DGIdb - TOP2A Gene Record

TOP2A 7153 Druggable GenomeClinically Actionable

Alternate Names:

7153
DNA TOPOISOMERASE II ALPHA
TOP2A
TOP2
TP2A
126430
11989
ENSG00000131747
OTTHUMG00000155008
DNA topoisomerase II, alpha isozyme
DNA topoisomerase 2-alpha
TOPOISOMERASE II ALPHA (FRAGMENT). [SOURCE:UNIPROT/SPTREMBL;ACC:Q71UQ5]
Q71UN1_HUMAN
PA354
2637
P11388
TOP2A_HUMAN
BE0000742
T17048
NM_001067
NP_001058
BE0004951

Gene Info:

Human Readable Name	DRUGGABLE GENOME
Target Class	Enzymes
Target Subclass	EC:5.99.1.3
Interpro Name	DNA topoisomerase, type IIA
Interpro Type	Domain
Interpro Short Name	Topo_IIA
Interpro Short Name	Topo_IIA_A/C
Interpro Type	Family
Interpro Acc	IPR003594
Interpro Name	ATPase-like, ATP-binding domain
Interpro Name	DNA topoisomerase, type IIA, subunit A/C-terminal
Uniprot Evidence	1: Evidence at protein level
Interpro Acc	IPR001241
Interpro Short Name	ATPase-like_ATP-bd
Uniprot Status	Swiss-Prot
Interpro Acc	IPR002205
Target Subclass	5.99.1.3
Target Main Class	Enzymes
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	DNA topoisomerases
GuideToPharmacology Gene Category ID	851

(16 More Sources)

Gene Categories: Category Details

DRUGGABLE GENOME
CLINICALLY ACTIONABLE
ENZYME

Publications:

