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DNA Topoisomerases, Type I

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Definition: DNA TOPOISOMERASES that catalyze ATP-independent breakage of one of the two strands of DNA, passage of the unbroken strand through the break, and rejoining of the broken strand. DNA Topoisomerases, Type I enzymes reduce the topological stress in the DNA structure by relaxing the superhelical turns and knotted rings in the DNA helix.  do not confuse entry term DNA UNTWISTING PROTEIN with DNA UNWINDING PROTEINS see DNA HELICASES; coordinate with BACTERIAL PROTEINS or ARCHAEAL PROTEINS if pertinent    Other names DNA Untwisting Protein; DNA Untwisting Enzyme; DNA Topoisomerase I; DNA Topoisomerase; DNA Relaxing Protein; DNA Relaxing Enzyme; DNA Nicking-Closing Protein; Type I DNA Topoisomerase; Topoisomerase I; DNA Untwisting Proteins; DNA Untwisting Enzymes; DNA Type 1 Topoisomerase; DNA Relaxing Enzymes; DNA Nicking-Closing Proteins
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
cyclohexyl(2-phenylquinazolin-4-yl)amine  0   *Cyclohexylamines *Quinazolines DNA Topoisomerases, Type I Topoisomerase I Inhibitors. Bioorg Med Chem. 2011 Jul 15;19(14):4399-404.
12,13-dihydro-N-methyl-6,11,13-trioxo-5H-benzo(4,5)cyclohepta(1,2-b)naphthalen-5,12-imine  0   *Naphthoquinones DNA Topoisomerases, Type II DNA Topoisomerases, Type I Topoisomerase Inhibitors. Biochem Biophys Res Commun 2011 Apr 29;408(1):94-8
5-piperazin-1-ylindeno(1,2-c)isoquinolin-11-one  0   *Isoquinolines *Piperazines DNA Topoisomerases, Type I. Bioorg Med Chem 2011 Mar 15;19(6):1924-9
7-butyl-10-amino-camptothecin-beta-alanine-lysine  0   *Dipeptides Camptothecin/*analogs & derivatives DNA Topoisomerases, Type I. Cancer Chemother Pharmacol 2011 Apr;67(4):855-65
7-butyl-10-amino-camptothecin  0   Camptothecin/*analogs & derivatives DNA Topoisomerases, Type I. Cancer Chemother Pharmacol 2011 Apr;67(4):855-65
ethyl 7-fluoro-5,12-dioxo-5,12-dihydroindolizino(2,3-g)quinoline-6-carboxylate  0   *Indolizines *Quinolones DNA Topoisomerases, Type I. Biochemistry 2010 Nov 30;49(47):10131-6
docosyl 4-coumarate  0   *Coumaric Acids DNA Topoisomerases, Type I. Int J Oncol 2010 oct;37(4):993-1000
NSC 724998  0   *Isoquinolines *Benzodioxoles DNA Topoisomerases, Type I. Cancer Res 2007 Nov 1;67(21):10397-405
2-hydroxy-28-(1H-triazol-1-yl)-lup-1,20(29)-dien-3,28-dione  0   *Triazoles *Triterpenes DNA Topoisomerases, Type I. Bioorg Med Chem 2010 Jun 15;18(12):4385-96
28-(1H-triazol-1-yl)-28-oxo-lup-20(29)-en-3-yl-1H-triazole-1-carboxylate  0   *Triazoles *Triterpenes DNA Topoisomerases, Type I. Bioorg Med Chem 2010 Jun 15;18(12):4385-96
NSC 725776  0   *Isoquinolines *Benzodioxoles DNA Topoisomerases, Type I. J Pharm Biomed Anal 2010 Sep 5;52(5):714-20
NSC 743400  0   *Isoquinolines *Benzodioxoles DNA Topoisomerases, Type I. J Pharm Biomed Anal 2010 Sep 5;52(5):714-20
7-tert-butyldimethylsilyl-10-hydroxyhomocamptothecin  0   Camptothecin/*analogs & derivatives DNA Topoisomerases, Type I/antagonists & inhibitors. Pharmacol Res 2010 Feb;61(2):108-15
3-O-(N-(phenylsulfonyl)carbamoyl-17beta-N-(phenylsulfonyl)amide)betulinic acid  0   *Triterpenes DNA Topoisomerases, Type I/antagonists & inhibitors. J Nat Prod. 2009 Sep;72(9):1643-50
CPUY013 compound  0   *Oxazoles *Fluoroquinolones DNA Topoisomerases, Type I/antagonists & inhibitors. Yao Xue Xue Bao 2008 Aug;43(8):811-8
4,11-dimethoxynaphtho(2,3-f)indole-5,10-dione  0   *Anthraquinones *Pyrroles DNA Topoisomerases, Type I/antagonists & inhibitors. Bull Exp Biol Med 2008 Mar;145(3):334-7
