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InhibitorsChemotherapyTeniposideAnticancerInhibitor of topoisomeraseInhibitsVePesidCamptothecinInhibitionPathwaysReplicationCatalytic activityDrugsInducesCytotoxicResistanceCleavageComplexesHypoxicCyclophosphamideTOP1ApoptosisNeuroblastomaEnzyme activityDosesChromosomeTumorMechanismsLeukemiaTargetsInteractionsCellAgentsPotentExposureGeneStrandTopologyTreatmentHumanExpressionActivityCellsCancerDamageEffect

Inhibitors19

• Because MMR is assumed to modulate cytotoxicity to various chemotherapeutic agents that act upon DNA, our objectives have been to define its possible involvement in the cytotoxicity of topoisomerase inhibitors. (aacrjournals.org)
• Our results also indicate that neither p53 status, nor cell cycle alterations correlate with the sensitivity of colorectal cancer cells to topoisomerase inhibitors. (aacrjournals.org)
• Furthermore, they imply that coadministration of agents that inhibit NF-κB may enhance the efficacy of topoisomerase II inhibitors in clinical cancer chemotherapy. (aspetjournals.org)
• The results found here warrant further studies of combined treatment of neuroblastoma cells with etoposide with HDAC inhibitors and may help in the design of new protocols geared to the treatment of high risk neuroblastomas. (nel.edu)
• Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive Staphylococcus aureus. (osu.edu)
• Novel bacterial topoisomerase inhibitors derived from isomannide. (osu.edu)
• He revealed the interfacial inhibition paradigm based on molecular mechanisms of topoisomerase inhibitors, and has championed its broad relevance for molecular pharmacology and drug discovery. (cancer.gov)
• He discovered the indenoisoquinolines as novel Top1 inhibitors, which are in clinical development, and the mitochondrial topoisomerase gene, TOP1mt. (cancer.gov)
• To understand the determinants of response to topoisomerase inhibitors, he is studying the repair pathway centered on tyrosyl-DNA-phosphodiesterases (TDP1 and TDP2) and poly(ADP-ribose)polymerases (PARP). (cancer.gov)
• Dr. Pommier conceptualized the "interfacial inhibitors" mechanism based on his finding that DNA topoisomerase inhibitors act by trapping topoisomerase-DNA complexes (Capranico et al. (cancer.gov)
• 3] This is believed to constitute an important mechanism of resistance to topoisomerase I inhibitors in malignant cells. (cancernetwork.com)
• Certain alkylating agents like melphalan, platinum compounds, and topoisomerase II inhibitors like etoposide reported to confer a five fold increase risks for therapy related myelodysplasia or AML. (standardofcare.com)
• Several chemotherapy agents that include alkylating agents, topoisomerase inhibitors, and tax anew are associated with the development of acute myelogenous leukemia and myelodysplastic syndrome. (standardofcare.com)
• Alkylating agents and topoisomerase II inhibitors induce therapy related leukemia. (standardofcare.com)
• Chromosomal changes in AML related to topoisomerase II inhibitors are rearrangement abnormalities without gain or loss of chromosomal material. (standardofcare.com)
• DNA topoisomerase I inhibitors: camptothecin, irinotecan and topotecan 14. (present5.com)
• Another type of medicine, called topoisomerase inhibitors, also attacks enzymes that help cancer cells divide and grow. (webmd.com)
• Secondary MDS after prior treatment with topoisomerase II inhibitors like anthracyclines and etoposide occurs 1-3 years after exposure to these agents. (medscape.com)
• Occupational exposure limits with proteins such as topoisomerase inhibitors, and mitotic and meiotic spindle poisons. (cdc.gov)

Chemotherapy5

• In contrast, the topoisomerase class of chemotherapy drugs that include adriamycin and etoposide cause acute myeloid leukemia quicker and with different genetic alterations. (oncolink.org)
• Second-line chemotherapy for recurrent osteosarcoma includes ifosfamide or cyclophosphamide, possibly together with etoposide and/or carboplatin, and other active drugs including gemcitabine and docetaxel, sorafenib, or regorafenib, as well as samarium sm 153 lexidronam. (medscape.com)
• First-line therapy in ES-SCLC currently consists of chemotherapy, combining a platinum drug with either etoposide or irinotecan as a possible alternative. (ersjournals.com)
• The first-line treatment of ES-SCLC currently consists of chemotherapy with a platinum derivative and etoposide, a combination that was first reported to be effective in the treatment of SCLC in 1985 8 , 9 . (ersjournals.com)
• Combination chemotherapy with cisplatin and etoposide (cisplatin-etoposide [PE]) has long been the mainstay of treatment for small cell lung cancer (SCLC). (the-medical-dictionary.com)