Kurata et al., 2007, Amrubicin for non-small-cell lung cancer and small-cell lung cancer., Invest New Drugs
Petit et al., 2004, Comparative value of tumour grade, hormonal receptors, Ki-67, HER-2 and topoisomerase II alpha status as predictive markers in breast cancer patients treated with neoadjuvant anthracycline-based chemotherapy., Eur. J. Cancer
Liang et al., 2007, Solamargine upregulation of Fas, downregulation of HER2, and enhancement of cytotoxicity using epirubicin in NSCLC cells., Mol Nutr Food Res
Knoop et al., 2005, retrospective analysis of topoisomerase IIa amplifications and deletions as predictive markers in primary breast cancer patients randomly assigned to cyclophosphamide, methotrexate, and fluorouracil or cyclophosphamide, epirubicin, and fluorouracil: Danish Breast Cancer Cooperative Group., J. Clin. Oncol.
Kamal A et al., 2011, Synthesis of 4β-carbamoyl epipodophyllotoxins as potential antitumour agents., Bioorg Med Chem
Evdokimov NM et al., 2011, Structural simplification of bioactive natural products with multicomponent synthesis. 3. Fused uracil-containing heterocycles as novel topoisomerase-targeting agents., J Med Chem
Tan S et al., 2015, Antiproliferative and apoptosis-inducing activities of novel naphthalimide-cyclam conjugates through dual topoisomerase (topo) I/II inhibition., Bioorg Med Chem
Chhikara BS et al., 2012, Synthesis, anticancer activities, and cellular uptake studies of lipophilic derivatives of doxorubicin succinate., J Med Chem
Chen Z et al., 2010, A new class of naphthalimide-based antitumor agents that inhibit topoisomerase II and induce lysosomal membrane permeabilization and apoptosis., J Med Chem
Hayashi et al., 2006, Enhancement of radiosensitivity by topoisomerase II inhibitor, amrubicin and amrubicinol, in human lung adenocarcinoma A549 cells and kinetics of apoptosis and necrosis induction., Int. J. Mol. Med.
Koehn et al., 2007, Differential regulation of DNA repair protein Rad51 in human tumour cell lines exposed to doxorubicin., Anticancer Drugs
Rody et al., 2007, Gene expression profiling of breast cancer patients treated with docetaxel, doxorubicin, and cyclophosphamide within the GEPARTRIO trial: HER-2, but not topoisomerase II alpha and microtubule-associated protein tau, is highly predictive of tumor response., Breast
Azarova et al., 2007, Roles of DNA topoisomerase II isozymes in chemotherapy and secondary malignancies., Proc. Natl. Acad. Sci. U.S.A.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Menendez et al., 2006, DNA topoisomerase IIalpha (TOP2A) inhibitors up-regulate fatty acid synthase gene expression in SK-Br3 breast cancer cells: in vitro evidence for a 'functional amplicon' involving FAS, Her-2/neu and TOP2A genes., Int. J. Mol. Med.
Hussy et al., 1986, Effect of 4-quinolones and novobiocin on calf thymus DNA polymerase alpha primase complex, topoisomerases I and II, and growth of mammalian lymphoblasts., Antimicrob. Agents Chemother.
Robinson et al., 1992, Effects of novel fluoroquinolones on the catalytic activities of eukaryotic topoisomerase II: Influence of the C-8 fluorine group., Antimicrob. Agents Chemother.
Jiménez-Alonso S et al., 2008, Design and synthesis of a novel series of pyranonaphthoquinones as topoisomerase II catalytic inhibitors., J Med Chem
Sperry J et al., 2009, Pyranonaphthoquinone derivatives of eleutherin, ventiloquinone L, thysanone and nanaomycin A possessing a diverse topoisomerase II inhibition and cytotoxicity spectrum., Bioorg Med Chem
Brown et al., 1998, Immunohistochemical staining for DNA topoisomerase IIa in Hodgkin's disease., Am. J. Clin. Pathol.
Faure et al., 1996, [Topoisomerases: therapeutic value]., Ann Pharm Fr
Umanskaya et al., Inhibition of DNA topoisomerase II in living cells stimulates illegitimate recombination., Dokl. Biochem. Biophys.
de Lucio et al., 2005, Characterization of human NSCLC cell line with innate etoposide-resistance mediated by cytoplasmic localization of topoisomerase II alpha., Cancer Sci.
Winnicka et al., Cardiac glycosides in cancer research and cancer therapy., Acta Pol Pharm
Uesaka et al., 2007, Enhanced expression of DNA topoisomerase II genes in human medulloblastoma and its possible association with etoposide sensitivity., J. Neurooncol.
Atkinson et al., 2007, Examination of the distribution of the bioreductive drug AQ4N and its active metabolite AQ4 in solid tumours by imaging matrix-assisted laser desorption/ionisation mass spectrometry., Rapid Commun. Mass Spectrom.
Schmidt EW et al., 1995, Makaluvamines H-M and damirone C from the pohnpeian sponge Zyzzya fuliginosa., J Nat Prod
Aubel-Sadron et al., 1984, Daunorubicin and doxorubicin, anthracycline antibiotics, a physicochemical and biological review., Biochimie
Zunino et al., 1990, DNA topoisomerase II as the primary target of anti-tumor anthracyclines., Anticancer Drug Des.
McPherson et al., Selective sensitization of adriamycin-resistant P388 murine leukemia cells to antineoplastic agents following transfection with human DNA topoisomerase II alpha., Anticancer Res.
Guerrant W et al., 2012, Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors., J Med Chem
Shi DK et al., 2012, Design, synthesis and biological evaluation of novel glycosylated diphyllin derivatives as topoisomerase II inhibitors., Eur J Med Chem
Ko et al., 2008, Acute promyelocytic leukemic involvement of the optic nerves following mitoxantrone treatment for multiple sclerosis., J. Neurol. Sci.
Mao et al., 1999, Mutations of human topoisomerase II alpha affecting multidrug resistance and sensitivity., Biochemistry
Wang et al., 2001, Atp-bound topoisomerase ii as a target for antitumor drugs., J. Biol. Chem.
Takeda et al., 1998, A case of therapy-related acute myeloblastic leukemia with t(16;21)(q24;q22) after chemotherapy with DNA-topoisomerase II inhibitors, etoposide and mitoxantrone, and the alkylating agent, cyclophosphamide., Int. J. Hematol.
Satherley et al., 2000, Relationship between expression of topoisomerase II isoforms and chemosensitivity in choroidal melanoma., J. Pathol.
Hasinoff et al., 2001, The catalytic DNA topoisomerase II inhibitor dexrazoxane (ICRF-187) induces differentiation and apoptosis in human leukemia K562 cells., Mol. Pharmacol.
Langer et al., 2001, Dexrazoxane is a potent and specific inhibitor of anthracycline induced subcutaneous lesions in mice., Ann. Oncol.
Hasinoff et al., 2002, The doxorubicin cardioprotective agent dexrazoxane (ICRF-187) induces endopolyploidy in rat neonatal myocytes through inhibition of DNA topoisomerase II., Anticancer Drugs
Hasinoff et al., 2007, Dexrazoxane: how it works in cardiac and tumor cells. Is it a prodrug or is it a drug?, Cardiovasc. Toxicol.
Kik et al., 2006, [Dexrazoxane (ICRF-187)--a cardioprotectant and modulator of action of some anticancer drugs]., Postepy Hig Med Dosw (Online)
Hasinoff et al., 1999, The cardioprotective and DNA topoisomerase II inhibitory agent dexrazoxane (ICRF-187) antagonizes camptothecin-mediated growth inhibition of Chinese hamster ovary cells by inhibition of DNA synthesis., Anticancer Drugs
Renodon-Cornière et al., 2003, Analysis of bisdioxopiperazine dexrazoxane binding to human DNA topoisomerase II alpha: decreased binding as a mechanism of drug resistance., Biochemistry