isocamptothecin B  0   Camptothecin/*analogs & derivatives DNA Topoisomerases, Type I/antagonists & inhibitors. Exp Dermatol 2008 Jun;17(6):530-6
isocamptothecin A  0   Camptothecin/*analogs & derivatives DNA Topoisomerases, Type I/antagonists & inhibitors. Exp Dermatol 2008 Jun;17(6):530-6
TOP1 protein, human  EC 5.99.1.2   *DNA Topoisomerases, Type I. Nucleic Acids Res 2008 Apr;36(7):2301-10
Bin4 protein, Arabidopsis  EC 5.99.-   *DNA Topoisomerases, Type I *Arabidopsis Proteins Protein Subunits. Plant Cell 2007 Nov;19(11):3655-68
S 38809  0   *Dioxoles Camptothecin/*analogs & derivatives DNA Topoisomerases, Type I/antagonists & inhibitors. Mol Pharmacol 2007 Aug;72(2):311-9
lysyl-cysteinyl-cysteinyl-arginyl-cysteinyl-lysine  0   *Oligopeptides DNA Topoisomerases, Type I/antagonists & inhibitors. J Mol Biol 2006 Nov 10;363(5):891-907
tryptophyl-tyrosyl-cysteinyl-arginyl-cysteinyl-lysine  0   *Oligopeptides DNA Topoisomerases, Type I/antagonists & inhibitors. J Mol Biol 2006 Nov 10;363(5):891-907
bis-1,3-((5,6-dihydro-5,11-diketo-11H-indeno(1,2-c)isoquinoline)-6-propylamino)propane  0   *Indenes *Isoquinolines DNA Topoisomerases, Type I/antagonists & inhibitors. Mol Pharmacol 2006 Sep;70(3):1109-20
norindenoisoquinoline  0   *Indenes *Isoquinolines DNA Topoisomerases, Type I/antagonists & inhibitors. Mol Cancer ther 2006 Feb;5(2):287-95
leptosin F  0   *Indole Alkaloids DNA Topoisomerases, Type II/antagonists & inhibitors DNA Topoisomerases, Type I/antagonists & inhibitors. Cancer Sci 2005 Nov;96(11):816-24
leptosin C  0   *Indole Alkaloids DNA Topoisomerases, Type I/antagonists & inhibitors. Cancer Sci 2005 Nov;96(11):816-24
2,3-dimethoxy-8,9-methylenedioxy-11H-indeno(1,2-c)isoquinoline  0   *Isoquinolines DNA Topoisomerases, Type I/antagonists & inhibitors. J Med Chem 2005 Jul 28;48(15):4803-14
kalihinol F  0   *Diterpenes *Nitriles DNA Topoisomerases, Type I/antagonists & inhibitors. Biosci Biotechnol Biochem 2003 Nov;67(11):2365-72
2,5-bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone  0   *Benzylidene Compounds *Pentanones DNA Topoisomerases, Type I/antagonists & inhibitors. Biochem Pharmacol 2004 Jul 15;68(2):293-303
ardisin  72629-62-0   *Resorcinols DNA Topoisomerases, Type II/antagonists & inhibitors DNA Topoisomerases, Type I/antagonists & inhibitors. Food Chem Toxicol 2003 Nov;41(11):1527-35
DNA topoisomerase IB, Trypanosoma brucei  EC 5.99.1.-   *DNA Topoisomerases, Type I. Proc Natl Acad Sci U S A 2003 Jun 24;100(13):7539-44
TOP1beta protein, Arabidopsis  EC 5.99.1.2   *DNA Topoisomerases, Type I *Arabidopsis Proteins. Plant Cell 2002 Aug;14(8):2085-93
TOP1alpha protein, Arabidopsis  EC 5.99.1.2   *DNA Topoisomerases, Type I *Arabidopsis Proteins. Plant Cell 2002 Aug;14(8):2085-93
topoisomerase IIIalpha  EC 5.99.1.2   *DNA Topoisomerases, Type I. Nucleic Acids Res 2002 Nov 15;30(22):4823-9
4-methoxybenzo(a)phenazine-11-carboxylic acid (2-(dimethylamino)-1-methylethyl)amide  0   *Phenazines DNA Topoisomerases, Type II/antagonists & inhibitors DNA Topoisomerases, Type I/antagonists & inhibitors. J Med Chem 2002 Jan 31;45(3):721-39
topoisomerase III beta  EC 3.1.-   *DNA Topoisomerases, Type I *Isoenzymes. Biochem Biophys Res Commun 2001 Sep 14;287(1):282-7
topopyrone B  0   *Anthraquinones *Pyrones DNA Topoisomerases, Type I/antagonists & inhibitors. J Antibiot (Tokyo) 2000 Sep;53(9):873-8
topopyrone C  0   *Anthraquinones *Pyrones DNA Topoisomerases, Type I/antagonists & inhibitors. J Antibiot (Tokyo) 2000 Sep;53(9):873-8