Teniposide3

• Plant alkaloids are mitotic spindle poisons active in G2 and M phases of cell division (vinca alkaloids, taxanes) or are topoisomerase interactive agents (etoposide and teniposide). (vin.com)
• Vincristine and vinblastine are most commonly used, and new drugs such as etoposide, teniposide, and vinorelbine are being used in human medicine but have not yet received widespread use in veterinary oncology. (vin.com)
• This group of medicine includes etoposide , irinotecan , teniposide , and topotecan . (webmd.com)

Anticancer4

• Impact of histone deacetylase inhibitor valproic acid on the anticancer effect of etoposide on neuroblastoma cells. (nel.edu)
• Groh T, Hrabeta J, Poljakova J, Eckschlager T, Stiborova M. Impact of histone deacetylase inhibitor valproic acid on the anticancer effect of etoposide on neuroblastoma cells. (nel.edu)
• Dr. Yalowich's lab focuses on the mechanisms of action and resistance to DNA topoisomerase II (topo II)-targeted agents, such as the anticancer agent etoposide (VP-16). (osu.edu)
• We recently reported that enzyme-mediated DNA cleavage complexes (in which TopoII is covalently linked to the cleaved DNA during catalysis) formed in the presence of the anticancer drug etoposide persisted approximately 3-fold longer with TopoIIα than TopoIIβ. (h-its.org)

Inhibitor of topoisomerase1

• Etoposide (Vepesid, VP-16), an inhibitor of topoisomerase II, is a chemotherapeutic drug commonly used for treatment of different types of malignant diseases. (nel.edu)

Inhibits3

• In this study, we show that IκBαM expression inhibits stress-induced NF-κB activation and prevents BFA-, hypoxia-, and OA-induced resistance to etoposide. (aspetjournals.org)
• Inhibits topoisomerase II and causes DNA strand breakage, causing cell proliferation to arrest in late S or early G 2 portion of cell cycle. (medscape.com)
• Etoposide inhibits topoisomerase II , thus stopping DNA replication. (medchemexpress.com)

VePesid1

• Etoposide phosphate (Eposin®, Etopophos®, Vepesid®, VP-16®) is an inhibitor of the enzyme topoisomerase II. (the-medical-dictionary.com)

Camptothecin2

• We have shown that colorectal cancer cell lines defective in DNA MMR exhibit an increased sensitivity to both camptothecin, a topoisomerase I inhibitor, and etoposide, a topoisomerase II inhibitor. (aacrjournals.org)
• Altered topoisomerase I and II activity prevents drugs such as doxorubicin, etoposide and camptothecin from binding the topoisomerase-DNA complex, allowing the broken strands to be repaired. (nature.com)

Inhibition2

• Thus, when topoisomerase I inhibition occurs with agents such as SN-38 in cell lines, the cells compensate by increasing expression of topoisomerase II and vice versa. (cancernetwork.com)
• 3] This antagonism might be related to topoisomerase I inhibition of DNA synthesis, which is required for the cytotoxic effect of topoisomerase II-induced cleavable complexes. (cancernetwork.com)

Pathways2

• In parallel, Dr. Pommier has profoundly contributed to the elucidation of the repair pathways for topoisomerase-=induced DNA damage (Pommier et al. (cancer.gov)
• 2018). While studying the tyrosyl-DNA-phosphodiesterase (TDP1 and TDP2) repair pathways for the excision of topoisomerases from DNA, Dr. Pommier revealed that TDP1 repairs a broad range of 3'-blocking lesions in addition to TOP1 (Murai et al. (cancer.gov)

Replication3

• Topoisomerases are nuclear enzymes that modify the topological state of DNA and participate in fundamental metabolic processes such as replication, transcription, repair, recombination, and chromosome segregation (1) . (aacrjournals.org)
• Human DNA topoisomerase II-binding protein 1 (hTopBP1) plays an important role in DNA replication and the DNA damage checkpoint pathway. (biomedcentral.com)
• Human DNA topoisomerase II-binding protein 1 (TopBP1) and its orthologs play important roles in DNA replication and checkpoint control [ 1 ]. (biomedcentral.com)

Catalytic activity2

• TOP2A is one of the isoenzymes which can mediate the catalytic activity of type II topoisomerases [ 6 ]. (jcancer.org)
• Selected flavonoids were tested for their ability to inhibit the catalytic activity of DNA topoisomerase (topo) I and II. (ucy.ac.cy)

Drugs3

• Sensitivity to these drugs cannot be predicted by measuring endogenous levels of topoisomerase I and II. (aacrjournals.org)
• They also indicate that the impact of VPA on cytotoxicity of etoposide in these tumor cells varies depending on the sequence of cultivation of the cells with the drugs. (nel.edu)
• Etoposide and VPA were found as cycle phase specific drugs that are cytotoxic to human UKF-NB-4 neuroblastoma cells used either as single drugs or both together. (nel.edu)

