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Information on EC 5.6.2.1 - DNA topoisomerase and Organism(s) Homo sapiens and UniProt Accession P11387

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EC Tree
IUBMB Comments
These enzymes bring about the conversion of one topological isomer of DNA into another, e.g., the relaxation of superhelical turns in DNA, the interconversion of simple and knotted rings of single-stranded DNA, and the intertwisting of single-stranded rings of complementary sequences, cf. EC 5.6.2.2 DNA topoisomerase (ATP-hydrolysing).
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: P11387
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
ATP-independent breakage of single-stranded DNA, followed by passage and rejoining
Synonyms
topoisomerase, topoisomerase i, topo i, dna topoisomerase i, topoisomerase iv, dna topoisomerase, topoisomerase 1, human topoisomerase i, reverse gyrase, topoisomerase-i, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
DNA topoisomerase I
-
DNA topoisomerase IB
-
human topoisomerase I
-
topoisomerase 1
-
topoisomerase IB
-
Deoxiribonucleate topoisomerase
-
-
-
-
Deoxiribonucleic topoisomerase
-
-
-
-
DNA Top IB
-
-
DNA topo I
-
-
DNA topoisomerase
-
-
DNA topoisomerase 1
-
-
DNA topoisomerase IB
-
-
DNA topoisomerase IIIalpha
-
-
HssTopoI
-
-
hTop1p
-
-
hTopI
-
-
hTopo
-
-
htopo I
-
-
hTopo IIIalpha
-
-
hTopoI
human DNA topoisomerase I
-
-
human topo I
-
-
Isomerase, deoxiribonucleate topo-
-
-
-
-
Late protein H6
-
-
-
-
Nicking-closing enzyme
-
-
-
-
omega-Protein
-
-
-
-
Relaxing enzyme
-
-
-
-
Reverse gyrase
-
-
-
-
Swivelase
-
-
-
-
TOP1mt
-
-
-
-
TopIB
-
-
Topo I
Topoisomerase
-
-
-
-
topoisomerase 1
-
-
Topoisomerase I
topoisomerase IIIalpha
-
-
topoisomerase-I
-
-
TpI
-
-
-
-
Type I DNA topoisomerase
-
-
-
-
Untwisting enzyme
-
-
-
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP-independent breakage of single-stranded DNA, followed by passage and rejoining
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
isomerization
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
DNA topoisomerase
These enzymes bring about the conversion of one topological isomer of DNA into another, e.g., the relaxation of superhelical turns in DNA, the interconversion of simple and knotted rings of single-stranded DNA, and the intertwisting of single-stranded rings of complementary sequences, cf. EC 5.6.2.2 DNA topoisomerase (ATP-hydrolysing).
CAS REGISTRY NUMBER
COMMENTARY hide
80449-01-0
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
negatively supercoiled DNA
relaxed DNA
show the reaction diagram
-
-
-
?
negatively supercoiled pBlueScript KSII(+) DNA
relaxed pBlueScript KSII(+) DNA
show the reaction diagram
-
-
-
?
supercoiled pBR322 plasmid DNA
relaxed pBR322 plasmid DNA
show the reaction diagram
-
-
-
?
supercoiled plasmid DNA pBR322
relaxed plasmid DNA pBR322
show the reaction diagram
-
-
-
?
117-base pair DNA oligonucleotide
?
show the reaction diagram
-
-
-
-
?
DNA
DNA
show the reaction diagram
-
so-called suicide substrate, contains a htopoI preferential binding sequence and is designed to trap the liberated 5'-OH end
-
-
?
Holliday Junction Substrate H1-4
?
show the reaction diagram
-
close relationship between tyrosine recombinases and type IB topoisomerases, investigation of ability of human topoisomerase I to resolve the typical intermediate of recombinase catalysis, the Holliday junction, results consolidate the relationship between type IB topoisomerases and tyrosine recombinases
-
-
?
negatively supercoiled DNA
?
show the reaction diagram
negatively supercoiled DNA
relaxed DNA
show the reaction diagram
-
-
-
-
?
negatively supercoiled pHC624 plasmid DNA
relaxed pHC624 plasmid DNA
show the reaction diagram
-
-
-
-
?
negatively supercoiled pHOTI plasmid DNA
?
show the reaction diagram
-
-
-
?
Nicked circular DNA
Large catenated DNA networks
show the reaction diagram
relaxed pBR322 DNA
?
show the reaction diagram
-
-
-
-
?
SF2/ASF protein + ATP
?
show the reaction diagram
-
kinase activity
-
?
supercoiled DNA
relaxed closed circular DNA
show the reaction diagram
supercoiled DNA
relaxed DNA
show the reaction diagram
-
-
-
-
?
supercoiled pBR322 DNA
?
show the reaction diagram
-
-
-
-
?
supercoiled pBR322 plasmid DNA
relaxed pBR322 plasmid DNA
show the reaction diagram
-
-
-
-
?
supercoiled plasmid DNA pGEM-5T
?
show the reaction diagram
-
relaxation
-
?
supercoiled plasmid pBAD-GFPuv
?
show the reaction diagram
-
-
-
-
?
