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Search results for: TOPOISOMERASE II
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Targeting DNA Topoisomerase II in Antifungal Chemotherapy.
PublicationTopoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand...
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Catalytic topoisomerase II inhibitors in cancer therapy.
PublicationDNA topoizomeraza II jest jednym z głównych celów molekularnych dla leków stosowanych w terapii przeciwnowotworowej. Wszystkie inhibitory tego enzymu są zdolne do zakłócania w jeden z etapów cyklu katalitycznego topoizomerazy II. Związki, które stabilizują kowalencyjny kompleks DNa i topoizomerazy II (znany jako kompleks rozszczepialny) są nazywane truciznami topoizomerazy, inne związki, które hamują aktywność enzymu na innych...
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Targeting yeast topoisomerase II by imidazo and triazoloacridinone derivatives resulting in their antifungal activity
PublicationFungal pathogens are considered as serious factors for deadly diseases and are a case of medical concern. Invasive fungal infections also complicate the clinical course of COVID-19, leading to a significant increase in mortality. Furthermore, fungal strains' multidrug resistance has increased the demand for antifungals with a different mechanism of action. The present study aimed to identify antifungal compounds targeting yeast...
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Perturbation of cellular functions by topoisomerase II inhibitors: all roads lead to cell death?
PublicationPraca przeglądowa opisuje jakie funkcje mogą ulec zahamowaniu/zmianie pod wpływem działania inhibitorów topoizomerazy typu II w komórkach nowotworowych. W szczególności dyskutujemy jakie zmiany w szlakach sygnalizacji wewnątrzkomórkowej mogą prowadzić do zahamowania wzrostu oraz indukcji różnych rodzajów śmierci komórkowej i czy rodzaj śmierci komórkowej może decydować o skuteczności leków przeciwnowotoworowych, które hamują aktywność...
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Isoform-specific inhibition of DNA topoisomerase II as the mechanism of action of novel anticancer agent C-1305
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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublicationIn the last few years,increasing importance is attached to problems caused by fungal pathogens. Current methods of preventing fungal infections remain unsatisfactory. There are several antifungal compounds whichare highly effective in some cases, however, they have limitations in usage: Nephrotoxicity and other adverse effects. In addition, the frequent use of available fungistatic drugs promotes drug resistance....
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublicationHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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A new 1-nitro-9-aminoacridine derivative targeting yeast topoisomerase II able to overcome fluconazole-resistance
PublicationFungal resistance remains a significant threat and a leading cause of death worldwide. Thus, overcoming microbial infections have again become a serious clinical problem. Although acridine derivatives are widely analyzed as anticancer agents, only a few reports have demonstrated their antifungal activity. In an effort to develop biologically active antifungals, twelve novel C-857 (9-(2′ -hydroxyethylamino)-1-nitroacridine) and...
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Effect of antitumor compounds on the yeast topoisomerase II relaxation activity
Open Research DataThe datasets contain results of antitumor compounds* (known inhibitors of human topoisomerase alpha II) inhibitory activity against yeast topoisomerase II. DNA topoisomerases (Topo) are enzymes that catalyze changes in the spatial structure of DNA and play an important role in replication, transcription and recombination. Beyond their normal functions,...
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Do not die, become senescent: a new type of cellular resistance induced by topoisomerase II inhibitors in tumor cells with functional p53
PublicationJednym z efektów wywoływanych przez związki przeciwnowotworowe w komórkach nowotworowych jest trwałe zahamowanie wzrostu, związane z pojawieniem się markerów procesu starzenia komórkowego. Proponuje się, że może to być nowy sposób na zahamowanie postępu choroby nowotworowej. W naszych badaniach wykazujemy, że zahamowanie wzrostu indukowane przez związki z grupy inhibitorów topoizomerazy II w komórkach raka płuc A549 jest związane...