Hasinoff et al., 2000, The catalytic DNA topoisomerase II inhibitor dexrazoxane (ICRF-187) induces endopolyploidy in Chinese hamster ovary cells., J. Pharmacol. Exp. Ther.
López-Lázaro et al., 2005, Digitoxin inhibits the growth of cancer cell lines at concentrations commonly found in cardiac patients., J. Nat. Prod.
Moneypenny et al., 2006, MLL rearrangements are induced by low doses of etoposide in human fetal hematopoietic stem cells., Carcinogenesis
Nitiss et al., 1998, The bis(naphthalimide) DMP-840 causes cytotoxicity by its action against eukaryotic topoisomerase II., Biochemistry
Asano et al., 1996, Transfection of human topoisomerase II alpha into etoposide-resistant cells: transient increase in sensitivity followed by down-regulation of the endogenous gene., Biochem. J.
Asano et al., 1996, Transfection of a human topoisomerase II alpha gene into etoposide-resistant human breast tumor cells sensitizes the cells to etoposide., Oncol. Res.
Negi A et al., 2015, Imine/amide-imidazole conjugates derived from 5-amino-4-cyano-N1-substituted benzyl imidazole: Microwave-assisted synthesis and anticancer activity via selective topoisomerase-II-α inhibition., Bioorg Med Chem
Zhang X et al., 2013, The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase., Bioorg Med Chem
Chee GL et al., 2010, A diazirine-based photoaffinity etoposide probe for labeling topoisomerase II., Bioorg Med Chem
Chaniyara R et al., 2013, Novel antitumor indolizino[6,7-b]indoles with multiple modes of action: DNA cross-linking and topoisomerase I and II inhibition., J Med Chem
de Oliveira Figueiredo P et al., 2014, Further constituents of Galianthe thalictroides (Rubiaceae) and inhibition of DNA topoisomerases I and IIα by its cytotoxic β-carboline alkaloids., Bioorg Med Chem Lett
Li YB et al., 2013, Discovery, synthesis and biological evaluation of cycloprotoberberine derivatives as potential antitumor agents., Eur J Med Chem
Shankaraiah N et al., 2015, One-pot synthesis of podophyllotoxin-thiourea congeners by employing NH₂SO₃H/NaI: Anticancer activity, DNA topoisomerase-II inhibition, and apoptosis inducing agents., Bioorg Med Chem Lett
Liu LP et al., 2014, Topoisomerase II inhibitors from the roots of Stellera chamaejasme L., Bioorg Med Chem
Zhao W et al., 2014, A rational design strategy of the novel topoisomerase II inhibitors for the synthesis of the 4-O-(2-pyrazinecarboxylic)-4'-demethylepipodophyllotoxin with antitumor activity by diminishing the relaxation reaction of topoisomerase II-DNA decatenation., Bioorg Med Chem
Tan S et al., 2013, Oxo-heterocyclic fused naphthalimides as antitumor agents: synthesis and biological evaluation., Eur J Med Chem
Yadav AA et al., 2015, Structure-based design, synthesis and biological testing of piperazine-linked bis-epipodophyllotoxin etoposide analogs., Bioorg Med Chem
Chen W et al., 2014, Design and synthesis of 2-phenylnaphthalenoids as inhibitors of DNA topoisomeraseIIα and antitumor agents., Eur J Med Chem
Kamal A et al., 2012, Synthesis and biological evaluation of 4β-sulphonamido and 4β-[(4'-sulphonamido)benzamide]podophyllotoxins as DNA topoisomerase-IIα and apoptosis inducing agents., Bioorg Med Chem
Qiu J et al., 2015, Synthesis, biological evaluation and modeling studies of terphenyl topoisomerase IIα inhibitors as anticancer agents., Eur J Med Chem
Hajbi Y et al., 2010, Synthesis and biological activities of new furo[3,4-b]carbazoles: potential topoisomerase II inhibitors., Eur J Med Chem
Chen TC et al., 2015, Structure-based hybridization, synthesis and biological evaluation of novel tetracyclic heterocyclic azathioxanthone analogues as potential antitumor agents., Eur J Med Chem
Oppegard LM et al., 2012, Inhibition of human topoisomerases I and II by simocyclinone D8., J Nat Prod
He S et al., 2015, Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors., ACS Med Chem Lett
Genès C et al., 2011, Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents., Eur J Med Chem
Baviskar AT et al., 2015, Switch in Site of Inhibition: A Strategy for Structure-Based Discovery of Human Topoisomerase IIα Catalytic Inhibitors., ACS Med Chem Lett
Aleksić M et al., 2014, Anilides and quinolones with nitrogen-bearing substituents from benzothiophene and thienothiophene series: synthesis, photochemical synthesis, cytostatic evaluation, 3D-derived QSAR analysis and DNA-binding properties., Eur J Med Chem
Lemster T et al., 2009, Photochemical electrocyclisation of 3-vinylindoles to pyrido[2,3-a]-, pyrido[4,3-a]- and thieno[2,3-a]-carbazoles: design, synthesis, DNA binding and antitumor cell cytotoxicity., Eur J Med Chem
Hasinoff et al., 2008, The structure-based design, synthesis and biological evaluation of DNA-binding bisintercalating bisanthrapyrazole anticancer compounds., Bioorg. Med. Chem.
Hao H et al., 2015, Design and synthesis of 2-phenylnaphthalenoids and 2-phenylbenzofuranoids as DNA topoisomerase inhibitors and antitumor agents., Eur J Med Chem
Baviskar AT et al., 2011, N-fused imidazoles as novel anticancer agents that inhibit catalytic activity of topoisomerase IIα and induce apoptosis in G1/S phase., J Med Chem
Zhou Y et al., 2013, Synthesis, cytotoxicity and topoisomerase II inhibitory activity of lomefloxacin derivatives., Bioorg Med Chem Lett
Kamal A et al., 2015, Design and synthesis of dithiocarbamate linked β-carboline derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability., Bioorg Med Chem
Wang MJ et al., 2014, Design, synthesis, mechanisms of action, and toxicity of novel 20(s)-sulfonylamidine derivatives of camptothecin as potent antitumor agents., J Med Chem
Furbacher TR et al., 2001, Catalytic inhibition of topoisomerase IIalpha by demethylzeylasterone, a 6-oxophenolic triterpenoid from Kokoona zeylanica., J Nat Prod
Baviskar AT et al., 2013, Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity., Bioorg Med Chem
Huang ZH et al., 2013, Design, synthesis and biological evaluation of novel mansonone E derivatives prepared via CuAAC click chemistry as topoisomerase II inhibitors., Eur J Med Chem
Aleksić M et al., 2012, Novel substituted benzothiophene and thienothiophene carboxanilides and quinolones: synthesis, photochemical synthesis, DNA-binding properties, antitumor evaluation and 3D-derived QSAR analysis., J Med Chem
Ashour A et al., 2014, Rational design and synthesis of topoisomerase I and II inhibitors based on oleanolic acid moiety for new anti-cancer drugs., Bioorg Med Chem
Bar FM et al., 2009, Rational design and semisynthesis of betulinic acid analogues as potent topoisomerase inhibitors., J Nat Prod
Mariani A et al., 2015, Differential Targeting of Human Topoisomerase II Isoforms with Small Molecules., J Med Chem
Dunlap N et al., 2014, Synthesis and evaluation of ether-linked demethylepipodophyllotoxin dimers., Bioorg Med Chem Lett
Dong G et al., 2012, New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure-activity relationship analysis and biological evaluations., J Med Chem
Su TL et al., 2006, Potent antitumor 9-anilinoacridines and acridines bearing an alkylating N-mustard residue on the acridine chromophore: synthesis and biological activity., J Med Chem
