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TOP1 Gene Record

  • Summary
  • Interactions
  • Claims
  • TOP1 7150 Druggable GenomeClinically Actionable

    Alternate Names:

    7150
    DNA TOPOISOMERASE I
    TOP1
    TOPI
    126420
    11986
    ENSG00000198900
    OTTHUMG00000033057
    DNA topoisomerase 1
    PA353
    5845
    P11387
    TOP1_HUMAN
    DNA TOPOISOMERASE I (EC 5.99.1.2). [SOURCE:UNIPROT/SWISSPROT;ACC:P11387]
    T09826

    Gene Info:

    Target Subclass 5.99.1.2
    Target Main Class Enzymes
    Human Readable Name DRUGGABLE GENOME
    Target Class Enzymes
    Target Subclass EC:5.99.1.2
    Interpro Name DNA topoisomerase I
    Uniprot Status Swiss-Prot
    Uniprot Evidence 1: Evidence at protein level
    Interpro Short Name TopoI
    Interpro Type Family
    Interpro Acc IPR001631
    Gene Biotype PROTEIN_CODING
    (18 More Sources)

    Gene Categories: Category Details

    SERINE THREONINE KINASE
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE
    ENZYME

    Publications:

    Khan QA et al., 2009, Calothrixins, a new class of human DNA topoisomerase I poisons., J Nat Prod
    Clericuzio M et al., 2006, Cucurbitane triterpenes from the fruiting bodies and cultivated mycelia of Leucopaxillus gentianeus., J Nat Prod
    Wang L et al., 2015, Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents., Bioorg Med Chem
    Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett
    Cananzi S et al., 2011, Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D., Bioorg Med Chem
    Luo Y et al., 2012, Synthesis and biological evaluation of new homocamptothecin analogs., Eur J Med Chem
    Parrino B et al., 2015, Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action., Eur J Med Chem
    Samorì C et al., 2009, Semisynthesis, biological activity, and molecular modeling studies of C-ring-modified camptothecins., J 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
    Masurier N et al., 2012, Imidazonaphthyridine systems (part 2): Functionalization of the phenyl ring linked to the pyridine pharmacophore and its replacement by a pyridinone ring produces intriguing differences in cytocidal activity., Eur J Med Chem
    Oppegard LM et al., 2012, Inhibition of human topoisomerases I and II by simocyclinone D8., J Nat Prod
    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
    Gálvez-Peralta M et al., 2009, On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents., Bioorg Med Chem Lett
    Kiselev E et al., 2014, Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells., J Med Chem
    Kollmannsberger et al., 1999, Topotecan - A novel topoisomerase I inhibitor: pharmacology and clinical experience., Oncology
    Dennis et al., 1997, An overview of the clinical pharmacology of topotecan., Semin. Oncol.
    Schmidt et al., 2001, Glioma cell sensitivity to topotecan: the role of p53 and topotecan-induced DNA damage., Eur. J. Pharmacol.
    strel'tsov et al., [Interaction of topotecan--a DNA topoisomerase I inhibitor--with dual-stranded polydeoxyribonucleotides. II. Formation of a complex containing several DNA molecules in the presence of topotecan]., Mol. Biol. (Mosk.)
    Aisner et al., 2003, Sequencing topotecan and etoposide plus cisplatin to overcome topoisomerase I and II resistance: a pharmacodynamically based Phase I trial., Clin. Cancer Res.
    Zhang et al., 2002, [Preliminary study of apoptosis of human hepatocarcinoma cell line HepG2 induced by topotecan]., Ai Zheng
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Herben et al., 1996, Clinical pharmacokinetics of topotecan., Clin Pharmacokinet