Induces2

• On the other hand, etoposide treatment reliably induces DNA damage-related senescence in human articular chondrocytes evidenced by loss of proliferative capacity, DNA damage accumulation, and expression of some SASP components. (aging-us.com)
• Etoposide induces cell cycle arrest, apoptosis and autophagy . (medchemexpress.com)

Cytotoxic2

• However, whereas VPA might sensitize the cells to etoposide, inappropriate sequence of cultivation of the cells with VPA can decrease the etoposide cytotoxic efficacy. (nel.edu)
• In cell lines, the cytotoxic effect of topoisomerase I and II is scheduledependent. (cancernetwork.com)

Resistance6

• In this study, treatment of EMT6 mouse mammary tumor cells with hypoxia or the chemical stress agents brefeldin A (BFA) or okadaic acid (OA) causes the development of resistance to the topoisomerase II inhibitor etoposide. (aspetjournals.org)
• These results indicate that NF-κB activation mediates both chemical and physiological drug resistance to etoposide. (aspetjournals.org)
• CRISPR/Cas9 Genome Editing of the Human Topoisomerase II Intron 19 5' Splice Site Circumvents Etoposide Resistance in Human Leukemia K562 Cells. (osu.edu)
• hsa-miR-9-3p and hsa-miR-9-5p as Post-Transcriptional Modulators of DNA Topoisomerase II in Human Leukemia K562 Cells with Acquired Resistance to Etoposide. (osu.edu)
• Effects of DNA topoisomerase IIα splice variants on acquired drug resistance. (osu.edu)
• Tumor cell resistance to anthracyclines and epipodophyllotoxins can be due to reduced drug accumulation and/or alterations in the activity of topoisomerase II (TOPO II). (ucy.ac.cy)

Cleavage1

• This may explain the greater persistence of etoposide-stabilized cleavage complexes formed with Topo TopoIIα. (h-its.org)

Complexes2

• J Med Chem 2005) and extended it to macromolecular complexes involving proteins and protein-RNA complexes beyond topoisomerases (Pommier et al. (cancer.gov)
• We also used smoothed potential MD to estimate etoposide dissociation kinetics from the two isoform complexes. (h-its.org)

Hypoxic3

• The effects of etoposide and VPA on UKF-NB-4 cells were tested under the normoxic and also the hypoxic (1% O2) cultivation conditions. (nel.edu)
• Hypoxic melanoma cells sorted for VEGF-R2/CD133 positivity also undergo apoptosis when exposed to Etoposide and Bevacizumab. (oncotarget.com)
• When Etoposide and Bevacizumab-treated hypoxic cells were injected intravenously into immunodeficient mice revealed a reduced capacity to induce lung colonies, which also appear with a longer latency period. (oncotarget.com)

Cyclophosphamide1

• The incidence of acute myeloid leukemia following treatment of neuroblastoma is rare, however, only recently have patients with neuroblastoma received high doses of leukomogenic agents like etoposide and cyclophosphamide. (oncolink.org)

TOP11

• Recently, Dr. Pommier demonstrated that misincorporated ribonucleotides (the most frequent DNA alteration) trap topoisomerases, which convert them to toxic and mutagenic nicks by TOP1 (Kim et al. (cancer.gov)

Apoptosis1

• Etoposide does not influence phenotype of this sub-population of melanoma cells, while a combined treatment with Etoposide and Bevacizumab significantly abolished P1 sphere-forming ability, an effect associated with apoptosis of this subset of cells. (oncotarget.com)

Neuroblastoma3

• The cytotoxicity of etoposide and VPA to a UKF-NB-4 neuroblastoma cell line was evaluated with MTT assay. (nel.edu)
• The results of the study demonstrate that UKF-NB-4 neuroblastoma cells are sensitive both to etoposide and to VPA. (nel.edu)
• As a suitable sequence of cultivation, with a high rate of suppression of neuroblastoma cell growth was found the preincubation of the cells with etoposide, which was followed by their cultivation with VPA. (nel.edu)

Enzyme activity1

• By inhibiting the topoisomerase II enzyme activity in cancer cells, this drug leads to DNA damage and subsequently to cell death. (nel.edu)

Doses1

• With the addition of granulocytecolony-stimulating factor (G-CSF [Neupogen]) to the regimen,patients received epirubicin at clinically relevant doses after dose-escalation.Results of the topoisomerase activity will be reported with thefinal results of this phase I study. (cancernetwork.com)

Chromosome1

• TOP2A (DNA topoisomerase II alpha) gene, mapped to chromosome 17q12-q21, covers approximately 27.5 kb and includes 35 exons, encoding a 170 kDa protein [ 7 ]. (jcancer.org)

Tumor1

• It was identified that the nuclear division cycle 80, cyclin B2 and topoisomerase 2‑α may serve important roles in adrenocortical tumor development. (cancerindex.org)

