and checkpoint inhibitor immunotherapies are increasingly used in combinations. We determined associations between the presence of anti-PD-1/PD-L1 therapeutic biomarkers and protein markers of potential chemotherapy response.
Arguello, David +5 more
core +2 more sources
PROSPECTS FOR SEARCHING MULTITARGET TOPOISOMERASE INHIBITORS WITH ANTITUMOR PROPERTIES
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 +1 more source
Enhancement of radiosensitivity by the novel anticancer quinolone derivative vosaroxin in preclinical glioblastoma models [PDF]
Purpose: Glioblastoma multiforme (GBM) is the most aggressive brain tumor. The activity of vosaroxin, a first-in-class anticancer quinolone derivative that intercalates DNA and inhibits topoisomerase II, was investigated in GBM preclinical models as a ...
Colapietro, Alessandro +11 more
core +1 more source
The potential role and application of PARP inhibitors in cancer treatment [PDF]
Background: Since many anti-cancer agents act by inflicting DNA damage on tumour cells, there is increasing interest in the use of inhibitors of DNA repair to increase the cytotoxicity of these agents.
Chalmers, Anthony J
core +2 more sources
Topoisomerase I inhibitors: camptothecins and beyond [PDF]
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 ...
openaire +2 more sources
Novel DNA topoisomerase IIα inhibitors from combined ligand- and structure-based virtual screening.
DNA topoisomerases are enzymes responsible for the relaxation of DNA torsional strain, as well as for the untangling of DNA duplexes after replication, and are important cancer drug targets.
Malgorzata N Drwal +5 more
doaj +1 more source

