topoisomerase inhibitors

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  • Topoisomerase-1 gene copy aberrations are frequent in patients with breast cancer.
  • Kümler I1, Balslev E2, Poulsen TS2, Nielsen SL3, Nygård SB3, Rømer MU4, Christensen IJ5, Høgdall E2, Moreira J3, Nielsen DL1, Brünner N3, Stenvang J3.
  • International journal of cancer. Journal international du cancer.Int J Cancer.2015 Oct 15;137(8):2000-6. doi: 10.1002/ijc.29556. Epub 2015 Apr 27.
  • Topoisomerase-1 (Top1) targeting drugs have shown promising efficacy in patients with metastatic breast cancer (BC). However, these drugs are rather toxic calling for development and validation of predictive biomarkers to increase the therapeutic index. As these drugs are targeting the Top1 protein
  • PMID 25855483
  • Interfacial inhibitors.
  • Pommier Y1, Kiselev E1, Marchand C1.
  • Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2015 Sep 15;25(18):3961-5. doi: 10.1016/j.bmcl.2015.07.032. Epub 2015 Jul 18.
  • Targeting macromolecular interface is a general mechanism by which natural products inactivate macromolecular complexes by stabilizing normally transient intermediates. Demonstrating interfacial inhibition mechanism ultimately relies on the resolution of drug-macromolecule structures. This review fo
  • PMID 26235949
  • Insights into the Mechanism of Inhibition of Novel Bacterial Topoisomerase Inhibitors from Characterization of Resistant Mutants of Staphylococcus aureus.
  • Lahiri SD1, Kutschke A2, McCormack K2, Alm RA2.
  • Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2015 Sep;59(9):5278-87. doi: 10.1128/AAC.00571-15. Epub 2015 Jun 15.
  • The type II topoisomerases DNA gyrase and topoisomerase IV are clinically validated bacterial targets that catalyze the modulation of DNA topology that is vital to DNA replication, repair, and decatenation. Increasing resistance to fluoroquinolones, which trap the topoisomerase-DNA complex, has led
  • PMID 26077256


  • Smarcal1 promotes double-strand-break repair by nonhomologous end-joining.
  • Therapy-related Leukemia with Inv(16)(p13.1q22) and Type D CBFB/MYH11 Developing after Exposure to Irinotecan-containing Chemoradiotherapy
  • 濾胞性リンパ腫に対するRFM療法後に発症した治療関連慢性骨髄性白血病


Topoisomerase inhibitors are agents designed to interfere with the action of topoisomerase enzymes [1] (topoisomerase I and II), which are enzymes that control the changes in DNA structure [2] by catalyzing the breaking and ...
Both topoisomerase I and II inhibitors bind to the topoisomerase molecule. This makes the enzyme nonfunctional by blocking the ability of the topoisomerase to bind the DNA back together after it has been cut.


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  • n.

WordNet   license wordnet

「a substance that retards or stops an activity」

PrepTutorEJDIC   license prepejdic

「抑制する人(物) / 化学反応抑制剤」


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