supercoiled plasmid pBR322 DNA
relaxed plasmid pBR322 DNA
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
supercoiled DNA
relaxed DNA
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
cyclin
-
-
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I inhibitory activity, cytotoxicity, and structure-activity relationship, overview. 2-Furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(-)-epigallocatechin
(-)-epigallocatechin 3-O-(E)-p-coumarate
-
(-)-epigallocatechin 3-O-(E)-p-coumaroate
-
(-)-epigallocatechin-3-gallate
-
(-)-epigallocatechin3-O-(Z)-p-coumarate
-
(-)-epigallocatechin3-O-(Z)-p-coumaroate
-
(-)-gallocatechin
(1S,12aR,12bR)-1,4,9,12a-tetrahydroxy-1,2,11,12,12a,12b-hexahydroperylene-3,10-dione
i.e. altertoxin I
(1S,12S,12aR,12bR)-1,4,9,12,12a-pentahydroxy-1,2,11,12,12a,12b-hexahydroperylene-3,10-dione
i.e. 6-epi-stemphytriol
(2E)-3-[(6R,7S)-7-[(2,4-dihydroxy-6-methylbenzoyl)oxy]-6-hydroxy-7-methyl-8-oxo-6,7,8,8a-tetrahydro-1H-2-benzopyran-3-yl]prop-2-enoic acid
i.e. pinophilin F
(2E)-3-[(7R)-7-[(2,4-dihydroxy-6-methylbenzoyl)oxy]-7-methyl-6,8-dioxo-6,7,8,8a-tetrahydro-1H-2-benzopyran-3-yl]prop-2-enoic acid
i.e. (-)-mitorubrinic acid
(2R)-2-[(2S,3S)-3-acetamido-5-oxooxolan-2-yl]-2-hydroxy-N-[(S)-[(3S)-8-hydroxy-1-oxo-3,4-dihydro-1H-2-benzopyran-3-yl][(propan-2-yl)amino]methyl]acetamide (non-preferred name)
i.e. AI-77-C
(3beta,5alpha,6beta,17alpha,22E)-6-methoxyergost-22-ene-3,5-diol
i.e. 3beta,5alpha-dihydroxy-6beta-methoxy-ergosta-7,22-diene
(3beta,5alpha,6beta,17alpha,22E)-ergost-22-ene-3,5,6-triol
i.e. ergosta-7,22-diene-3beta,5alpha,6beta-triol
(3S,8aR)-3-[[(3S)-7,7-dimethyl-3-(2-methylbut-3-en-2-yl)-2-oxo-1,2,3,7-tetrahydropyrano[2,3-g]indol-3-yl]methyl]-8a-methoxyhexahydropyrrolo[1,2-a]pyrazine-1,4-dione
i.e. notoamide Q
(5aR,7R,9aR)-7',7',8,8-tetramethyl-1',2,3,7',8a,9-hexahydro-1H,2'H,5H,6H,8H,10H-spiro[5a,9a-(epiminomethano)cyclopenta[f]indolizine-7,3'-pyrano[2,3-g]indole]-2',5,10-trione
i.e. (-)-versicolamide B
(5aS,13bS)-1,5a,9,13-tetrahydroxy-3,7-dimethyl-5,5a-dihydro-4H,10H,12H,14H,16H-pyrano[3''',4''',5''':4'',5'']naphtho[2'',1'':4',5']furo[2',3':7,8]naphtho[1,8-cd]pyran-4,10,16-trione (non-preferred name)
i.e. bacillosporin C
(6bR,7aS,12aS,14aS)-6b-hydroxy-3,3-dimethyl-14a-(2-methylbut-3-en-2-yl)-3,6b,7,7a,10,11,12,12a,14a,15-decahydro-8H,13H-pyrano[2,3-g]pyrrolo[1'',2'':4',5']pyrazino[1',2':1,5]pyrrolo[2,3-b]indole-8,13-dione
i.e. notoamide D
(7aS,12aS,13aR)-3,3,14,14-tetramethyl-3,7,11,12,13,13a,14,15-octahydro-8H,10H-7a,12a-(epiminomethano)indolizino[6,7-h]pyrano[3,2-a]carbazole-8,16-dione
i.e. 6-epi-stephacidin A
(7aS,12aS,13aS)-3,3,14,14-tetramethyl-3,7,11,12,13,13a,14,15-octahydro-8H,10H-7a,12a-(epiminomethano)indolizino[6,7-h]pyrano[3,2-a]carbazole-8,16-dione
i.e. stephacidin A
(7R)-3-[(1E)-3-hydroxyprop-1-en-1-yl]-7-methyl-6,8-dioxo-6,7,8,8a-tetrahydro-1H-2-benzopyran-7-yl 2,4-dihydroxy-6-methylbenzoate
i.e. (-)-mitorubrinol
(7S,8S,8aS)-7-hydroxy-3-[(1E)-3-hydroxyprop-1-en-1-yl]-7-methyl-6-oxo-6,7,8,8a-tetrahydro-1H-2-benzopyran-8-yl 2,4-dihydroxy-6-methylbenzoate
i.e. pinophilin B
(7S,8S,8aS)-8-hydroxy-3-[(1E)-3-hydroxyprop-1-en-1-yl]-7-methyl-6-oxo-6,7,8,8a-tetrahydro-1H-2-benzopyran-7-yl 2,4-dihydroxy-6-methylbenzoate
i.e. pinophilin D
1,3-[6-(3-Amino-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline]-[5',6'-dihydro-6'-(3'-amino-1'-propyl)-5',11'-dioxo-11'H-indeno[1,2-c]-isoquinoline]propane bis(trifluoroacetate)
-
11-hydroxy-3-[(1R)-1-hydroxy-3-methylbutyl]-4-methoxy-9-methyl-5H,7H-dibenzo[b,g][1,5]dioxocin-5-one
i.e. vermixocin A
12H-5,11a-diazadibenzo[b,h]fluoren-11-one
i.e. rosettacin
14-(1-imidazolylmethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
14-(1-morpholinomethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
14-(10'-aminodecyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(11'-aminoundecyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(12'-aminododecyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(2'-aminoethyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(3'-aminopropyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(3-aminopropyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one dihydrochloride
-
14-(3-N-ethanolaminopropyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trifluoroacetate
-
14-(4'-aminobutyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(5'-aminopentyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(6'-aminohexyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(7'-aminoheptyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(8'-aminooctyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(9'-aminononyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
