Results 21 to 30 of about 61,437 (248)
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
Effects of camptothecin derivatives and topoisomerase dual inhibitors on Trypanosoma cruzi growth and ultrastructure [PDF]
, 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
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
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
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
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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
Identification of early gene expression changes in primary cultured neurons treated with topoisomerase I poisons. [PDF]
, 2016 Topoisomerase 1 (TOP1) poisons like camptothecin (CPT) are currently used in cancer chemotherapy but these compounds can have damaging, off-target effects on neurons leading to cognitive, sensory and motor deficits.
Butchbach, Matthew E.R. +7 more
core +2 more sources
MRE11 facilitates the removal of human topoisomerase II complexes from genomic DNA [PDF]
, 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 ...
Austin, Caroline +10 more
core +3 more sources
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
Bioinformatic Analysis for the Validation of Novel Biomarkers for Cancer Diagnosis and Drug Sensitivity [PDF]
, 2015 Background: The genetic control of tumour progression presents the opportunity for bioinformatics and gene expression data to be used as a basis for tumour grading.
Lockwood, Laura Anne Rebecca
core +2 more sources