Liu JF et al., 2013, Synthesis and cytotoxic activity on human cancer cells of carbamate derivatives of 4β-(1,2,3-triazol-1-yl)podophyllotoxin., Eur J Med Chem
Wada S et al., 2001, Screening of triterpenoids isolated from Phyllanthus flexuosus for DNA topoisomerase inhibitory activity., J Nat Prod
Zhou et al., 1999, Topoisomerase II-mediated alterations of K562 drug resistant sublines., Med. Oncol.
Willmore et al., 2002, Formation and longevity of idarubicin-induced DNA topoisomerase II cleavable complexes in K562 human leukaemia cells., Biochem. Pharmacol.
De Renzo et al., 1999, Acute promyelocytic leukemia after treatment for non-Hodgkin's lymphoma with drugs targeting topoisomerase II., Am. J. Hematol.
Bigioni et al., 1994, Base mutation analysis of topoisomerase II-idarubicin-DNA ternary complex formation. Evidence for enzyme subunit cooperativity in DNA cleavage., Nucleic Acids Res.
González-Cid et al., 2002, Correlation between chromosome damage and apoptosis induced by fludarabine and idarubicin in normal human lymphocytes., Toxicology
Tselepi M et al., 2011, Catalytic inhibition of eukaryotic topoisomerases I and II by flavonol glycosides extracted from Vicia faba and Lotus edulis., J Nat Prod
Van Quaquebeke E et al., 2007, 2,2,2-Trichloro-N-({2-[2-(dimethylamino)ethyl]-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin- 5-yl}carbamoyl)acetamide (UNBS3157), a novel nonhematotoxic naphthalimide derivative with potent antitumor activity., J Med Chem
Terada et al., 1992, Antitumor agents. I. DNA topoisomerase II inhibitory activity and the structural relationship of podophyllotoxin derivatives as antitumor agents., Chem. Pharm. Bull.
Zhang et al., 1992, Antitumor agents, 130, Novel 4 beta-arylamino derivatives of 3',4'-didemethoxy-3',4'-dioxo-4-deoxypodophyllotoxin as potent inhibitors of human DNA topoisomerase II., J. Nat. Prod.
Kamal et al., 2005, Synthesis and biological evaluation of new 4beta-anilino- and 4beta-imido-substituted podophyllotoxin congeners., Bioorg. Med. Chem.
Iida et al., 2000, Podophyllotoxin aza-analogue, a novel DNA topoisomerase II inhibitor., Chem. Pharm. Bull.
Ruckdeschel, 1991, Etoposide in the management of non-small cell lung cancer., Cancer
Quintana-Espinoza P et al., 2013, Synthesis and study of antiproliferative, antitopoisomerase II, DNA-intercalating and DNA-damaging activities of arylnaphthalimides., Bioorg Med Chem
Nitiss et al., 1992, Amsacrine and etoposide hypersensitivity of yeast cells overexpressing DNA topoisomerase II., Cancer Res.
Finlay et al., 1999, Inhibition of the action of the topoisomerase II poison amsacrine by simple aniline derivatives: evidence for drug-protein interactions., Oncol. Res.
Arimondo et al., 2000, Design of two etoposide-amsacrine conjugates: topoisomerase II and tubuline polymerization inhibition and relation to cytotoxicity., Anticancer Drug Des.
Ferlin et al., 2000, Synthesis and antiproliferative activity of some variously substituted acridine and azacridine derivatives., Eur J Med Chem
Matsumoto et al., 2001, Hypophosphorylation of topoisomerase IIalpha in etoposide (VP-16)-resistant human carcinoma cell lines associated with carboxy-terminal truncation., Jpn. J. Cancer Res.
Lee et al., 1992, Two independent amsacrine-resistant human myeloid leukemia cell lines share an identical point mutation in the 170 kDa form of human topoisomerase II., J. Mol. Biol.
Dalla Via L et al., 2009, Benzothiopyranoindole-based antiproliferative agents: synthesis, cytotoxicity, nucleic acids interaction, and topoisomerases inhibition properties., J Med Chem
Dalla Via L et al., 2012, A novel tetrahydrobenzoangelicin with dark and photo biological activity., Bioorg Med Chem
Christodoulou MS et al., 2015, Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2., Eur J Med Chem
Dalla Via L et al., 2009, DNA-targeting pyrroloquinoline-linked butenone and chalcones: synthesis and biological evaluation., Eur J Med Chem
Diana P et al., 2007, 3,5-bis(3'-indolyl)pyrazoles, analogues of marine alkaloid nortopsentin: synthesis and antitumor properties., Bioorg Med Chem Lett
Rene et al., 1996, The 1'-substituent on the anilino ring of the antitumor drug amsacrine is a critical element for topoisomerase II inhibition and cytotoxicity., Mol. Pharmacol.
Houlbrook et al., 1995, Relationship between expression of topoisomerase II isoforms and intrinsic sensitivity to topoisomerase II inhibitors in breast cancer cell lines., Br. J. Cancer
Nair et al., Differential effect of camptothecin treatment on topoisomerase II alpha expression in ML-1 and HL-60 leukemia cell lines., Anticancer Res.
Ferri N et al., 2011, Synthesis, structural, and biological evaluation of bis-heteroarylmaleimides and bis-heterofused imides., Bioorg Med Chem
Perabo et al., 2005, New agents in intravesical chemotherapy of superficial bladder cancer., Scand. J. Urol. Nephrol.
Zahir A et al., 1996, DNA topoisomerase I inhibitors: cytotoxic flavones from Lethedon tannaensis., J Nat Prod
Constantinou A et al., 1995, Flavonoids as DNA topoisomerase antagonists and poisons: structure-activity relationships., J Nat Prod
Snyder et al., 1999, Photogenotoxicity of fluoroquinolones in Chinese hamster V79 cells: dependency on active topoisomerase II., Photochem. Photobiol.
Maki et al., 2008, Drug resistance mechanism of the fish-pathogenic bacterium Lactococcus garvieae., J. Fish Dis.
Chawla SP et al., 2015, A phase 1B/2 study of aldoxorubicin in patients with soft tissue sarcoma., Cancer
Song G et al., 2010, Synthesis and biological evaluation of cytotoxic activity of novel anthracene L-rhamnopyranosides., Bioorg Med Chem
McKeage, 2015, Finafloxacin: first global approval., Drugs
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Wohlkonig et al., 2010, Structural basis of quinolone inhibition of type IIA topoisomerases and target-mediated resistance., Nat. Struct. Mol. Biol.
Reuveni et al., 2010, Moxifloxacin enhances etoposide-induced cytotoxic, apoptotic and anti-topoisomerase II effects in a human colon carcinoma cell line., Int. J. Oncol.
Baechler SA et al., 2013, Synthesis, topoisomerase-targeting activity and growth inhibition of lycobetaine analogs., Bioorg Med Chem
Du L et al., 2011, Unprecedented citrinin trimer tricitinol B functions as a novel topoisomerase IIα inhibitor., J Med Chem
Lindsey et al., 2005, Effects of benzene metabolites on DNA cleavage mediated by human topoisomerase II alpha: 1,4-hydroquinone is a topoisomerase II poison., Chem. Res. Toxicol.
Divo et al., 1988, Activity of fluoroquinolone antibiotics against Plasmodium falciparum in vitro., Antimicrob. Agents Chemother.
Zeglis BM et al., 2011, Role of metalation in the topoisomerase IIα inhibition and antiproliferation activity of a series of α-heterocyclic-N4-substituted thiosemicarbazones and their Cu(II) complexes., J Med Chem
Casu L et al., 2011, Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases., Bioorg Med Chem Lett
Dassonneville et al., 1999, Stimulation of topoisomerase II-mediated DNA cleavage by an indazole analogue of lucanthone., Biochem. Pharmacol.
Bases et al., 1997, Topoisomerase inhibition by lucanthone, an adjuvant in radiation therapy., Int. J. Radiat. Oncol. Biol. Phys.
Felix CA et al., 1995, ALL-1 gene rearrangements in DNA topoisomerase II inhibitor-related leukemia in children., Blood