-
14-(N,N-dimethylaminomethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
14-(N-ethanolaminomethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11one
-
14-aminomethyl-12H-5,11a-diazadibenzo[b,h]fluoren-11-one dihydrochloride
-
14-chloromethyl-12H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
14-[(1-imidazolyl)propylaminomethyl]-12H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
14-[1-(N-methylpiperazinylmethyl)]-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
14-[3(1-morpholinopropyl)]-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trifluoroacetate
-
14-[3-(1-imidazolylpropyl)]-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trifluoroacetate
-
14-[3-(N,N-dimethylaminopropyl)]-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trifluoroacetate
-
14-[N-(S)-3-hydroxypyrrolidinomethyl]-12H-5,11a diazadibenzo[b,h]fluoren-11-one
-
2(2.6-dihydrobenzoyl)-3-hydroxy-5-hydroxymethylbenzoic acid methyl ester
-
2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
i.e. NSC314622
2,3-dimethoxy-8,9-methylenedioxy-10-(1H-imidazol-yl)methyl-11H-indeno[1,2-c]isoquinoline
-
2,3-dimethoxy-8,9-methylenedioxy-10-(4-methylpiperazin-1-yl)-methyl-11H-indeno[1,2-c]isoquinoline
-
2,3-dimethoxy-8,9-methylenedioxy-10-(4-morpholino)methyl-11H-indeno[1,2-c]isoquinoline
-
2,3-dimethoxy-8,9-methylenedioxy-10-(dimethylamino)methyl-11H-indeno[1,2-c]isoquinoline
influence of protonation state on Top1 inhibition
2,3-dimethoxy-8,9-methylenedioxy-10-(N,N',N'-trimethylethylenediamino)methyl-11H-indeno[1,2-c]isoquinoline
-
2,3-dimethoxy-8,9-methylenedioxy-10-(pyrrolidin-1-yl)methyl-11H-indeno[1,2-c]isoquinoline
influence of protonation state on Top1 inhibition
2,3-dimethoxy-8,9-methylenedioxy-10-methyl-11H-indeno[1,2-c]-isoquinoline
-
2-O-(3,4-dihydroxybenzoyl)-2,4,6-trihydroxyphenylacetic acid
-
22-hydroxyacuminatine
-
4-[3-[ethyl(methyl)amino]propyl]furo[3,2-c]phenanthridine-5,10,11(4H)-trione
-
6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
class of non-camptothecin topoisomerase I inhibitors, exert cytotoxicity by trapping the covalent complex formed between DNA and Top1during relaxation of DNA supercoils
6-epi-stemphytriol
-
6-{3-[(2-hydroxyethyl)amino]propyl}-2,3-dimethoxy-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
i.e. MJ-III-65
altertoxin I
-
bacillosporin C
-
bis-1,2-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-(ethylamino)-ethylamino]ethane tetra(trifluoroacetate)
-
bis-1,2-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-ethylamino]ethane bis(trifluoroacetate)
weak activity
bis-1,2-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino]ethane bis(trifluoroacetate)
similar activity as 1 microM camptothecin
bis-1,3-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-ethylamino]propane bis(trifluoroacetate)
similar activity as 1 microM camptothecin
bis-1,3-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino]propane bis(trifluoroacetate)
similar activity as 1 microM camptothecin
bis-1,3-[(5,6-dihydro-5,11-diketo-2,3-dimethoxy-11H-indeno-[1,2-c]isoquinoline)-6-ethylamino]propane bis(trifluoroacetate)
-
bis-1,3-[(5,6-dihydro-5,11-diketo-2,3-dimethoxy-11H-indeno-[1,2-c]isoquinoline)-6-propylamino]propane bis(trifluoroacetate)
-
bis-1,3-[(5,6-dihydro-5,11-diketo-3-nitro-11H-indeno[1,2-c]isoquinoline)-6-ethylamino]propane bis(trifluoroacetate)
-
bis-1,4-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-(6-propyl-tert-BOCamino)]butane
weak activity
bis-1,4-[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino]butane bis(trifluoroacetate)
similar activity as 6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-(ethylamino)-ethyl]amine tris(trifluoroacetate)
similar activity as 6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-ethyl]amine
weak activity
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propyl]amine
weak activity
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propyl]methylamine
weak activity
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)]-(6-ethyl,6'-propyl)ammonium Trifluoroacetate
weak activity
bis[(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)]-(6-propyl,6'-butyl)amine hydrochloride
weak activity
camptothecin
curcumin sulfate
i.e. diferuloylmethane sulfate
cyclocurcumin
-
dihydroquercetin
i.e. (2R,3R)-2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-2,3-dihydro-4H-1-benzopyran-4-one
dimethoxyaromathecin
-
