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Genotoxicity of several clinically used topoisomerase II inhibitors
Toxicology Letters, 2000DNA topoisomerase II is an essential nuclear enzyme that modulates DNA topology during multiple cellular processes such as DNA replication and chromosome segregation. Several important clinical antitumor drugs and antibiotics act through inhibition of topoisomerase II.
G, Boos, H, Stopper
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Tannins as Potent Inhibitors of DNA Topoisomerase II In Vitro
Journal of Pharmaceutical Sciences, 1993Fifty-two out of 60 tannins, including gallo-, ellagi-, condensed, and complex tannins, are inhibitors of human DNA topoisomerase II in vitro. Thirty-six compounds that completely inhibited enzyme activity at a concentration of 500 nM or less, as assessed by ATP-dependent unknotting of P4 phage DNA, were at least 100-fold more potent than the ...
Y, Kashiwada +7 more
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Topoisomerase II Inhibitors: Chemical Biology
2011DNA topoisomerase II (Top2) is the target of a chemically diverse set of compounds with substantial antitumor activity. Agents such as doxorubicin and etoposide are FDA approved for the treatment of both leukemias and solid tumors. Most clinically active drugs targeting Top2 lead to elevated levels of covalent Top2-cleaved DNA complexes and exert their
Anna Rogojina +4 more
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Topoisomerase II Inhibitors in Cancer Treatment
International Journal of Pharmaceutical Sciences and Nanotechnology, 2011Topoisomerase II constitutes a family of nuclear enzymes essential to all living cells. These enzymes are capable of transferring one DNA double helix through a transient break in another DNA double helix. Type II topoisomerases play important roles in DNA metabolic processes, in which they are involved in DNA replication, transcription, chromosome ...
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Pyrroloquinolinone-based dual topoisomerase I/II inhibitor
European Journal of Medicinal Chemistry, 2014A new series of pyrroloquinolinones bearing different alkylamino side chains were synthesized and evaluated as cytotoxic compounds against three different human tumor cell lines (HeLa, HL-60 and A431). Some compounds showed interesting antiproliferative activity, in particular against A431 cells.
DALLA VIA, LISA +4 more
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Induction of diplochromosomes in mammalian cells by inhibitors of topoisomerase II
Chromosoma, 1998Diplochromosomes, consisting of four chromatids lying side-by-side, instead of the normal two, are produced when cells go through two rounds of DNA replication without separation of chromatids. They are thus an indication of the failure of the normal chromosome separation mechanism.
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Genotoxicity of topoisomerase II inhibitors: An anti-infective perspective
Toxicology, 2008At present, an inevitable consequence of a chemical's inhibitory activity on key regulators of DNA topology in bacteria, the type II topoisomerases, is a less pronounced effect on their eukaryotic counterparts. In the context of anti-infectives drug development, this may pose a risk to patient safety as inhibition of eukaryotic type II topoisomerases ...
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[Molecular determinants of response to topoisomerase I inhibitors].
Bulletin du cancer, 2011Nuclear topoisomerase I (Top1) is involved in the relaxation of DNA supercoiling and plays a pivotal role in the coordination of essential DNA processes such as transcription, replication, DNA recombination and DNA damage signalling. For all these reasons, Top1 has been an attractive target for the development of anticancer drugs, which poison Top1 by ...
Pourquier, Philippe, Lansiaux, Amélie
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A patent review of topoisomerase I inhibitors (2016–present)
Expert Opinion on Therapeutic Patents, 2021Asier Selas +2 more
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