Topoisomerase Inhibitors
Topoisomerase Inhibitors and Types of Them
... Topoisomerase inhibitors are agents designed to interfere with the action of topoisomerase enzymes (topoisomerase I and II), which are enzymes that control the changes in DNA structure by ...
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SMAC mimetic Debio 1143 synergizes with taxanes, topoisomerase inhibitors and bromodomain inhibitors to impede growth of lung adenocarcinoma cells
... metabolic and epigenetic modulators, and conventional chemotherapeutics. An Area Under the Curve (AUC) metric quantified the impact of combinations that inhibited growth more effectively and/or more potently than either ...
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Topoisomerase inhibitors promote cancer cell motility via ROS-mediated activation of JAK2-STAT1-CXCL1 pathway
... ADM: Adriamycin; CM: Conditioned medium; CPT-11: Irinotecan; CXCL1: Chemokine (C-X-C motif) ligand 1; DCFH-DA: 2,7-Dichlorodi -hydrofluorescein diacetate; Flu: Fludarabine; GSH: Reduced glutathione; JAK2: Janus kinase 2; ...
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Discovery and structure-activity relationships of a novel isothiazolone class of bacterial type II topoisomerase inhibitors
... In summary, this paper describes the SAR and in vitro evaluation of a novel isothiazolone-based series of bacterial topoisomerase II inhibitors. Broad-spectrum activity was observed for many compounds and ...
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Novel bacterial topoisomerase inhibitors with potent broad-spectrum activity against drug-resistant bacteria
... described previously (14). Reactions were stopped using 30 μL chloroform/iso-amyl alcohol (26:1) and 20 μL Stop Dye (40 % sucrose, 100 mM Tris.HCl [pH 7.5], 1 mM EDTA, 0.5 μg/mL bromophenol blue). Topoisomers were ...
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Quantitative Structure Activity Relationship Study of Naphthoquinone Analogs as Possible DNA Topoisomerase Inhibitors
... Quantitative Structure Activity Relationship (QSAR) is among the most widely used computational technology for analogue-based drug design. A molecular modeling approach of Naphthoquinone (NQ) analogue as anticancer ...
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Pim kinase inhibition sensitizes FLT3-ITD acute myeloid leukemia cells to topoisomerase 2 inhibitors through increased DNA damage and oxidative stress
... kinase inhibitors [36]. Four Pim kinase inhibitors have entered clinical trials to ...kinase inhibitors, are currently in clinical ...with topoisomerase inhibitors ...
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IDENTIFICATION OF POTENT VIRTUAL LEADS AS TOPOISOMERASE II INHIBITORS USING PHARMACOPHORE MODELLING, MOLECULAR DOCKING AND ADME STUDIES
... novel topoisomerase inhibitors with a new scaffold distinct from existing drugs with improved ...possess topoisomerase I and II inhibitory activity along with strong cytotoxicity against several ...
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Molluscum Contagiosum Virus Topoisomerase: Purification, Activities, and Response to Inhibitors
... Thus, inhibitors of the MCV topoisomerase might be useful as antiviral ...MCV topoisomerase, overexpressed and purified the protein, and begun to charac- terize its activities in ...MCV ...
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The dual topoisomerase inhibitor A35 preferentially and specially targets topoisomerase 2 aby enhancing pre-strand and post-strand cleavage and inhibiting DNA religation
... in topoisomerase (top) levels is the primary factor responsible for resistance, but in cells there is compensatory effect between the levels of top1 and ...a topoisomerase poison and had a district ...
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Characterization and structure-activity relationships of indenoisoquinoline-derived topoisomerase I inhibitors in unsilencing the dormant Ube3a gene associated with Angelman syndrome
... indotecan produce more stable cleavage complexes than camptothecins such as topotecan [45], which, based on the mechanism of Ube3a unsilencing [26], should enhance Ube3a unsilencing as we observed. Moreover, after drug ...
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Repair of Topoisomerase-Mediated DNA Damage in Bacteriophage T4
... II topoisomerase inhibitors are used to treat both tumors and bacterial ...These inhibitors stabilize covalent DNA-topoisomerase cleavage complexes that ultimately cause lethal DNA ...
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Acetylation of E2 by P300 Mediates Topoisomerase Entry at the Papillomavirus Replicon
... DNA, topoisomerase 1 (Topo1) is thought to be required for progression of the replication ...regulating topoisomerase recruitment to the replication ...
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TOPOISOMERASE INVOLVEMENT IN MULTIPLICITY REACTIVATION OF PHAGE T4
... We chose as our standard unit dose for all monocomplex and multicomplex inactivation experiments the time period of treatment which resulted in an average of 1.0 let[r] ...
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Human cytomegalovirus induces expression of cellular topoisomerase II.
... By measuring the abundance of topoisomerase II RNA and protein in infected cells at various times after infection, we hoped to determine whether HCMV might fulfill its need for topoisome[r] ...
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Topoisomerase I-mediated integration of hepadnavirus DNA in vitro.
... Lanes: 1 and 10, Topo I treatment of WHV plus C3 DNA mixtures followed by PCR using C3 primer e and WHV minus-strand primer b; 2 and 11, control reactions for lanes 1 and 10 in which Top[r] ...
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Restoration of Topoisomerase 2 Function by Complementation of Defective Monomers in Drosophila
... the Topoisomerase/Primase (TOPRIM) domain contains a triad of acidic amino acids that are required for the DNA cleavage reaction and the Winged helix domain (WHD) contains the active-site tyrosine, which forms the ...
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Topoisomerase I and II cleavage of adenovirus DNA in vivo: both topoisomerase activities appear to be required for adenovirus DNA replication.
... In this study, we have used camptothecin and VM26 to examine the sites of cleavage by the topoisomerases on the adenovirus type 5 Ad5 chromosome, the relationship between the sites and t[r] ...
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DNA Repair Functions That Control Sensitivity to Topoisomerase-Targeting Drugs
... Alternately, topoisomerase-targeting drugs may be a very efficient generator of double-strand breaks, leading to a requirement for high levels of rad22A protein for cell ...of topoisomerase I trapped by ...
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DNA Topoisomerase 1 Facilitates the Transcription and Replication of the Ebola Virus Genome
... Ebola virus (EBOV) protein L (EBOL) acts as a viral RNA-dependent RNA polymerase. To better understand the mechanisms underlying the transcription and replication of the EBOV genome, we sought to identify cellular ...
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