hydroxylcamptothecin
topoisomerase I inhibitor
indenoisoquinoline
irinotecan
methyl (2R)-2-([3-[(3,3-dimethyloxiran-2-yl)methyl]-4-hydroxyphenyl]methyl)-4-hydroxy-3-(4-hydroxyphenyl)-5-oxo-2,5-dihydrofuran-2-carboxylate
i.e. butyrolactone I
methyl (2R)-4-hydroxy-2-[[4-hydroxy-3-(3-methylbutyl)phenyl]methyl]-3-(4-hydroxyphenyl)-5-oxo-2,5-dihydrofuran-2-carboxylate
i.e. butyrolactone III
N,N-dimethyl(6-methyl-10,11-dioxo-10,11-dihydrophenanthro[1,2-b]furan-1-yl)methanaminium (2E)-3-carboxyprop-2-enoate
-
-
norindenoisoquinoline
-
NSC 314622
-
pyridoxal
-
pyridoxal 5'-diphospho-5'-adenosine
-
pyridoxal 5'-phosphate
competitive inhibitor of Candida guilliermondii topoisomerase I
quercetin
rosettacin
-
tanshinone-1
less than 10% inhibition at 0.005 mM
topotecan
Urea
inhibitory effect to W203A/W205A/W206A mutant
Zn(isaepy)Cl2
complete inhibition at 0.3 mM
[Cu(isaepy)H2O]ClO4
complete inhibition at 0.15 mM
[Cu(isapnsal)]ClO4
poor inhibition
[Zn(isapnsal)]ClO4
poor inhibition
(+)-cheilanthifoline
-
very weak inhibition
(+)-isocorydine
-
-
(-)-cavidine
-
very weak inhibition
(-)-cryptotanshinone
-
diterpenoid from Salvia castanea f. tomentos
(-)-pallidine
-
comparable to camptothecin
(-)-scoulerine
-
inhibition comparable to camptothecin
(-)-tetrahydropalmatine
-
very weak inhibition
(1,1',1'',1'''-[(1,4-dihydroporphyrin-5,10,15,20-tetrayl-k4N21,N22,N23,N24)tetrakis(benzene-4,1-diylmethanediyl)]tetrakis[1-methylpiperidiniumato(2-)])nickel(4+) tetraiodide
-
-
(1,1',1'',1'''-[(1,4-dihydroporphyrin-5,10,15,20-tetrayl-k4N21,N22,N23,N24)tetrakis(benzene-4,1-diylmethanediyl)]tetrakis[1-methylpiperidiniumato(2-)])zinc(4+) tetraiodide
-
-
(2,2',2'',2''',2'''',2''''',2'''''',2'''''''-[(5,28-dihydro-29H,31H-tetrabenzoporphine-2,3,9,10,16,17,23,24-octayl-k4N29,N30,N31,N32)octasulfanediyl]octakis(N,N-diethyl-N-methylethanaminiumato)(2-))zinc(8+) octaiodide
-
-
(2S,3R)-5-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-8-phenyl-2,3,8,9-tetrahydro-10H-[1,4]dioxino[2,3-f]chromen-10-one
-
-
(2S,3R,4S,6R)-4-amino-2-methyl-6-((3-(2-phenyl-1-tosyl-1H-indol-3-yl)prop-2-yn-1-yl)oxy)tetrahydro-2H-pyran-3-ol
-
92.8% inhibition at 0.1 mM
(2S,3R,4S,6R)-4-amino-2-methyl-6-((3-(2-phenylbenzofuran-3-yl)prop-2-yn-1-yl)oxy)tetrahydro-2H-pyran-3-ol
-
25.5% inhibition at 0.1 mM
(2S,3R,4S,6R)-4-amino-2-methyl-6-((3-(2-phenylbenzo[b]thiophen-3-yl)prop-2-yn-1-yl)oxy)tetrahydro-2H-pyran-3-ol
-
32.2% inhibition at 0.1 mM
(2S,3R,4S,6R)-4-amino-2-methyl-6-(3-(2-phenyl-1H-indol-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-ol
(2S,3S,6R)-2-methyl-6-(3-(2-phenyl-1-tosyl-1H-indol-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-amine
-
43.2% inhibition at 0.1 mM
(2S,3S,6R)-2-methyl-6-(3-(2-phenyl-1H-indol-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-amine
-
4.0% inhibition at 0.1 mM
(2S,3S,6R)-2-methyl-6-(3-(2-phenylbenzo[b]thiophen-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-amine
-
7.9% inhibition at 0.1 mM
(5Z,7E,9E,14Z,17Z)-icosa-5,7,9,14,17-pentaenoic acid
-
-
(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)carbamic acid
-
-
(6aR,11aS)-11-[(4-methylphenyl)sulfonyl]-6,6a,11,11a-tetrahydro-5H-benzo[a]carbazole
-
binds selectively to PfTopoI
(7aR,12aS)-5-methylidene-12-[(4-methylphenyl)sulfonyl]-7,7a,12,12a-tetrahydrobenzo[6,7]chromeno[4,3-b]indol-13(5H)-one
-
-
(7aS,12aS)-10-methoxy-5-methylidene-5,7,7a,12a-tetrahydro-13H-[1]benzofuro[3,2-c]benzo[g]chromen-13-one
-
-
(7aS,12aS)-11-methoxy-5-methylidene-13-oxo-5,7a,12a,13-tetrahydro-7H-[1]benzofuro[3,2-c]benzo[g]chromene-9-carbaldehyde
-
-
(7aS,12aS)-5-methylidene-5,7,7a,12a-tetrahydro-13H-[1]benzofuro[3,2-c]benzo[g]chromen-13-one
-
-
(9-([2-(1H-Indol-3-yl)ethyl]amino)-3-acridinyl)(4-methyl-1-piperazinyl)methanone
-
-
(9-([2-(1H-indol-3-yl)ethyl]amino)acridin-3-yl)(4-methylpiperazin-1-yl)methanone
-
-
(9-([2-(1H-indol-3-yl)ethyl]amino)acridin-4-yl)(4-methylpiperazin-1-yl)methanone
-
-
(9-[(1-benzylpiperidin-4-yl)amino]acridin-3-yl)(4-methylpiperazin-1-yl)methanone
-
-
(S)-6-(6-nitrobenzothiazol-2-yl)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine
-
-
(S)-6-(benzothiazol-2-yl)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-7H-pyrido[1,2,3-de][1,4]-benzoxazine
-
-
(S)-camptothecin
-
-
1,1',1'',1'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis(1-methylpiperidinium) tetraiodide
-
-
1,1',1'',1'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis[3-(ethoxycarbonyl)-1-methylpiperidinium] tetraiodide
-
-
1,1',1'',1'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis[3-(hydroxymethyl)-1-methylpiperidinium] tetraiodide