AMONAFIDE TOP2A

Interaction Score: 2.34

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name amonafide,Quinamed

Novel drug target Established target

PMIDs:
26211460 23353750 20170164 24054489 17658777

Sources:
DTC DrugBank TdgClinicalTrial
AMRUBICIN TOP2A

Interaction Score: 1.76

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

PMIDs:
17628745

Sources:
DrugBank ChemblInteractions
CHEMBL607534 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19783445

Sources:
DTC
CHEMBL594259 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19783445

Sources:
DTC
UNGEREMINE TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22014547

Sources:
DTC
CHEMBL507986 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21391686

Sources:
DTC
LUPEOL TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11754608

Sources:
DTC
DIAZIRINE TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20006518

Sources:
DTC
HURATOXIN TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24931277

Sources:
DTC
CHEMBL596082 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19783445

Sources:
DTC
OLEANDEROLIDE TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24326278

Sources:
DTC
TRICITRINOL B TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21761866

Sources:
DTC
13-DEOXYDOXORUBICIN TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name GPX-100

Novel drug target Established target

PMIDs:
None found

Sources:
DrugBank TdgClinicalTrial
CHEMBL594257 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19783445

Sources:
DTC
CHEMBL594153 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19783445

Sources:
DTC
MAKALUVAMINE E TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8691207