    Streltsov, 2002, Action models for the antitumor drug camptothecin: formation of alkali-labile complex with DNA and inhibition of human DNA topoisomerase I., J. Biomol. Struct. Dyn.
    Cinelli MA et al., 2010, The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode., Bioorg Med Chem
    Fehér D et al., 2008, A 2-substituted prodiginine, 2-(p-hydroxybenzyl)prodigiosin, from Pseudoalteromonas rubra., J Nat Prod
    Zahir A et al., 1996, DNA topoisomerase I inhibitors: cytotoxic flavones from Lethedon tannaensis., J Nat Prod
    Carballeira NM et al., 2002, Total synthesis and biological evaluation of (5Z,9Z)-5,9-hexadecadienoic acid, an inhibitor of human topoisomerase I., J Nat Prod
    Kostopoulos et al., 2009, Topoisomerase I but not thymidylate synthase is associated with improved outcome in patients with resected colorectal cancer treated with irinotecan containing adjuvant chemotherapy., BMC Cancer
    Yoshikawa et al., 2004, Novel camptothecin analogues that circumvent ABCG2-associated drug resistance in human tumor cells., Int. J. Cancer
    Nakagawa et al., 2006, Molecular modeling of new camptothecin analogues to circumvent ABCG2-mediated drug resistance in cancer., Cancer Lett.
    Ramesh et al., 2010, Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives., Biomed. Chromatogr.
    Ishikawa et al., 2006, Transport mechanism-based drug molecular design: novel camptothecin analogues to circumvent ABCG2-associated drug resistance of human tumor cells., Curr. Pharm. Des.
    Yang et al., 2005, Novel agents that potentially inhibit irinotecan-induced diarrhea., Curr. Med. Chem.
    Yoshikawa et al., 2004, Transport of SN-38 by the wild type of human ABC transporter ABCG2 and its inhibition by quercetin, a natural flavonoid., J. Exp. Ther. Oncol.
    Chabot, 1997, Clinical pharmacokinetics of irinotecan., Clin Pharmacokinet
    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
    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
    Hoskins JM et al., 2008, Irinotecan pharmacogenetics: influence of pharmacodynamic genes., Clin Cancer Res
    Slingerland M et al., 2012, The fate of camptothecin glycoconjugate: report of a clinical hold during a phase II study of BAY 56-3722 (formerly BAY 38-3441), in patients with recurrent or metastatic colorectal cancer resistant/refractory to irinotecan., Invest New Drugs
    Miao Z et al., 2013, A new strategy to improve the metabolic stability of lactone: discovery of (20S,21S)-21-fluorocamptothecins as novel, hydrolytically stable topoisomerase I inhibitors., J Med Chem
    Wu WB et al., 2011, Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors., Eur J Med Chem
    Tohda et al., 1992, A possible involvement of DNA topoisomerase I in "caffeine effect" after ultraviolet irradiation., Tohoku J. Exp. Med.
    Wang P et al., 2010, Cytotoxicity and inhibition of DNA topoisomerase I of polyhydroxylated triterpenoids and triterpenoid glycosides., Bioorg Med Chem Lett
    Dong G et al., 2010, Selection of evodiamine as a novel topoisomerase I inhibitor by structure-based virtual screening and hit optimization of evodiamine derivatives as antitumor agents., J Med Chem
    Kamal A et al., 2013, 4β-[4'-(1-(Aryl)ureido)benzamide]podophyllotoxins as DNA topoisomerase I and IIα inhibitors and apoptosis inducing agents., Bioorg Med Chem
    Shchekotikhin AE et al., 2014, Synthesis and evaluation of new antitumor 3-aminomethyl-4,11-dihydroxynaphtho[2,3-f]indole-5,10-diones., Eur J Med Chem
    Song Y et al., 2010, Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors., J Med Chem
