Topoisomerase inhibitors influence these essential cellular processes. Some topoisomerase inhibitors prevent topoisomerases ... Topoisomerase inhibitors are chemical compounds that block the action of topoisomerases, which are broken into two broad ... Catalytic inhibitors are the other main identification of TopII inhibitors. Common catalytic inhibitors are Bisdioxopiperazine ... topoisomerase inhibitors hold a prominent place among antibiotics and anticancer drugs in active medical use, as inhibitors ...

Topoisomerase inhibitors, Biosynthesis). ...

... distinct from catalytic inhibitors. Several human topoisomerase inhibitors are included on the World Health Organization's List ... Type I topoisomerase Type II topoisomerase Topoisomerase I Topoisomerase IIα Topoisomerase IIβ Topoisomerase IIIα Topoisomerase ... Other protein inhibitors of gyrase prevent DNA binding by the topoisomerase rather than stabilizing cleavage complexes. These ... The anthracyclines were the first topoisomerase inhibitors used to treat cancer and remain among the most widely employed and ...

16 topoisomerase inhibitors unsilence paternal UBE3A. Topoisomerases are enzymes that regulate the unwinding of DNA. Of these ... Topoisomerase-I is a nuclear enzyme that relieves torsional strain in DNA by opening single strand breaks. Once topoisomerase-I ... Pommier Y (October 2006). "Topoisomerase I inhibitors: camptothecins and beyond". Nature Reviews. Cancer. 6 (10): 789-802. doi: ... "Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons". Nature. 481 (7380): 185-9. doi:10.1038/nature10726 ...

... a topoisomerase inhibitor. Fludarabine and cytosine are less effective than standard ADE chemotherapy in high-risk acute ...

... a topoisomerase inhibitor. A phase II trial of mesna / ifosfamide, mitoxantrone and etoposide for refractory lymphomas Results ...

... a topoisomerase inhibitor. Cycles are repeated every 14 days for 3 cycles, then high-dose chemotherapy with autologous stem- ...

... and many topoisomerase inhibitors have been made. Resistance can occur when topoisomerase levels are decreased, or when ... Ganapathi, Ram; Ganapathi, Mahrukh K. (2013-01-01). "Mechanisms regulating resistance to inhibitors of topoisomerase II". ... as well as mutations in other cancers that confer resistance to topoisomerase inhibitors. One of the mechanisms of ... Topoisomerase is a lucrative target for cancer therapy due to its critical role as an enzyme in DNA replication, ...

Pommier, Yves; Cushman, Mark; Doroshow, James H. (2018-12-18). "Novel clinical indenoisoquinoline topoisomerase I inhibitors: a ... "Indenoisoquinoline Topoisomerase Inhibitors Strongly Bind and Stabilize the MYC Promoter G-Quadruplex and Downregulate MYC". ... "Indenoisoquinoline derivatives as topoisomerase I inhibitors that suppress angiogenesis by affecting the HIF signaling pathway ... "Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors". Bioorganic & Medicinal Chemistry Letters. 14 (14): ...

... as a New Topoisomerase Poison Inhibitor". PLOS ONE. 8 (4): e60770. Bibcode:2013PLoSO...860770C. doi:10.1371/journal.pone. ...

... as a New Topoisomerase Poison Inhibitor". PLOS ONE. 8 (4): e60770. Bibcode:2013PLoSO...860770C. doi:10.1371/journal.pone. ... Kekuda, T.R Prashith; Lavanya, D .; Pooja, Rao (March 2019). "Lichens as promising resources of enzyme inhibitors: A review". ... Anziaic acid works as an antibacterial compound by inhibiting topoisomerase. Anziaic acid has been artificially produced from ...

They are potent inhibitors on topoisomerase I and both have alkylsilyl groups in position 7 which make them lipophilic and more ... Camptothecin (CPT) is a topoisomerase inhibitor. It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening ... For example, is a derivate called CKD-602, which is a potent topoisomerase I inhibitor and successfully overcomes the poor ... Topoisomerase inhibitors, Quinoline alkaloids, Tertiary alcohols, Delta-lactones, Delta-lactams, Pyranoindolizinoquinolines, ...

... is a topoisomerase inhibitor. Robinson HM, Bratlie-Thoresen S, Brown R, Gillespie DA (May 2007). "Chk1 is required for ... Topoisomerase inhibitors, All stub articles, Organic compound stubs). ... G2/M checkpoint response induced by the catalytic topoisomerase II inhibitor ICRF-193". Cell Cycle. 6 (10): 1265-7. doi:10.4161 ...

... is a chemotherapeutic agent that is a topoisomerase inhibitor (Top1). It varies from other camptothecin based Top1 inhibitors ... potent topoisomerase I inhibitors and promising anticancer drugs". Critical Reviews in Oncology/Hematology. 45 (1): 91-108. doi ...

... is a type II topoisomerase inhibitor; it disrupts DNA synthesis and DNA repair in both healthy cells and cancer ... Topoisomerase inhibitors, IARC Group 2B carcinogens, Primary alcohols, Merck brands, Aromatic amines, Dihydroxyanthraquinones, ... "On the structural basis and design guidelines for type II topoisomerase-targeting anticancer drugs". Nucleic Acids Research. 41 ...

It works as a topoisomerase I inhibitor. Chemically, it consists of four units of irinotecan (a topoisomerase I inhibitor in ... Topoisomerase inhibitors, All stub articles, Antineoplastic and immunomodulating drug stubs). ...