-
-
1,5-dideoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-xylo-hexitol
-
-
1-(alpha-L-idopyranosyl)-N-(2-methylbenzoyl)-5-(methylsulfanyl)-1H-1,2,4-triazol-3-amine
-
-
1-(hydroxymethyl)-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-beta-carbolin-1-yl)-cyclopentanol
-
-
1-deoxy-1-(3-nitro-5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-glucitol
-
-
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-allitol
-
-
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-arabinitol
-
-
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-galactitol
-
-
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-glucitol
-
-
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-mannitol
-
-
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-ribitol
-
-
1-ethoxycarbonyl-naphthoquinone-[2,3-d]indolizidine-6,11-dione
-
0.1 mg/ml, 4.1% inhibition of relaxation
1-ethyl-3-(5-aminobenzimidazol-2-yl)-6-fluoro-7-(4-methyl-1-piperazinyl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-aminobenzoimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naph- thyridin-4(1H)-one
-
-
1-ethyl-3-(6-aminobenzoimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridin-4(1H)-one
-
-
1-ethyl-3-(6-aminobenzoimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-chlorobenzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
-
-
1-ethyl-3-(6-chlorobenzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-nitrobenzimidazol-2-yl)-6-fluoro-7-(4-methyl-1-piperazinyl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-nitrobenzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
-
-
1-ethyl-3-(6-nitrobenzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-nitrobenzothiazol-2-yl)-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-nitrobenzothiazol-2-yl)-6-fluoro-7-(4-methylpiperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-nitrobenzothiazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
-
-
1-ethyl-3-(6-nitrobenzothiazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-nitrobenzoxazol-2-yl)-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4(1H)-quinolone
1-ethyl-3-(6-nitrobenzoxazol-2-yl)-6-fluoro-7-(4-methylpiperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(6-nitrobenzoxazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
-
-
1-ethyl-3-(6-nitrobenzoxazol-2-yl)-6-fluoro-7-chloro-4(1H)-quinolone
-
-
1-ethyl-3-(benzimidazol-2-yl)-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4(1H)-quinolone
-
9% and 11% inhibition at 0.1 mM and 0.02 mM, respectively
1-ethyl-3-(benzothiazol-2-yl)-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(benzothiazol-2-yl)-6-fluoro-7-(4-methylpiperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-3-(benzothiazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
-
-
1-ethyl-3-(benzothiazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
-
-
1-ethyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)-3-(6-nitro-1,3-benzoxazol-2-yl)quinolin-4(1H)-one
-
interacts with DNA-Top I complex and induces cancer cell apoptosis to produce antitumor effects
1-ethylKuQuinone
-
synthesis of the pentacyclic-diquinoid synthetic compound, overview. It efficiently inhibits the cleavage step of the enzyme reaction fitting well into the catalytic site. When incubated with the binary topoisomerase-DNA cleaved complex, the compound helps the enzyme to remove itself from the cleaved DNA and close the DNA gap, increasing the religation rate. Et-KuQ inhibits the relaxation activity of Top1. The compound also induces the religation of the stalled enzyme-camptothecin-DNA ternary complex. Docking and molecular modeling, overview
1-hydroxy-3-(oxiran-2-ylmethoxy)-9H-xanthen-9-one
-
-
1-hydroxy-3-[2-hydroxy-3-[(2-hydroxyethyl)amino]propoxy]-9H-xanthen-9-one
-
1.1% inhibition at 0.02 mM
1-hydroxy-3-[2-hydroxy-3-[(3-hydroxypropyl)amino]propoxy]-9H-xanthen-9-one
-
3.5% inhibition at 0.02 mM
1-hydroxy-8-methoxyanthracene-9,10-dione
-
-
1-methyl-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-beta-carbolin-1-yl)-cyclopentanol
-
-
1-[2-(dimethylamino)ethoxy]-8-methoxyanthracene-9,10-dione
-
-
1-[2-(dimethylamino)ethyl]-3-[(4-methylphenyl)sulfonyl]-1H-pyrrolo[2,3-b]quinoxalin-2-amine
-
-
10-Hydroxycamptothecin
10-methoxy-9-{2-[(2,9,10-trimethoxy-5,6-dihydroisoquino[3,2-a]isoquinolinium-3-yl)oxy]ethoxy}[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium dichloride
-
synthetic protoberberine alkaloid, highly active
10-methoxy-9-{3-[(2,9,10-trimethoxy-5,6-dihydroisoquino[3,2-a]isoquinolinium-3-yl)oxy]propoxy}[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium dichloride