Sources:
DTC
CHEMBL2023733 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22276998

Sources:
DTC
FINAFLOXACIN TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
25808831

Sources:
DrugBank
FRANGULIN B TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20561793

Sources:
DTC
TROVAFLOXACIN TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11752352

Sources:
DrugBank
ALDOXORUBICIN TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name INNO-206

Novel drug target Established target

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

PMIDs:
25312684

Sources:
DrugBank TdgClinicalTrial ChemblInteractions
MAKALUVAMINE F TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8691207

Sources:
DTC
CHEMBL593570 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19783445

Sources:
DTC
CHEMBL594379 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19783445

Sources:
DTC
CHEMBL594695 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19783445

Sources:
DTC
DEMETHYLZEYLASTERONE TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11678653

Sources:
DTC
MAKALUVAMINE A TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8691207

Sources:
DTC
VALRUBICIN TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

Direct Interaction yes

Trial Name -

PMIDs:
16019763 11752352

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND
ELINAFIDE TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21880496

Sources:
DTC
CHEMBL1080077 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19691293

Sources:
DTC
CHEMBL244268 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17658777

Sources:
DTC
KAEMPFERITRIN TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22014228

Sources:
DTC
BETULIN TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11754608

Sources:
DTC
4'-O-ACETYLPATENTIFLORIN B TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22119124

Sources:
DTC
MAKALUVAMINE C TFA SALT TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8691207

Sources:
DTC
CHEMBL1773343 TOP2A

Interaction Score: 1.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21489802

Sources:
DTC
DEXRAZOXANE TOP2A

Interaction Score: 1.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11179439 11332155 11984069 17652819 17115008 10194547 12911317 11046078 11752352

Sources:
DrugBank NCI
TENIPOSIDE TOP2A

Interaction Score: 0.88

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction DNA topoisomerase II inhibitor

PMIDs:
9426516 8702194 16480143 16271071 17514873 11752352 17361331

Sources:
DrugBank TdgClinicalTrial ChemblInteractions NCI TEND
MOXIFLOXACIN TOP2A

Interaction Score: 0.78

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
20802486 11752352 20596674

Sources:
DrugBank
ENOXACIN TOP2A

Interaction Score: 0.78

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10089819 11752352 18471102

Sources:
DrugBank
FLEROXACIN TOP2A

Interaction Score: 0.78

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
3015015 11752352 1323952

Sources:
DrugBank
ETOPOSIDE TOP2A

Interaction Score: 0.66

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
16271071 17514873 11752352 16309315 16377807 17361331 9494516 9485461 9426516 8870683 8823806 26216018 24095018 20006518 23360284 24507920 24012683 26292628 18816045 24931277 24775914 23353750 25922181 25240702 22364746 25800514 20863598 25799376 22867097 25815139 21435753 25941559 24334150 19386396 18258442 26291037 21644529 23566520 19783445 26264845 25003995 11678653 23920485 23968711 22620261 24326278 19691293 25945730 25466187 22867019 16759114 23711769

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions NCI TEND GuideToPharmacology
LUCANTHONE TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10487533 11752352 9169823

Sources:
DrugBank
SIMOCYCLINONE D8 TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22867097

Sources:
DTC
AMRUBICIN HYDROCHLORIDE TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
SECAUBRYOLIDE TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL2171812 TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22867019

Sources:
DTC
CHEMBL2332128 TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL2332126 TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AMSACRINE TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
1322791 10691026 11716434 11752352 11006484 11473732 1311390 19725581 22537681 25626146 19155103 17911018 8823806 8632768 8519659

Sources:
DTC DrugBank NCI
CHEMBL2171794 TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22867019

Sources:
DTC
CHEMBL2171781 TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22867019

Sources:
DTC
CHEMBL2332127 TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DAUNORUBICIN CITRATE TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
CARINATIN G TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BANOXANTRONE TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17340571

Sources:
DrugBank
VOSAROXIN TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Voreloxin

Novel drug target Established target

Mechanism of Interaction DNA topoisomerase II inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
BECATECARIN TOP2A

Interaction Score: 0.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name becatecarin, XL 119, rebeccamycin

Novel drug target Established target

Mechanism of Interaction DNA topoisomerase II inhibitor

PMIDs:
None found

Sources:
DrugBank TdgClinicalTrial ChemblInteractions
LOMEFLOXACIN TOP2A

Interaction Score: 0.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11752352

Sources:
DrugBank
LYCOBETAINE TOP2A

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23266176

Sources:
DTC
SPARFLOXACIN TOP2A

Interaction Score: 0.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11752352

Sources:
DrugBank
DECLOPRAMIDE TOP2A

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
ANNAMYCIN TOP2A

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
DIPHYLLIN TOP2A

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22119124

Sources:
DTC
BERUBICIN HYDROCHLORIDE TOP2A

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA topoisomerase II inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NORFLOXACIN TOP2A

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11752352

Sources:
DrugBank
GANCOTAMAB TOP2A

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PEFLOXACIN TOP2A

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11752352

Sources:
DrugBank
C-1311 TOP2A

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction DNA topoisomerase II inhibitor

Trial Name C-1311, XLS-002,Symadex

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
PODOFILOX TOP2A

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
1334447 1331331 11752352 16061385 10783066 1845848

