Prospects of Topoisomerase Inhibitors as Promising Anti-Cancer Agents
Pharmaceuticals, 2023 Topoisomerases are very important enzymes that regulate DNA topology and are vital for biological actions like DNA replication, transcription, and repair. The emergence and spread of cancer has been intimately associated with topoisomerase dysregulation.
Syed Shafi +2 more
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Chromatinization modulates topoisomerase II processivity [PDF]
Nature Communications, 2023 Type IIA topoisomerases are essential DNA processing enzymes that must robustly and reliably relax DNA torsional stress. While cellular processes constantly create varying torsional stress, how this variation impacts type IIA topoisomerase function ...
Jaeyoon Lee +10 more
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Structural and functional insights into the T-even type bacteriophage topoisomerase II [PDF]
Nature CommunicationsT-even type bacteriophages are virulent phages commonly used as model organisms, playing a crucial role in understanding various biological processes. One such process involves the regulation of DNA topology during phage replication upon host infection ...
Yuhui Xin +6 more
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In Silico Evaluation of Some Computer-Designed Fluoroquinolone–Glutamic Acid Hybrids as Potential Topoisomerase II Inhibitors with Anti-Cancer Effect [PDF]
PharmaceuticalsBackground/Objectives: Fluoroquinolones (FQs) are topoisomerase II inhibitors with antibacterial activity, repositioned recently as anti-cancer agents. Glutamic acid (GLA) is an amino acid that affects human metabolism.
Octavia-Laura Oancea +4 more
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Synthesis, in vitro and in silico studies of a novel chrysin-ferrocene Schiff base with potent anticancer activity via G1 arrest, caspase-dependent apoptosis and inhibition of topoisomerase II [PDF]
Journal of Enzyme Inhibition and Medicinal ChemistryA novel chrysin-ferrocene Schiff base (CFSB) was synthesised as a potential anticancer agent. CFSB demonstrated high cytotoxicity against cancer cells with HepG2 (liver) being the most susceptible (IC50 = 3.11 µM).
Mohammed Khaled Bin Break +5 more
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Potential COX2 mediated Therapeutic effect of Ciprofloxacin [PDF]
Minia Journal of Medical Research, 2021 Fluoroquinolones (FQs) are broad-spectrum, synthetic antibiotics that inhibit bacterial DNA synthesis. FQs directly block DNA synthesis in the bacterial cell via inhibition the activity of two tetrameric, ATPdependent, homologous type II topoisomerase ...
Marwa Eisa +2 more
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Marine-Derived Compounds Targeting Topoisomerase II in Cancer Cells: A Review
Marine Drugs, 2022 Cancer affects more than 19 million people and is the second leading cause of death in the world. One of the principal strategies used in cancer therapy is the inhibition of topoisomerase II, involved in the survival of cells.
Giulia Greco +5 more
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Voreloxin is an anticancer quinolone derivative that intercalates DNA and poisons topoisomerase II. [PDF]
PLoS ONE, 2010 Topoisomerase II is critical for DNA replication, transcription and chromosome segregation and is a well validated target of anti-neoplastic drugs including the anthracyclines and epipodophyllotoxins.
Rachael E Hawtin +9 more
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Inhibition of Zn(II) binding type IA topoisomerases by organomercury compounds and Hg(II). [PDF]
PLoS ONE, 2015 Type IA topoisomerase activities are essential for resolving DNA topological barriers via an enzyme-mediated transient single strand DNA break. Accumulation of topoisomerase DNA cleavage product can lead to cell death or genomic rearrangement.
Bokun Cheng +4 more
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Identification of Suppressors of top-2 Embryonic Lethality in Caenorhabditis elegans
G3: Genes, Genomes, Genetics, 2020 Topoisomerase II is an enzyme with important roles in chromosome biology. This enzyme relieves supercoiling and DNA and RNA entanglements generated during mitosis. Recent studies have demonstrated that Topoisomerase II is also involved in the segregation
Nirajan Bhandari +8 more
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