    Khadka DB et al., 2011, 3-Arylisoquinolines as novel topoisomerase I inhibitors., Bioorg Med Chem
    D'yakonov VA et al., 2015, Stereoselective synthesis of 11-phenylundeca-5Z,9Z-dienoic acid and investigation of its human topoisomerase I and IIα inhibitory activity., Bioorg Med Chem Lett
    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
    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
    Verones V et al., 2013, Synthesis, antiproliferative activity and tubulin targeting effect of acridinone and dioxophenothiazine derivatives., Eur J Med Chem
    Racané L et al., 2013, New anticancer active and selective phenylene-bisbenzothiazoles: synthesis, antiproliferative evaluation and DNA binding., Eur J Med Chem
    Parrino B et al., 2014, 11H-Pyrido[3',2':4,5]pyrrolo[3,2-c]cinnoline and pyrido[3',2':4,5]pyrrolo[1,2-c][1,2,3]benzotriazine: two new ring systems with antitumor activity., J Med Chem
    Fan Y et al., 1998, Molecular modeling studies of the DNA-topoisomerase I ternary cleavable complex with camptothecin., J Med Chem
    Shchekotikhin AE et al., 2007, Naphthoindole-based analogues of tryptophan and tryptamine: synthesis and cytotoxic properties., Bioorg Med Chem
    Bar FM et al., 2009, Rational design and semisynthesis of betulinic acid analogues as potent topoisomerase inhibitors., J Nat Prod
    Christodoulou MS et al., 2013, Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase I and sirtuins., 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
    You QD et al., 2009, Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification., J Med Chem
    Nagarajan M et al., 2004, Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings., J 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
    Kiselev E et al., 2012, Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships., J Med Chem
    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
    Van HT et al., 2007, Convenient synthesis of indeno[1,2-c]isoquinolines as constrained forms of 3-arylisoquinolines and docking study of a topoisomerase I inhibitor into DNA-topoisomerase I complex., Bioorg Med Chem Lett
    He S et al., 2015, Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors., ACS Med Chem Lett
    Cinelli MA et al., 2009, Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships., Bioorg Med Chem
    Majumdar P et al., 2015, Design, synthesis and evaluation of thiohydantoin derivatives as potent topoisomerase I (Top1) inhibitors with anticancer activity., Eur J Med Chem
    Lee CC et al., 2013, Design, synthesis and antiproliferative evaluation of fluorenone analogs with DNA topoisomerase I inhibitory properties., Bioorg Med Chem
    Santos RC et al., 2010, Synthesis and structure-activity relationship study of novel cytotoxic carbamate and N-acylheterocyclic bearing derivatives of betulin and betulinic acid., Bioorg Med Chem
    Hecht SM et al., 1992, A strategy for identifying novel, mechanistically unique inhibitors of topoisomerase I., J Nat Prod
    Zhou BN et al., 2000, Use of COMPARE analysis to discover new natural product drugs: isolation of camptothecin and 9-methoxycamptothecin from a new source., J Nat Prod
    Kashyap M et al., 2013, Indenoindolone derivatives as topoisomerase II-inhibiting anticancer agents., Bioorg Med Chem Lett
    Wang L et al., 2014, Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs., Bioorg Med Chem Lett
    Beck DE et al., 2015, Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore., J Med Chem
    Taliani S et al., 2013, Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors., J Med Chem