Sources:
DrugBank TdgClinicalTrial TEND
CIPROFLOXACIN TOP2A

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
3015015 11752352 1323952

Sources:
DrugBank
ELSAMITRUCIN TOP2A

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
MITOXANTRONE TOP2A

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
9494516 9426516 18687447 10451375 11278845 11752352 9631585 11004693

Sources:
DrugBank TdgClinicalTrial NCI TEND GuideToPharmacology
IDARUBICIN TOP2A

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10523799 12034365 10203104 8036155 11752352 11836027

Sources:
DrugBank TdgClinicalTrial TEND
EPIRUBICIN TOP2A

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
14728934 17639997 16234514

Sources:
DrugBank TdgClinicalTrial TEND PharmGKB
IDRONOXIL TOP2A

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
DOXORUBICIN TOP2A

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name AEZS-108, AN-152

Novel drug target Established target

Trial Name MTC-DOX, MTC-doxorubicin

PMIDs:
21388138 26211460 22276998 20170164 17016621 17351394 17010609 17578914 11752352 17089011

Sources:
DTC DrugBank TdgClinicalTrial ClearityFoundationClinicalTrial TEND GuideToPharmacology
OFLOXACIN TOP2A

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
2847647

Sources:
DrugBank
FISETIN TOP2A

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8759170

Sources:
DTC
ETOPOSIDE PHOSPHATE TOP2A

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DAUNORUBICIN TOP2A

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name CPX-351, cytarabine + daunorubicin

PMIDs:
6380596 1963303 9494516 22260166

Sources:
DTC DrugBank TdgClinicalTrial NCI
DACTINOMYCIN TOP2A

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
7756657

Sources:
DrugBank
HYDROQUINONE TOP2A

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15833037

Sources:
NCI
DIGITOXIN TOP2A

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16309315

Sources:
DTC
ADRIAMYCIN TOP2A

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9494516

Sources:
NCI
ELLIPTECINE TOP2A

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18816045 19783445

Sources:
DTC
GENISTEIN TOP2A

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17016423 17139284 7769390

Sources:
DTC DrugBank
IDARUBICIN HYDROCHLORIDE TOP2A

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MYRICETIN TOP2A

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8759170 7769390

Sources:
DTC
CAMPTOTHECIN TOP2A

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11205246

Sources:
NCI
VINCRISTINE TOP2A

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9494516

Sources:
NCI
MITOXANTRONE HYDROCHLORIDE TOP2A

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DAUNORUBICIN HYDROCHLORIDE TOP2A

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DOXORUBICIN HYDROCHLORIDE TOP2A

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
QUERCETIN TOP2A

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8759170 7769390

Sources:
DTC
PACLITAXEL TOP2A

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name liposomal encapsulated paclitaxel (LEP)

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
FLUOROURACIL TOP2A

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

Ensembl: ENSG00000131747
- Version: 101_38
Alternate Names:

TOP2A Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
RussLampel: ENSG00000131747
- Version: 26-July-2011
Alternate Names:

Q71UN1_HUMAN Display Id

TOPOISOMERASE II ALPHA (FRAGMENT). [SOURCE:UNIPROT/SPTREMBL;ACC:Q71UQ5] Description

ENSG00000131747 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: P11388
- Version: 01-August-2011
Alternate Names:

P11388 Uniprot Accession

ENSG00000131747 Ensembl Gene Id

TOP2A_HUMAN Uniprot Id

Gene Info:

Target Subclass 5.99.1.3

Target Main Class Enzymes

Publications:
TdgClinicalTrial: P11388
- Version: January-2014
Alternate Names:

TOP2A Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:5.99.1.3

Publications:
HopkinsGroom: P11388
- Version: 11-September-2012
Alternate Names:

P11388 Uniprot Accession

7153 Entrez Gene Id

TOP2A Uniprot Gene Name

Gene Info:

Interpro Name DNA topoisomerase, type IIA

Interpro Type Domain

Interpro Short Name Topo_IIA

Gene Categories:

DRUGGABLE GENOME

Publications:
GuideToPharmacology: 7153
- Version: 29-September-2020
Alternate Names:

11989 HUGO Gene ID

11989 HUGO Gene Symbol

DNA topoisomerase II alpha HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name DNA topoisomerases

GuideToPharmacology Gene Category ID 851

Gene Categories:

ENZYME

Publications:

DrugBank: BE0000742

Version: 5.1.7

Alternate Names:

TOP2A DrugBank Gene Name

P11388 UniProt Accession

7153 Entrez Gene Id

Gene Info:

Publications:

Lee et al., 1992, Two independent amsacrine-resistant human myeloid leukemia cell lines share an identical point mutation in the 170 kDa form of human topoisomerase II., J. Mol. Biol.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Finlay et al., 1999, Inhibition of the action of the topoisomerase II poison amsacrine by simple aniline derivatives: evidence for drug-protein interactions., Oncol. Res.

DrugBank: BE0004951
- Version: 5.1.7
Alternate Names:

TOP2A DrugBank Gene Name

P11388 UniProt Accession

7153 Entrez Gene Id

Gene Info:

Publications:

Felix CA et al., 1995, ALL-1 gene rearrangements in DNA topoisomerase II inhibitor-related leukemia in children., Blood

NCI: TOP2A

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

McPherson et al., Selective sensitization of adriamycin-resistant P388 murine leukemia cells to antineoplastic agents following transfection with human DNA topoisomerase II alpha., Anticancer Res.