Mechanisms2

• Mechanisms of action include intercalation of DNA and interference with topoisomerase enzyme function. (vin.com)
• According to their different acting mechanisms, DNA topoisomerases can be classified as type I and type II enzymes [ 3 , 6 ]. (jcancer.org)

Leukemia1

• Alkylating agents or radiation related and topoisomerase II inhibitor related acute myelogenous leukemia are often related to deletions of monosomies of chromosomes 5 and 7 amd a relatively long latency of 4-6 years. (standardofcare.com)

Targets1

• Hence, our study indicates that a combined exposure to Etoposide and Bevacizumab targets melanoma cells endowed with stem-like properties and might be considered a novel approach to treat cancer-initiating cells. (oncotarget.com)

Interactions2

• In this study, we report the results of classical molecular dynamics (MD) simulations to comparatively analyze the molecular interactions formed within the TopoII/DNA/etoposide complex with both isoforms. (h-its.org)
• These extensive classical and enhanced sampling simulations revealed stabilizing interactions of etoposide with two serine residues (Ser763 and Ser800) in TopoIIα. (h-its.org)

Cell4

• The effect of etoposide and VPA on the cell cycle distribution was determined by flow cytometric analysis using propidium iodide staining. (nel.edu)
• The effect of such combined treatment can be explained by measuring the cell cycle distribution, which shows that both etoposide and VPA change the cell cycle phase distribution. (nel.edu)
• Human type II topoisomerases (TopoII) are essential for controlling DNA topology within the cell. (h-its.org)
• The effects of WR-1065 (2-((aminopropyl)amino)ethanethiol) on cell cycle progression, topoisomerase (topo) IIα activity, and topo IIα phosphorylation in Chinese hamster ovary (CHO) cells have been investigated. (ucy.ac.cy)

Agents1

• Associated with topoisomerase II agents usually not associated with myelodysplastic syndrome and frequently associated with 11q23 cytogenetic abnormality. (standardofcare.com)

Potent1

• Podofilox (Podophyllotoxin) is a potent inhibitor of microtubule assembly and DNA topoisomerase II. (medchemexpress.com)

Exposure1

• This study used etoposide, to induce DNA damage-related senescence or chronic exposure to IL-1β to entail inflammation-related senescence in human OA chondrocytes. (aging-us.com)

Gene2

• This gene encodes a DNA topoisomerase, an enzyme that controls and alters the topologic states of DNA during transcription. (cancerindex.org)
• Dr. Pommier discovered the 6th vertebrate topoisomerase gene, TOP1MT (Zhang et al. (cancer.gov)

Strand1

• The presence of antitumor antibiotics within the structure of DNA induced failure to replicate DNA, impaired protein production through interference with transcription of messenger RNA, and chromosomal strand breaks caused by interference with the unwinding of DNA via topoisomerase. (vin.com)

Topology1

• DNA topoisomerases, ubiquitously present in eukaryotes, archaebacteria and Eubacteria, are necessary for the regulation of DNA topology in various cellular procedures [ 3 , 4 ]. (jcancer.org)

Treatment1

• These data suggest that JAG-6A could be an alternative topoisomerase IIα inhibitor and used for the treatment of HGG. (psu.edu)

Human2

• 3,5] The additive/synergistic effect of sequential topoisomerase I and II inhibitor administration has been examined in vivo in several phase I and II human trials that explored their sequential administration. (cancernetwork.com)
• Smoothed Potential MD Simulations for Dissociation Kinetics of Etoposide To Unravel Isoform Specificity in Targeting Human Topoisomerase II. (h-its.org)

Expression1

• Ren L, Liu J, Gou K, Xing C. Copy number variation and high expression of DNA topoisomerase II alpha predict worse prognosis of cancer: a meta-analysis. (jcancer.org)

Activity1

• Results of the topoisomerase activity will be reported with the final results of this phase I study. (cancernetwork.com)

Cells2

• In contrast, the reversed combination (preincubation of the cells with VPA before their treating with etoposide) did not give any increase in etoposide cytotoxicity. (nel.edu)
• Later, they were administered high-dose etoposide, 1,500 mg/[m.sup.2], followed by granulocyte colony-stimulating factor for collection of peripheral blood stem cells. (the-medical-dictionary.com)

Cancer1

• Dr. Pommier is a leader on DNA topoisomerase biology and biochemistry, and their cancer relevance. (cancer.gov)

Damage1

• He was the first to show that topoisomerases are trapped by DNA damage (by oxidative base lesions, base alkylation, DNA nicks) (Pourquier et al. (cancer.gov)

Effect1

• 4] For example, topoisomerase I and II have shown antagonism when administered simultaneously,[ 5] but an additive synergistic effect when administered sequentially. (cancernetwork.com)