    Di Salvo A et al., 2013, Synthesis, cytotoxicity and DNA binding of oxoazabenzo[de]anthracenes derivatives in colon cancer Caco-2 cells., Eur J Med Chem
    Kiselev E et al., 2011, 7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents., J Med Chem
    Chen CL et al., 2014, Ring fusion strategy for the synthesis of anthra[2,3-d]oxazole-2-thione-5,10-dione homologues as DNA topoisomerase inhibitors and as antitumor agents., Eur J Med Chem
    Sović I et al., 2014, Novel phenyl and pyridyl substituted derivatives of isoindolines: Synthesis, antitumor activity and DNA binding features., Eur J Med Chem
    Baviskar AT et al., 2013, Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity., Bioorg Med Chem
    Teicher, 2008, Next generation topoisomerase I inhibitors: Rationale and biomarker strategies., Biochem. Pharmacol.
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    van der Merwe et al., 2008, Mutation of Gly721 alters DNA topoisomerase I active site architecture and sensitivity to camptothecin., J. Biol. Chem.
    Saif et al., 2005, Edotecarin: a novel topoisomerase I inhibitor., Clin Colorectal Cancer
    Carvajal et al., 2007, Possible role of edotecarin, a novel topoisomerase I inhibitor, in therapy-related myelodysplastic syndrome., Leuk. Lymphoma
    Jiao Y et al., 2011, Synthesis and antitumor activity of 10-arylcamptothecin derivatives., Bioorg Med Chem Lett
    Shi W et al., 2011, Cytotoxicity and topoisomerase I/II inhibition of glycosylated 2-phenyl-indoles, 2-phenyl-benzo[b]thiophenes and 2-phenyl-benzo[b]furans., Bioorg Med Chem
    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
    Bandekar PP et al., 2010, Antimicrobial activity of tryptanthrins in Escherichia coli., J Med Chem
    Bolognese A et al., 2008, Antitumor agents 6. Synthesis, structure-activity relationships, and biological evaluation of spiro[imidazolidine-4,3'-thieno[2,3-g]quinoline]-tetraones and spiro[thieno[2,3-g]quinoline-3,5'-[1,2,4]triazinane]-tetraones with potent antiproliferative activity., J Med Chem
    Chedid S et al., 2006, Minimal clinical benefit of single agent Orathecin (Rubitecan) in heavily pretreated metastatic breast cancer., Cancer Chemother Pharmacol
    Tevyashova AN et al., 2009, Reaction of the antitumor antibiotic olivomycin I with aryl diazonium salts. Synthesis, cytotoxic and antiretroviral potency of 5-aryldiazenyl-6-O-deglycosyl derivatives of olivomycin I., Bioorg Med Chem
    Li X et al., 2011, Synthesis, structure-activity relationship and biological evaluation of anticancer activity for novel N-substituted sophoridinic acid derivatives., 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
    Tan H et al., 2015, Synthesis of novel 10-hydroxycamptothecin derivatives utilizing topotecan hydrochloride as ortho-quinonemethide precursor., Bioorg Med Chem
    Díaz-Carballo D et al., 2008, The contribution of plukenetione A to the anti-tumoral activity of Cuban propolis., Bioorg Med Chem
    López-Lázaro M et al., 2007, Curcumin induces high levels of topoisomerase I- and II-DNA complexes in K562 leukemia cells., J Nat Prod
    Kotoh et al., 1994, Increased expression of DNA topoisomerase I gene and collateral sensitivity to camptothecin in human cisplatin-resistant bladder cancer cells., Cancer Res.
    Baechler SA et al., 2013, Synthesis, topoisomerase-targeting activity and growth inhibition of lycobetaine analogs., Bioorg Med Chem
    van der Zee et al., 1991, P-glycoprotein expression and DNA topoisomerase I and II activity in benign tumors of the ovary and in malignant tumors of the ovary, before and after platinum/cyclophosphamide chemotherapy., Cancer Res.
  • CHEMBL79513   TOP1