Renodon-Cornière et al., 2003, Analysis of bisdioxopiperazine dexrazoxane binding to human DNA topoisomerase II alpha: decreased binding as a mechanism of drug resistance., Biochemistry

Mueller et al., 2004, Amplification of the TOP2A gene does not predict high levels of topoisomerase II alpha protein in human breast tumor samples., Genes Chromosomes Cancer

DTC: TOP2A

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Schmidt EW et al., 1995, Makaluvamines H-M and damirone C from the pohnpeian sponge Zyzzya fuliginosa., J Nat Prod

Van Quaquebeke E et al., 2007, 2,2,2-Trichloro-N-({2-[2-(dimethylamino)ethyl]-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin- 5-yl}carbamoyl)acetamide (UNBS3157), a novel nonhematotoxic naphthalimide derivative with potent antitumor activity., J Med Chem

Diana P et al., 2007, 3,5-bis(3'-indolyl)pyrazoles, analogues of marine alkaloid nortopsentin: synthesis and antitumor properties., Bioorg Med Chem Lett

ChemblInteractions: TOP2
- Version: chembl_23
Alternate Names:

TOP2 GENE_SYMBOL

TOP2A GENE_SYMBOL

DNA topoisomerase 2-alpha UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000131747
- Version: 31-May-2017
Alternate Names:

ENSG00000131747 Gene Symbol

TOP2A Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
PharmGKB: TOP2A
- Version: 18-August-2020
Alternate Names:

PA354 PharmGKB ID

Gene Info:

Publications:
Pharos: TOP2A
- Version: 03-September-2020
Alternate Names:

DNA topoisomerase 2-alpha Gene Name

P11388 UniProt ID

Gene Info:

Gene Categories:

ENZYME

Publications:
Tempus: TOP2A
- Version: 11-November-2018
Alternate Names:

TOP2A Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
TTD: DNA topoisomerase II alpha
- Version: 2020.06.01
Alternate Names:

TOP2A TTD Gene Abbreviation

T17048 TTD Target ID

Gene Info:

Publications:
ClearityFoundationBiomarkers: TOP2A
- Version: 26-July-2013
Alternate Names:

Gene Info:

Publications:
CGI: TOP2A
- Version: 27-September-2017
Alternate Names:

Gene Info:

Publications:
ClearityFoundationClinicalTrial: TOP2A
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MskImpact: TOP2A
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Trial Name	amonafide,Quinamed
Novel drug target	Established target

Direct Interaction	yes
Mechanism of Interaction	DNA topoisomerase II alpha inhibitor

Trial Name	INNO-206
Novel drug target	Established target
Mechanism of Interaction	DNA topoisomerase II alpha inhibitor

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Trial Name	Voreloxin
Novel drug target	Established target
Mechanism of Interaction	DNA topoisomerase II inhibitor

Trial Name	becatecarin, XL 119, rebeccamycin
Novel drug target	Established target
Mechanism of Interaction	DNA topoisomerase II inhibitor

Trial Name	AEZS-108, AN-152
Novel drug target	Established target
Trial Name	MTC-DOX, MTC-doxorubicin

Trial Name	liposomal encapsulated paclitaxel (LEP)
Novel drug target	Established target

Q71UN1_HUMAN	Display Id
TOPOISOMERASE II ALPHA (FRAGMENT). [SOURCE:UNIPROT/SPTREMBL;ACC:Q71UQ5]	Description
ENSG00000131747	Ensembl Gene Id

P11388	Uniprot Accession
ENSG00000131747	Ensembl Gene Id
TOP2A_HUMAN	Uniprot Id

11989	HUGO Gene ID
11989	HUGO Gene Symbol
DNA topoisomerase II alpha	HUGO Gene Name

TOP2A	DrugBank Gene Name
P11388	UniProt Accession
7153	Entrez Gene Id

TOP2	GENE_SYMBOL
TOP2A	GENE_SYMBOL
DNA topoisomerase 2-alpha	UNIPROT

TOP2A Gene Record

TOP2A 7153 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Trial Name amonafide,Quinamed Novel drug target Established target

PMIDs: 26211460 23353750 20170164 24054489 17658777

Sources: DTC DrugBank TdgClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction DNA topoisomerase II alpha inhibitor

PMIDs: 17628745

Sources: DrugBank ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19783445

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19783445

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22014547

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21391686

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11754608

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20006518

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24931277

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19783445

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24326278

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21761866

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: Trial Name GPX-100 Novel drug target Established target

PMIDs: None found

Sources: DrugBank TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19783445

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19783445

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8691207

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22276998

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 25808831

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name amonafide,Quinamed

Novel drug target Established target

PMIDs:
26211460 23353750 20170164 24054489 17658777

Sources:
DTC DrugBank TdgClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

PMIDs:
17628745

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
19783445

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19783445

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22014547

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
21391686

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
11754608

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20006518

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24931277

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19783445

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24326278

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
21761866

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name GPX-100

Novel drug target Established target

PMIDs:
None found

Sources:
DrugBank TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
19783445

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19783445

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
8691207

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22276998

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
25808831

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
20561793

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
11752352

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name INNO-206

Novel drug target Established target

Mechanism of Interaction DNA topoisomerase II alpha inhibitor

PMIDs:
25312684

Sources:
DrugBank TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
8691207

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19783445

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19783445

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19783445

Sources:
DTC

Interaction Types & Directionality:

n/a