-
synthetic protoberberine alkaloid, highly active
10-methoxy-9-{4-[(2,9,10-trimethoxy-5,6-dihydroisoquino[3,2-a]isoquinolinium-3-yl)oxy]butoxy}[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium dichloride
-
synthetic protoberberine alkaloid, highly active
11-acetyl-10-amino-indolizino[3,2-g]quinoline-5,12-dione
-
-
11-acetyl-10-bromo-indolizino[3,2-g]quinoline-5,12-dione
-
-
11-acetyl-10-chloro-indolizino[3,2-g]quinoline-5,12-dione
-
-
11-acetyl-10-fluoro-indolizino[3,2-g]quinoline-5,12-dione
-
-
11-acetyl-10-hydroxy-indolizino[3,2-g]quinoline-5,12-dione
-
-
11-acetylindolizino[3,2-g]quinoline-5,12-dione
-
-
11-hexyl-5-(4-methylpiperazin-1-yl)-11H-indeno[1,2-c]isoquinolin-11-ol
-
-
11-hydroxy-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
11-hydroxy-2-methyl-8-nitro-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
11-hydroxy-2-phenyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
11-methoxy-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
11-methoxy-2-phenyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
11-methyl-5-(4-methylpiperazin-1-yl)-11H-indeno[1,2-c]isoquinolin-11-ol
-
-
11-methylindolizino[3,2-g]quinoline-5,12-dione
-
-
11-[2-(dimethylamino)ethoxy]-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
14-chloromethyl-12H-5,11adiazadibenzo[b,h]fluoren-11-one
-
-
17-beta-3-oxo-18-norandrost-4-ene-17-carboxylic acid -4-bromo-benzene sulfonic acid ester
-
partial or complete inhibition of hTopo is only observed at relatively high compound concentrations in the range 5 to 20 microM
17beta-O-[N-(benzyl)carbomyl]-oleanolic acid
-
-
2'-(4-(3,6,9,12,15,18-hexaoxahenicos-20-ynyloxy)phenyl)-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
-
2'-(4-ethoxyphenyl)-5-(4-methylpiperazinyl)-2,5'-bi-1H-benzimidazole
-
reversibly traps enzyme cleavage complexes with a different and more specific sequence selectivity
2'-(4-ethoxyphenyl)-6-(4-methylpiperazin-1-yl)-1H,3'H,2,5'-bisbenzimidazole
-
Hoechst 33342
2'-(4-hydroxyphenyl)-5-(4-methylpiperazinyl)-2,5'-bi-1H-benzimidazole
-
reversibly traps enzyme cleavage complexes with a different and more specific sequence selectivity
2'-[4-([6-[(but-3-yn-1-yl)oxy]hexyl]oxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
-
2'-[4-[(but-3-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
-
2'-[4-[(heptadec-16-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
-
2'-[4-[(hex-5-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
-
-
2,3-dichloro-5H-isoindolo[2,1-a]quinoxalin-6-one
-
-
2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
2,3-dimethyl-5H-isoindolo[2,1-a]quinoxalin-6-one
-
-
2,4-di(furan-2-yl)-5H-chromeno[4,3-b]pyridine
2,4-di(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine
-
-
2,4-di(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
-
-
2,4-di(thiophen-3-yl)-5H-chromeno[4,3-b]pyridine
-
-
2,4-diphenyl-5H-chromeno[4,3-b]pyridine
-
-
2-((6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino)acetic acid
-
-
2-((6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino)acetic acid hydrochloride
-
-
2-(4-((1-(2-azidoethyl)-1H-1,2,3-triazol-4-yl)methoxy)-phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole
-
-
2-(4-(2-(4-(4-ethynylphenyl)-1H-1,2,3-triazol-1-yl)ethoxy)-phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole
-
-
2-(4-chlorophenyl)-4-(furan-3-yl)-6-(3-methylthiophen-2-yl) pyridine
-
86% inhibition at 0.1 mM
2-(4-chlorophenyl)-6-(5-chlorothiophen-2-yl)-4-(furan-2-yl) pyridine
-
53% inhibition at 0.1 mM
2-(4-ethoxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]-imidazole
-
-
2-(4-hydroxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo-[d]imidazole-4-carboxylic acid
-
-
2-(4-[[1-(6-azidohexyl)-1H-1,2,3-triazol-4-yl]methoxy]phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
-
-
2-(5-chlorothiophen-2-yl)-4-(furan-3-yl)-6-(5-methylfuran-2-yl) pyridine
-
13.2% inhibition at 0.1 mM
2-(5-chlorothiophen-2-yl)-4-(furan-3-yl)-6-o-tolylpyridine
-
4.6% inhibition at 0.1 mM
2-(5-chlorothiophen-2-yl)-6-(furan-2-yl)-4-(furan-3-yl)pyridine
-
9.6% inhibition at 0.1 mM
2-(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)-N-[2-methyl-1-(morpholin-4-ylcarbonyl)propyl]acetamide
-
-
2-(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)-N-[3-methyl-1-[(4-methylpiperazin-1-yl)carbonyl]butyl]acetamide
-
-
2-(furan-2-yl)-4-(furan-3-yl)-6-(3-methylthiophen-2-yl)pyridine
-
5.4% inhibition at 0.1 mM
2-(furan-2-yl)-4-(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine
2-(furan-2-yl)-4-(pyridin-3-yl)-5H-chromeno[4,3-b]pyridine
2-(furan-2-yl)-4-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
-
-
2-(furan-2-yl)-4-phenyl-5H-chromeno[4,3-b]pyridine
2-(piperidin-1-yl)ethyl5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
2-(pyridin-2-yl)-4-(pyridin-3-yl)-5H-chromeno[4,3-b]pyridine
2-(pyridin-2-yl)-4-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
2-(pyridin-2-yl)ethyl5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
2-(pyrrolidin-1-yl)ethyl 5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
2-Amino-1-(1-benzyl-piperidin-4-yl)-4,9-dioxo-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 4.1% inhibition of relaxation
2-Amino-1-(2-bromo-ethyl)-4,9-dioxo-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 58.7% inhibition of relaxation
2-Amino-1-(2-hydroxy-ethyl)-4,9-dioxo-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 27.3% inhibition of relaxation
2-Amino-1-(4-amino-phenyl)-4,9-dioxo-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 9.4% inhibition of relaxation
2-Amino-1-(4-fluoro-phenyl)-4,9-dioxo-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 67.8% inhibition of relaxation
2-Amino-1-benzyl-4,9-dioxo-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 15.7% inhibition of relaxation
2-Amino-1-cyclohexyl-4,9-dioxo-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 12.2% inhibition of relaxation
2-Amino-1-isopropyl-4,9-dioxo-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 8.6% inhibition of relaxation
2-amino-3-ethoxycarbonyl-N-(4-fluorophenyl)benz[f]indole-4,9-dione
-
potent inhibitor
2-amino-3-ethoxycarbonyl-N-methyl-benz[f]indole-4,9-dione
-
0.1 mg/ml, 5.6% inhibition of relaxation
2-Amino-4,9-dioxo-1-p-tolyl-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 4.3% inhibition of relaxation
2-Amino-4,9-dioxo-1-phenyl-3a,4,9,9a-tetrahydro-1H-benzo[f]indole-3-carboxylic acid ethyl ester
-
0.1 mg/ml, 2.9% inhibition of relaxation
2-bromoethyl 5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
2-hydroxy-3-ethoxycarbonyl-N-(3,4-dimethylphenyl)-benz[f]indole-4,9-dione
-
0.1 mg/ml, 6.6% inhibition of relaxation
2-phenyl-4-(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine
-
-
2-phenyl-4-(pyridin-3-yl)-5H-chromeno[4,3-b]pyridine
-
-
2-phenyl-4-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
-
-
2-phenyl-4-(thiophen-3-yl)-5H-chromeno[4,3-b]pyridine
2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetic acid
-
-
2-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)amino]acetic acid
-
-
2-[4-(2-azidoethoxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
-
-
2-[4-[(4,11-dihydroxy-5,10-dioxo-5,10-dihydro-1H-naphtho[2,3-f]indol-3-yl)methyl]piperazin-1-yl]ethyl acetate
-
-
20(S)-camptothecin
-
-
20-mercaptocamptothecin
-
weak
20-thio camptothecin
-
analogue of camptothecin, inhibit a modified human topoisomerase I
3,10-dibromo-11-hydroxy-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
3,3'-(4-phenylpyridine-2,6-diyl)diphenol
-
67.2% inhibition at 0.1 mM
3,3'-[butane-1,4-diylbis(oxy)]bis(2,9,10-trimethoxy-5,6-dihydroisoquino[3,2-a]isoquinolinium) dichloride
-
synthetic protoberberine alkaloid, highly active
3,3'-[ethane-1,2-diylbis(oxy)]bis(2,9,10-trimethoxy-5,6-dihydroisoquino[3,2-a]isoquinolinium) dichloride
-
synthetic protoberberine alkaloid, highly active. Strongly stabilize the enzyme-DNA binary complex at low concentration (50–100microM). From 0.1 to 1 mM, their ability to stabilize is weak
3,3'-[propane-1,3-diylbis(oxy)]bis(2,9,10-trimethoxy-5,6-dihydroisoquino[3,2-a]isoquinolinium) dichloride
-
synthetic protoberberine alkaloid, highly active
3-(1,3-benzoxazol-2-yl)-1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)quinolin-4(1H)-one
-
-
3-(1,3-benzoxazol-2-yl)-1-ethyl-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridin-4(1H)-one
-
-
3-(1,3-benzoxazol-2-yl)-7-chloro-1-ethyl-6,8-difluoroquinolin-4(1H)-one
-
-
3-(1,3-benzoxazol-2-yl)-7-chloro-1-ethyl-6-fluoroquinolin-4(1H)-one
-
-
3-(1H-benzimidazol-2-yl)-1-ethyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)quinolin-4(1H)-one
-
-
3-(1H-benzimidazol-2-yl)-1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)quinolin-4(1H)-one
-
-
3-(1H-benzimidazol-2-yl)-1-ethyl-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridin-4(1H)-one
-
-
3-(1H-benzimidazol-2-yl)-1-ethyl-6-fluoro-7-(piperazin-1-yl)quinolin-4(1H)-one
-
-
3-(2,3-dimethoxy-5,12-dioxo-5,12-dihydro-6H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinolin-6-yl)propan-1-aminium chloride
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
