Topoisomerase II Inhibitors

Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II.

Also Known As:

DNA Gyrase Inhibitors; DNA Topoisomerase II Inhibitors; DNA Type 2 Topoisomerase Inhibitors; Gyrase Inhibitor, DNA; Gyrase Inhibitors, DNA; II Inhibitor, Topoisomerase; Inhibitor, DNA Gyrase; Inhibitor, Topoisomerase II; Inhibitors, DNA Gyrase; Inhibitors, Topoisomerase 2; Inhibitors, Topoisomerase II; DNA Gyrase Inhibitor; DNA Topoisomerase II Inhibitor; Topoisomerase 2 Inhibitors; Topoisomerase II Inhibitor

Networked: 562 relevant articles (20 outcomes, 52 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Chemical Actions and Uses
- Pharmacologic Actions: 160
  - Therapeutic Uses: 47080
    - Antineoplastic Agents: 20689
      - Topoisomerase Inhibitors: 373
        Topoisomerase II Inhibitors: 562
  - Molecular Mechanisms of Pharmacological Action: 24
    - Enzyme Inhibitors: 1659
      - Topoisomerase Inhibitors: 373
        Topoisomerase II Inhibitors: 562

Experts

1.	Sullivan, Daniel M: 5 articles (01/2016 - 02/2003)
2.	Boichuk, Sergei: 4 articles (05/2022 - 01/2018)
3.	Galembikova, Aigul: 4 articles (05/2022 - 01/2018)
4.	Baer, Maria R: 4 articles (08/2021 - 09/2007)
5.	Ding, Jian: 4 articles (08/2011 - 08/2003)
6.	Bikinieva, Firuza: 3 articles (05/2022 - 11/2020)
7.	Dunaev, Pavel: 3 articles (01/2021 - 01/2018)
8.	Morton, Lindsay M: 3 articles (01/2021 - 01/2019)
9.	Guilbaud, Nicolas: 3 articles (01/2019 - 10/2014)
10.	Lin, Yun-Wei: 3 articles (01/2018 - 03/2012)

Related Diseases

1.	Neoplasms (Cancer) 01/25/2021 - "Importantly, 2-APCAs were also effective in cancer cell lines exhibiting resistance to certain chemotherapeutic agents, including MTAs and topoisomerase II inhibitors. " 03/01/2021 - "The findings provide evidence that PND is a topoisomerase II inhibitor and can hinder cancer progression in an animal model, further demonstrating PND's favorable characteristics as a repurposed anticancer drug." 01/01/2021 - "The results for topoisomerase II inhibitors are particularly important given their increasing use to treat childhood cancer." 10/01/2015 - "To develop novel selective topoisomerase II inhibitors, we designed and synthesized a series of conformationally constrained hydroxylated 4-phenyl-2-aryl chromenopyridines and evaluated their topoisomerase inhibitory activity and cytotoxicity against three human cancer cell lines (DU145, HCT15, and T47D) and a normal cell line (MCF10A). " 11/01/2014 - "Drug regimen used to treat the primary neoplasm was available for 54 patients; 52 had received a topoisomerase II inhibitor, known to induce MLL rearrangement. "
2.	Small Cell Lung Carcinoma (Small Cell Lung Cancer) 01/01/2014 - "Sequence-dependent improved efficacy of topoisomerase I followed by topoisomerase 2 inhibitors was assessed in a randomized phase II study in extensive-stage small-cell lung cancer (SCLC). " 04/01/2014 - "We conducted an open-label, multicenter, single-arm study to confirm the efficacy and safety of amrubicin (AMR), a topoisomerase II inhibitor, for treating refractory small-cell lung cancer (SCLC). " 12/01/2006 - "This multicenter, phase II study was conducted to evaluate the activity of amrubicin, a topoisomerase II inhibitor, against refractory or relapsed small-cell lung cancer (SCLC). " 09/01/2022 - "Amrubicin, a topoisomerase II inhibitor, is mainly used in the second-line treatment of patients with extensive-stage small cell lung cancer (ES-SCLC). " 12/10/2014 - "Amrubicin, a third-generation anthracycline and potent topoisomerase II inhibitor, showed promising activity in small-cell lung cancer (SCLC) in phase II trials. "
3.	Lymphoma (Lymphomas) 07/01/2008 - "In addition, we suggest that it might be possible to use topoisomerase II inhibitor agents in high grade gastric lymphomas." 01/01/1997 - "Topoisomerase II inhibitor-induced apoptosis in thymocytes and lymphoma cells." 01/01/1989 - "The cytotoxic and mutagenic effects of topoisomerase II inhibitors were measured in closely related strains of mouse lymphoma L5178Y cells differing in their sensitivity to ionizing radiation. " 01/01/2017 - "This work was part of a comparative oncology project assessing a new, clinical-stage topoisomerase II inhibitor and comparing it with etoposide in dogs with spontaneous lymphoma with the objective to translate findings from dogs to humans. " 06/01/2001 - "In addition, we determined the effects of DNA damage produced by the DNA topoisomerase II inhibitor etoposide on wild-type p53 transfected lymphoma cells. "
4.	Leukemia 10/01/2017 - "Cytogenetic and mutation profiling of the leukemia cells revealed the DNA-topoisomerase-II-inhibitor-associated t(9;11)(p22;q23) translocation and clonal KRAS and BRAF mutations. " 01/01/2011 - "Topoisomerase II inhibitors induce mainly acute leukemias which invariably correlate with dysregulation of the MLL gene. " 03/01/2008 - "The bisphenols represent a new structural class of topoisomerase II inhibitor that potently inhibited the growth of Chinese hamster ovary and K562 leukemia cells in the low micromolar range. " 09/08/2006 - "Felix, Leukemias related to treatment with DNA topoisomerase II inhibitors, Med. Pediatr. " 12/01/2005 - "Exposure to topoisomerase II inhibitors is linked to the generation of leukemia involving translocations of the MLL gene, normally restricted to an 8.3 kbp tract, the breakpoint cluster region (BCR). "
5.	Breast Neoplasms (Breast Cancer) 01/01/2009 - "Metnase mediates resistance to topoisomerase II inhibitors in breast cancer cells." 01/01/2000 - "Influence of topoisomerase II inhibitors and ionizing radiation on growth arrest and cell death pathways in the breast tumor cell." 04/15/1998 - "Previous work from this laboratory has demonstrated an association between the suppression of c-myc expression and the antiproliferative activity of both topoisomerase II inhibitors and ionizing radiation in MCF-7 breast tumor cells. " 09/01/2001 - "All 23 patients had previously received at least one topoisomerase II inhibitor, and in two patients 4-epi-doxorubicin had been administered as single-agent chemotherapy for breast cancer. " 11/01/1999 - "Previous studies from this laboratory as well as others have demonstrated that breast tumor cells fail to undergo primary apoptosis in response to agents which induce DNA damage such as ionizing radiation and the topoisomerase II inhibitor adriamycin. "

Related Drugs and Biologics

1.	Etoposide (VP 16)
2.	Alkylating Agents
3.	Type I DNA Topoisomerases (Topoisomerase I)
4.	sobuzoxane
5.	Doxorubicin (Adriamycin)
6.	Type II DNA Topoisomerases (Topoisomerase II)
7.	Amsacrine (AMSA)
8.	A-Form DNA (A-DNA)
9.	Enzymes
10.	Messenger RNA (mRNA)

Related Therapies and Procedures

1.	Drug Therapy (Chemotherapy)
2.	Therapeutics
3.	Radiotherapy
4.	Aftercare (After-Treatment)
5.	Adjuvant Chemotherapy