Cragg, Gordon M.; Newman, David J. (2004). "A Tale of Two Tumor Targets: Topoisomerase I and Tubulin. The Wall and Wani ... Agents which act as inhibitors of tubulin, also act as inhibitors of cell division. A microtubule exists in a continuous ... Development of inhibitors that have their binding site in α-tubulin. This part of tubulin dimer remains unused because all ... Tubulin inhibitors are chemotherapy drugs that interfere directly with the tubulin system, which is in contrast to those ...

Topoisomerase inhibitors are widely used as chemotherapeutics and cause replicating cells to undergo apoptosis by inducing ... December 2011). "Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons". Nature. 481 (7380): 185-189. doi: ... Another study tested a large library of different drugs, and identified several topoisomerase I and II inhibitors which ...

February 2003). "Phase II study of XR 5000 (DACA), an inhibitor of topoisomerase I and II, administered as a 120-h infusion in ... August 2003). "Phase II study of XR5000 (DACA), an inhibitor of topoisomerase I and II, administered as a 120-h infusion in ... It belongs to the family of drugs called topoisomerase inhibitors.[citation needed] While the agent was well tolerated in Phase ... January 2002). "Phase II study of XR 5000, an inhibitor of topoisomerases I and II, in advanced colorectal cancer". European ...

"Pyrrolopyrimidine inhibitors of DNA gyrase B (GyrB) and topoisomerase IV (ParE). Part I: Structure guided discovery and ... as well as the discovery of the TriBE inhibitors, a novel class of DNA gyrase/Topoisomerase IV antibacterial agents that target ... Novel DNA Gyrase inhibitors. At Trius Pharmaceuticals, Shaw lead the microbiology efforts in designing a screening regimen for ... novel DNA gyrase/topoisomerase IV program. These efforts led to the discovery of the TriBE inhibitors, a novel class of agents ...

Wu, Xing (2011). "Cadmium Is a Catalytic Inhibitor of DNA Topoisomerase II". Journal of Inorganic Biochemistry. 105 (6): 833-8 ... Cadmium cations react with the topoisomerase in the following manner: 8 Cd2+ + topoisomerase IIα − 8H → topoisomerase IIα − 8 ... Lead has been shown to be an inhibitor of cell division, water uptake, and photosynthesis, eventually causing death to the ... Cadmium has been shown to be carcinogenic due to interactions with DNA topoisomerase IIα. This enzyme helps facilitate cell ...

... is in the topoisomerase inhibitor family of medication. It is believed to work by damaging DNA. Etoposide was ... Hande KR (1998). "Etoposide: four decades of development of a topoisomerase II inhibitor". Eur. J. Cancer. 34 (10): 1514-21. ... Topoisomerase inhibitors, World Health Organization essential medicines, Wikipedia medicine articles ready to translate). ... which causes the DNA breaks made by topoisomerase II to stay broken, and also prevents the topoisomerase II molecule from ...

... a topoisomerase inhibitor from the group of epipodophyllotoxins; Prednisolone: a glucocorticoid hormone that can cause ...

Ishiyama, D; Kanai, Y; Senda, H; Iwatani, W; Iwatani, W; Konno, H; Kanazawa, S (2000). "Novel human topoisomerase I inhibitors ...

Inhibitors of topoisomerases can act at two different levels. First inhibiting topoisomerase, which stabilize the topoisomerase ... or induced by other inhibitors of topoisomerase II that act as inhibitors of topoisomerase. Even when 60% of the target cells ... HU-331 seems to be a catalytic inhibitor of topoisomerase II, probably by enzymatic ligation to the protein. This molecule does ... 2007). "HU-331, a novel cannabinoid-based anticancer topoisomerase II inhibitor". Mol. Cancer Ther. 6 (1): 173-183. doi:10.1158 ...

... also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II. In contrast, the ... Topoisomerase inhibitors, All stub articles, Antineoplastic and immunomodulating drug stubs). ... Ketron AC, Denny WA, Graves DE, Osheroff N (February 2012). "Amsacrine as a Topoisomerase II Poison: Importance of Drug-DNA ... Nitiss JL (May 2009). "Targeting DNA topoisomerase II in cancer chemotherapy". Nature Reviews. Cancer. 9 (5): 338-50. doi: ...

Furthermore, his group works on novel topoisomerase inhibitors for the treatment of cancer. For his research, many awards have ... "A Dual Topoisomerase Inhibitor of Intense Pro-Apoptotic and Antileukemic Nature for Cancer Treatment". ChemMedChem. 12 (5): 347 ...

... inhibitors and poisons. Due to their frequent presence in proliferating eukaryotic cells, inhibitors of type II topoisomerases ... Type IIA topoisomerases include the enzymes DNA gyrase, eukaryotic topoisomerase II (topo II), and bacterial topoisomerase IV ( ... The roles of type IIB topoisomerases are less understood. Unlike type IIA topoisomerases, type IIB topoisomerases cannot ... a novel bacterial topoisomerase inhibitor. The C-terminal region of the prokaryotic topoisomerases has been solved for multiple ...

... is a known potent and selective inhibitor of protein serine/threonine phosphatases, as well as DNA topoisomerase II ... "Phase I and pharmacokinetic study of the topoisomerase II catalytic inhibitor fostriecin". British Journal of Cancer. 79 (5-6 ... Armstrong SC, Gao W, Lane JR, Ganote CE (January 1998). "Protein phosphatase inhibitors calyculin A and fostriecin protect ... a novel inhibitor of cell adhesion to components of extracellular matrix produced by Streptomyces sp. MJ654-NF4. I. Taxonomy, ...

"DNA topoisomerase inhibitor acutissimin a and other flavano-ellagitannins in red wine". Angewandte Chemie. 42 (48): 6012-4. doi ... "DNA Topoisomerase Inhibitor Acutissimin A and Other Flavano-Ellagitannins in Red Wine". Angewandte Chemie. 115 (48): 6194-6. ...