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22329436 21823606 20155916 24502276


    Sources:
    DTC

  • EDOTECARIN   TOP1

    Interaction Score: 1.95

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15929804 17325867


    Sources:
    TTD

  • N-METHYLCALOTHRIXIN B   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19203291


    Sources:
    DTC

  • BROMOETHANE   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22503207


    Sources:
    DTC

  • AESCULIOSIDE IIID   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • CHEMBL1277315   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20942490


    Sources:
    DTC

  • PLUKENETIONE A   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18951805


    Sources:
    DTC

  • CHEMBL494283   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24094433


    Sources:
    DTC

  • INDOTECAN   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20630766


    Sources:
    DTC

  • AESCULIOSIDE IVC   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • AESCULIOSIDE IVB   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • AESCULIOSIDE IIB   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • (20S,21R)-FLUOROCAMPTOTHECIN   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24069881


    Sources:
    DTC

  • AESCULIOSIDE IIIB   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • AESCULIOSIDE IIIF   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • AESCULIOSIDE IIK   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • CALOTHRIXIN B   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19203291


    Sources:
    DTC

  • CHEMBL308106   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20373766


    Sources:
    DTC

  • CHEMBL1762593   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21333532


    Sources:
    DTC

  • SOPHORIDINE   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21807514


    Sources:
    DTC

  • AESCULIOSIDE IIIA   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • CALOTHRIXIN A   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19203291


    Sources:
    DTC

  • OLIVOMYCIN I   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19535252


    Sources:
    DTC

  • AESCULIOSIDE IIE   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • AESCULIOSIDE IIC   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • CHEMBL1094358   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • AESCULIOSIDE IID   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • CHEMBL2171803   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • CHEMBL2171795   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • NITIDINE CHLORIDE   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21435753


    Sources:
    DTC

  • LAMELLARIN D   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21783369


    Sources:
    DTC

  • CHEMBL2171778   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • AESCULIOSIDE IIIC   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • AESCULIOSIDE IIA   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • AESCULIOSIDE IIIE   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • CHEMBL1094674   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • CHEMBL2171807   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • AESCULIOSIDE IVA   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • CHEMBL1762594   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21333532


    Sources:
    DTC

  • CHEMBL2171782   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • (20S,21S)-FLUOROCAMPTOTHECIN   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24069881


    Sources:
    DTC

  • CHEMBL578220   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18922034


    Sources:
    DTC

  • CHEMBL1094675   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20371180


    Sources:
    DTC

  • ETIRINOTECAN PEGOL   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction DNA topoisomerase I inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions MyCancerGenomeClinicalTrial

  • MANSONONE F   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21600681


    Sources:
    DTC

  • CHEMBL2171793   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • (20S,21S)-7-CYCLOHEXYLFLUOROCAMPTOTHECIN   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24069881


    Sources:
    DTC

  • AFELETECAN   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21547368


    Sources:
    TTD

  • CHEMBL464637   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12444712


    Sources:
    DTC

  • INDIMITECAN   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20630766


    Sources:
    DTC

  • CHEMBL455004   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22503207


    Sources:
    DTC

  • O-METHYLCALOTHRIXIN A   TOP1

    Interaction Score: 1.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19203291


    Sources:
    DTC

  • RUBITECAN   TOP1

    Interaction Score: 0.98

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name rubitecan, RF-2000,Orathecin
    Novel drug target Established target

    PMIDs:
    16193332


    Sources:
    TdgClinicalTrial TTD

  • EVODIAMINE   TOP1

    Interaction Score: 0.98

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019 24103429


    Sources:
    DTC

  • CAMPTOTHECIN   TOP1

    Interaction Score: 0.98

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name XMT-1001
    Novel drug target Established target

    PMIDs:
    20942490 23849207 25244612 20155916 21600681 21095131 25913198 25799376 19386396 23202849 23603616 25003995 25317694 9632354 22867097 22647222 24502276 20630766 17276690 19691293 24103429 25626146 19715319 15509164 21388138 22329436 26216018 17827007 25815139 19783447 26312433 24094433 20494586 1324981 11000035 22867019 23321564 22503207 24529870 25909279 23987476 24099994 21823606 25240093 25282261 23920485 18061144 10592235 18056711 11752352


    Sources:
    DTC TdgClinicalTrial ClearityFoundationClinicalTrial TTD

  • HYDROXYCAMPTOTHECIN   TOP1

    Interaction Score: 0.87

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22647222 24012683 25481395


    Sources:
    DTC

  • TOPOTECAN   TOP1

    Interaction Score: 0.74

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name topotecan,Hycamtin
    Novel drug target Established target

    PMIDs:
    19501511 24502276 9885371 9122737 11166732 11443926 12855624 12520736 11752352 8853931 12437383


    Sources:
    DTC ClearityFoundationBiomarkers TdgClinicalTrial ClearityFoundationClinicalTrial TEND TTD

