Results 21 to 30 of about 32,790 (255)
Molecules, 2023 The antitumor drug topotecan (TPT) is a potent inhibitor of topoisomerase I, triggering DNA breaks lethal for proliferating cancer cells. The mechanism is common to camptothecins SN38 (the active metabolite of irinotecan) and belotecan (BLT).
Christian Bailly, Gérard Vergoten
doaj +1 more source
Biochemistry and Biophysics Reports, 2019 Renal cell carcinoma (RCC) is relatively resistant to chemotherapy and radiotherapy. Clear cell RCC (ccRCC) accounts for the majority of RCC, which have mutations or epigenetic silencing of the von Hippel–Lindau (VHL) gene.
Hiromi Koma +3 more
doaj +1 more source
The impact of the C-terminal domain on the interaction of human DNA topoisomerase II α and β with DNA [PDF]
, 2011 <b>Background</b> Type II DNA topoisomerases are essential, ubiquitous enzymes that act to relieve topological problems arising in DNA from normal cellular activity.
Caroline A. Austin +7 more
core +1 more source
Cell Reports, 2016 During transcription and DNA replication, the DNA template is overwound ahead of RNA and DNA polymerases and relaxed by DNA topoisomerases. Inhibitors of topoisomerases are potent anti-cancer agents.
Cyril Ribeyre +6 more
doaj +1 more source
Topoisomerase I poisons-induced autophagy: Cytoprotective, Cytotoxic or Non-protective
Autophagy Reports, 2023 Topoisomerase I inhibitors represent a widely used class of antineoplastic agents that promote both single-stranded and double-stranded breaks in the DNA of tumor cells, leading to tumor cell death.
Ahmed M. Elshazly +3 more
doaj +1 more source
Type IA Topoisomerases as Targets for Infectious Disease Treatments
Microorganisms, 2021 Infectious diseases are one of the main causes of death all over the world, with antimicrobial resistance presenting a great challenge. New antibiotics need to be developed to provide therapeutic treatment options, requiring novel drug targets to be ...
Ahmed Seddek +2 more
doaj +1 more source
DNA topoisomerases participate in fragility of the oncogene RET [PDF]
, 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 ...
Yuh-Hwa Wang (457429) +25 more
core +1 more source
Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents
Molecules, 2019 To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized and their biological activities were evaluated as potential topoisomerase II inhibitors.
Ming-Jie Chu +8 more
doaj +1 more source
Structural Basis of Gate-DNA Breakage and Resealing by Type II Topoisomerases [PDF]
, 2010 ype II DNA topoisomerases are ubiquitous enzymes with essential functions in DNA replication, recombination and transcription. They change DNA topology by forming a transient covalent cleavage complex with a gate-DNA duplex that allows transport of a ...
Laponogov, I +27 more
core +1 more source
Benzothiazole derivatives as human DNA topoisomerase IIα inhibitors [PDF]
, 2013 Benzothiazole derivatives resembling the structure of DNA purine bases were tested to determine their topoisomerase inhibition activities. Based on DNA topoisomerase I and II relaxation assay results, all 12 derivatives acted as human topoisomerase IIα ...
Kaplan-Ozen, C. +6 more
core +2 more sources