DGIdb - TOP1 Gene Record

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:

Direct Interaction	yes
Mechanism of Interaction	DNA topoisomerase I inhibitor

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

Trial Name	topotecan,Hycamtin
Novel drug target	Established target

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

Trial Name	Karenitecin, BNP 1350
Novel drug target	Established target

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

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

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

TOP1	GENE_SYMBOL
DNA topoisomerase 1	UNIPROT
DNA topoisomerase I	UNIPROT

TOP1 Gene Record

TOP1 7150 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22329436 21823606 20155916 24502276

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15929804 17325867

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19203291

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22503207

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20371180

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20942490

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18951805

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24094433

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20630766

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20371180

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20371180

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20371180

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24069881

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20371180

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20371180

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20371180

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19203291

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20373766

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
22329436 21823606 20155916 24502276

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
15929804 17325867

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
19203291

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22503207

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20942490

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
18951805

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24094433

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20630766

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24069881

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19203291

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20373766

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
21333532

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
21807514

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19203291

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19535252

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20371180