  • CHEMBL2171794   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • PEGAMOTECAN   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • DIFLOMOTECAN   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LURTOTECAN   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Liposomal lurtotecan, OSI-211
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • PEN-866   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • EXATECAN   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • AR-67   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CHEMBL2171781   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • IRINOTECAN SUCROSOFATE   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction DNA topoisomerase I inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • NAMITECAN   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • INTOPLICINE   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PYRAZOLOACRIDINE   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19501511


    Sources:
    DTC

  • KARENITECIN   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Karenitecin, BNP 1350
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD

  • GIMATECAN   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PRODIGIOSIN   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18922034


    Sources:
    DTC

  • CHEMBL2171812   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867019


    Sources:
    DTC

  • SIMOCYCLINONE D8   TOP1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22867097


    Sources:
    DTC

  • LYCOBETAINE   TOP1

    Interaction Score: 0.43

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23266176


    Sources:
    DTC

  • TAFLUPOSIDE   TOP1

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • TRYPTANTHRIN   TOP1

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20373766


    Sources:
    DTC

  • IRINOTECAN   TOP1

    Interaction Score: 0.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name CPX-1
    Novel drug target Established target
    Trial Name irinotecan hydrochloride injection,Camptosar

    PMIDs:
    19775480 15170677 16309825 19852077 16454746 15975002 15255290 9342501 11752352 25003995 24507920 23360284 18347181


    Sources:
    DTC ClearityFoundationBiomarkers TdgClinicalTrial ClearityFoundationClinicalTrial TEND CIViC MyCancerGenomeClinicalTrial PharmGKB TTD

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   TOP1

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17190463 25835359 23622981 21783369 22647222 25768699 19530720 25003995


    Sources:
    DTC PharmGKB TTD

  • DANIQUIDONE   TOP1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CUCURBITACIN B   TOP1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17190463


    Sources:
    DTC

  • IRINOTECAN HYDROCHLORIDE HYDRATE   TOP1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction DNA topoisomerase I inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BECATECARIN   TOP1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction DNA topoisomerase I inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • C-1311   TOP1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name C-1311, XLS-002,Symadex
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • FISETIN   TOP1

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8759170


    Sources:
    DTC

  • 9-AMINOCAMPTOTHECIN   TOP1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LAPACHONE   TOP1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Established target
    Trial Name ARQ-501

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD

  • CAFFEINE   TOP1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1339096


    Sources:
    NCI

  • MYRICETIN   TOP1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8759170


    Sources:
    DTC

  • DOXORUBICIN   TOP1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21094049 17276690 19053767


    Sources:
    DTC

  • DAUNORUBICIN   TOP1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21094049


    Sources:
    DTC

  • CURCUMIN   TOP1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18076140


    Sources:
    DTC

  • CYCLOPHOSPHAMIDE   TOP1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1682037


    Sources:
    NCI

  • QUERCETIN   TOP1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8759170


    Sources:
    DTC

  • CISPLATIN   TOP1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8205547


    Sources:
    NCI

  • Ensembl: ENSG00000198900

    • Version: 101_38

    Alternate Names:
    TOP1 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • RussLampel: ENSG00000198900

    • Version: 26-July-2011

    Alternate Names:
    DNA TOPOISOMERASE I (EC 5.99.1.2). [SOURCE:UNIPROT/SWISSPROT;ACC:P11387] Description
    ENSG00000198900 Ensembl Gene Id
    TOP1 Display Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P11387

    • Version: January-2014

    Alternate Names:
    TOP1 Gene Symbol

    Gene Info:
    Target Class Enzymes
    Target Subclass EC:5.99.1.2

    Publications:

  • HopkinsGroom: P11387

    • Version: 11-September-2012

    Alternate Names:
    7150 Entrez Gene Id
    TOP1_HUMAN Uniprot Id
    TOP1 Uniprot Gene Name