topopyrone D  0   *Anthraquinones *Pyrones DNA Topoisomerases, Type I/antagonists & inhibitors. J Antibiot (Tokyo) 2000 Sep;53(9):873-8
topopyrone A  0   *Anthraquinones *Pyrones DNA Topoisomerases, Type I/antagonists & inhibitors. J Antibiot (Tokyo) 2000 Sep;53(9):873-8
6-(3-(2-hydroxyethyl)amino-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno(1,2-)isoquinoline  0   *Indenes *Isoquinolines DNA Topoisomerases, Type I/antagonists & inhibitors. J Med Chem 2000 Oct 5;43(20):3688-98
2-acyl-5,8-dimethoxy-1,4-naphthoquinone  0   *Naphthoquinones DNA Topoisomerases, Type I/antagonists & inhibitors. Eur J Med Chem 2000 Mar;35(3):291-8
6-acyl-5,8-dimethoxy-1,4-naphthoquinone  0   *Naphthoquinones DNA Topoisomerases, Type I/antagonists & inhibitors. Eur J Med Chem 2000 Mar;35(3):291-8
dicentrinone  0   *Aporphines DNA Topoisomerases, Type I/antagonists & inhibitors Ocotea. J Nat Prod 2000 Feb;63(2):217-21
BNP 1350  0   Camptothecin/*analogs & derivatives DNA Topoisomerases, Type I/antagonists & inhibitors. Mol Pharmacol 2000 Mar;57(3):453-9
F 11782  0   *Naphthalenes *Pyrans DNA Topoisomerases, Type II/antagonists & inhibitors DNA Topoisomerases, Type I/antagonists & inhibitors. Biochem Pharmacol 2000 Apr 1;59(7):807-19
ethoxidine  0   *Phenanthridines DNA Topoisomerases, Type I/antagonists & inhibitors. J Biol Chem 2000 Feb 4;275(5):3501-9
R-6 compound  0   *Aminoglycosides DNA Topoisomerases, Type I/antagonists & inhibitors. C R Acad Sci III 1999 Sep;322(9):785-90
BN 80927  0   Camptothecin/*analogs & derivatives DNA Topoisomerases, Type II/antagonists & inhibitors DNA Topoisomerases, Type I/antagonists & inhibitors. Bioorg Med Chem Lett 1999 Sep 6;9(17):2599-602
edotecarin  174402-32-5   *Carbazoles DNA Topoisomerases, Type I/antagonists & inhibitors. Cancer Res 1999 Sep 1;59(17):4271-5
TOPORS protein, human  EC 6.3.2.-   *Neoplasm Proteins *Nuclear Proteins *Ubiquitin-Protein Ligases DNA Topoisomerases, Type I Tumor Suppressor Protein p53 Zinc Fingers. Gene 1999 Jul 22;235(1-2):93-101; Nucleic Acids Res 1999 Jun 15;27(12):2538-44
N,N-bis(3-(5-methylacridine-4-carboxamido)propyl)methylamine  0   *Acridines DNA Topoisomerases, Type II/antagonists & inhibitors DNA Topoisomerases, Type I/antagonists & inhibitors. J Med Chem 1999 Jul 1;42(13):2383-93
N,N-bis(3-(5-bromoacridine-4-carboxamido)propyl)methylamine  0   *Acridines DNA Topoisomerases, Type II/antagonists & inhibitors DNA Topoisomerases, Type I/antagonists & inhibitors. J Med Chem 1999 Jul 1;42(13):2383-93
3,9-dibromo-12-(4-O-methylglucopyranosyl)-6,7.12,13-tetrahydroindolo(2,3-a)pyrrolo(3,4-c)carbazole-5,7-dione  0   *Carbazoles Glucose/*analogs & derivatives DNA Topoisomerases, Type I/antagonists & inhibitors. J Med Chem 1999 May 20;42(10):1816-22
BM 2419-2  0   *Anthracyclines DNA Topoisomerases, Type I/antagonists & inhibitors. J Antibiot (Tokyo) 1998 Dec;51(12):1069-74
BM 2419-1  0   *Anthracyclines DNA Topoisomerases, Type I/antagonists & inhibitors. J Antibiot (Tokyo) 1998 Dec;51(12):1069-74
Cl-DACA  0   *Acridines DNA Topoisomerases, Type I/antagonists & inhibitors. Cancer Chemother Pharmacol 1999;43(4):302-8
topostatin  0   *Lactams DNA Topoisomerases, Type I/antagonists & inhibitors. J Antibiot (Tokyo) 1998 Nov;51(11):991-8
5-ethyl-9,10-difluoro-1,4,5,13-tetrahydro-5-hydroxy-3H,15H-oxepino(3',4'-6,7)indolizino(1,2-b)quinoline-3,15-dione  0   *Benzoxepins Camptothecin/*analogs & derivatives DNA Topoisomerases, Type I/antagonists & inhibitors. J Med Chem 1998 Dec 31;41(27):5410-9
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