    Gene Info:
    Interpro Name DNA topoisomerase I
    Uniprot Status Swiss-Prot
    Uniprot Evidence 1: Evidence at protein level

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TEND: P11387

    • Version: 01-August-2011

    Alternate Names:
    TOP1 Gene Symbol
    TOP1_HUMAN Uniprot Id
    P11387 Uniprot Accession

    Gene Info:
    Target Subclass 5.99.1.2
    Target Main Class Enzymes

    Publications:

  • PharmGKB: TOP1

    • Version: 18-August-2020

    Alternate Names:
    PA353 PharmGKB ID

    Gene Info:

    Publications:
    Hoskins JM et al., 2008, Irinotecan pharmacogenetics: influence of pharmacodynamic genes., Clin Cancer Res

  • CIViC: TOP1

    • Version: 14-September-2020

    Alternate Names:
    7150 Entrez Gene ID
    5845 CIViC Gene ID

    Gene Info:

    Publications:
    Kostopoulos et al., 2009, Topoisomerase I but not thymidylate synthase is associated with improved outcome in patients with resected colorectal cancer treated with irinotecan containing adjuvant chemotherapy., BMC Cancer

  • TTD: DNA topoisomerase I

    • Version: 2020.06.01

    Alternate Names:
    TOP1 TTD Gene Abbreviation
    T09826 TTD Target ID

    Gene Info:

    Publications:
    Slingerland M et al., 2012, The fate of camptothecin glycoconjugate: report of a clinical hold during a phase II study of BAY 56-3722 (formerly BAY 38-3441), in patients with recurrent or metastatic colorectal cancer resistant/refractory to irinotecan., Invest New Drugs

  • NCI: TOP1

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Kotoh et al., 1994, Increased expression of DNA topoisomerase I gene and collateral sensitivity to camptothecin in human cisplatin-resistant bladder cancer cells., Cancer Res.
    Fostel et al., 1996, Comparison of responses of DNA topoisomerase I from Candida albicans and human cells to four new agents which stimulate topoisomerase-dependent DNA nicking., FEMS Microbiol. Lett.
    Tan et al., 1989, Nonproductive rearrangement of DNA topoisomerase I and II genes: correlation with resistance to topoisomerase inhibitors., J. Natl. Cancer Inst.

  • DTC: TOP1

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Khan QA et al., 2009, Calothrixins, a new class of human DNA topoisomerase I poisons., J Nat Prod
    Oppegard LM et al., 2012, Inhibition of human topoisomerases I and II by simocyclinone D8., J Nat Prod
    Zahir A et al., 1996, DNA topoisomerase I inhibitors: cytotoxic flavones from Lethedon tannaensis., J Nat Prod

  • ChemblInteractions: TOP1

    • Version: chembl_23

    Alternate Names:
    TOP1 GENE_SYMBOL
    DNA topoisomerase 1 UNIPROT
    DNA topoisomerase I UNIPROT

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000198900

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000198900 Gene Symbol
    TOP1 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • Tempus: TOP1

    • Version: 11-November-2018

    Alternate Names:
    TOP1 Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • Pharos: TOP1

    • Version: 01-February-2022

    Alternate Names:
    DNA topoisomerase 1 Gene Name
    P11387 UniProt ID

    Gene Info:

    Gene Categories:
    ENZYME

    Publications:

  • MskImpact: TOP1

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • MyCancerGenomeClinicalTrial: TOP1

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • ClearityFoundationBiomarkers: TOP1

    • Version: 26-July-2013

    Alternate Names:

    Gene Info:

    Publications:

  • ClearityFoundationClinicalTrial: TOP1

    • Version: 15-June-2013

    Alternate Names:

    Gene Info:

    Publications:

  • FoundationOneGenes: TOP1

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: TOP1

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • GO: TOP1

    • Version: 01-February-2022

    Alternate Names:

    Gene Info:

    Gene Categories:
    SERINE THREONINE KINASE

    Publications:

  • Oncomine: TOP1

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21