3-(2,6-diphenylpyridin-4-yl)phenol
-
11.5% inhibition at 0.1 mM
3-(2-phenyl-1-benzofuran-3-yl)prop-2-yn-1-yl 3-amino-2,3,6-trideoxy-b-D-arabino-hexopyranoside
-
77.8% inhibition at 0.1 mM
3-(2-phenyl-1-benzothiophen-3-yl)prop-2-yn-1-yl 3-amino-2,3,6-trideoxy-b-D-arabino-hexopyranoside
-
36.9% inhibition at 0.1 mM
3-(2-phenyl-1H-indol-3-yl)prop-2-yn-1-yl 3-amino-2,3,6-trideoxy-b-D-arabino-hexopyranoside
-
8.8% inhibition at 0.1 mM
3-(4,6-diphenylpyridin-2-yl)phenol
-
12.9% inhibition at 0.1 mM
3-(4-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)-phenoxy)propan-1-amine
-
-
3-(4-chlorophenyl)-1-(4'-hydroxyphenyl)-2-propen-1-one
-
chalcones (1,3-diaryl-2-propen-1-ones) are alpha, beta-unsaturated ketones with cytotoxic and anticancer properties. Compound has the highest Hammett and log P values (0.23 and 4.21, respectively) and exerted both highest cytotoxicity and strongest DNA topoisomerase I inhibition
3-(4-methylphenyl)-1-(4'-hydroxyphenyl)-2-propen-1-one
-
chalcones (1,3-diaryl-2-propen-1-ones) are alpha, beta-unsaturated ketones with cytotoxic and anticancer properties. Compound shows moderate interference with the DNA topoisomerase I
3-(4-phenyl-2,4'-bipyridin-6-yl)phenol
-
70.4% inhibition at 0.1 mM
3-(6-phenyl-2,2'-bipyridin-4-yl)phenol
-
10.8% inhibition at 0.1 mM
3-(6-phenyl-2,3'-bipyridin-4-yl)phenol
-
8.8% inhibition at 0.1 mM
3-(6-phenyl-2,4'-bipyridin-4-yl)phenol
-
60.8% inhibition at 0.1 mM
3-(imidazolyl-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline hydrochloride
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
3-(piperidin-1-yl)propyl-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
3-(pyrrolidin-1-yl)propyl-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
3-amino-4-chloro-9,10-dioxo-9,10-dihydroanthracene-2-sulfonic acid
-
-
3-amino-6-(3-aminopropyl)-5,6-dihydro-9-methoxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride
-
-
3-amino-6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
3-amino-6-(3-azidopropyl)-5,6-dihydro-9-methoxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
-
3-arylisoquinoline
-
-
3-bromo-11-hydroxy-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
3-bromopropyl 5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
3-cyano-5,11-dihydro-6-[3-(1H-imidazolyl)propyl]-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinoline
-
-
3-cyano-5,11-dihydro-6-[3-(dimethylamino)propyl]-5,11-dioxoindeno[1,2-c]isquinoline
-
-
3-cyano-6,11-dihydro-5,11-dioxo-6-(3-morpholinylpropyl)-5H-indeno[1,2-c]isoquinoline
-
-
3-cyano-6,11-dihydro-5,11-dioxo-6-[3-(dimethylamino)propyl]-5H-indeno[1,2-c]isoquinoline
-
-
3-iodo-9-methoxy-6-[3-(dimethylamino)propyl]-5H-indeno-[1,2-c]isoquinoline-5,11(6H)-dione
-
-
3-methoxy-5H-isoindolo[2,1-a]quinoxalin-6-one
-
-
3-morpholinopropyl-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
3-O-(benzenesulfonyloxy)-oleanolic acid
-
-
3-O-[N-(1-naphthyl)-carbamoyl]-17-beta-[N-(1-naphthyl)-carbamoyl]-oleanolic acid
-
-
3-O-[N-(1-naphthyl)-carbamoyl]-oleanolic acid
-
-
3-O-[N-(allyl)carbamoyl]-oleanolic acid
-
-
3-O-[N-(benzyl)carbamoyl]-17beta-O-[N-(benzyl)carbomyl]-oleanolic acid
-
-
3-O-[N-(benzyl)carbamoyl]-oleanolic acid
-
-
3-O-[N-(biphenyl)-p-carbamoyl]-oleanolic acid
-
-
3-O-[N-(phenylsulfonyl)-carbamoyl-17beta-N-(phenylsulfonyl)amide]-oleanolic acid
-
-
3-phenyl-1-(4'-hydroxyphenyl)-2-propen-1-one
-
chalcones (1,3-diaryl-2-propen-1-ones) are alpha, beta-unsaturated ketones with cytotoxic and anticancer properties. Compound shows moderate interference with the DNA topoisomerase I
3-thiiranylmethyloxy-1-hydroxy-5-azaxanthone
-
50% and 27% inhibition at 0.1 mM and 0.02 mM, respectively
3-[(1-azabicyclo[2.2.2]oct-3-ylamino)methyl]-4,11-dihydroxy-1H-naphtho[2,3-f]indole-5,10-dione
-
-
3-[(1-hydroxyethyl-piperazine)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
similar activity as the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
3-[(1-methylpiperazinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
weak activity
3-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoic acid hydrochloride
-
-
3-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)amino]-3-oxopropanoic acid
-
-
3-[(dimethylamino)methyl]-4,11-dihydroxy-1H-naphtho[2,3-f]indole-5,10-dione
-
-
3-[(morpholinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
3-[(thiomorpholinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
similar activity as the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
3-[1-[(4-methylphenyl)sulfonyl]-2-phenyl-1H-indol-3-yl]prop-2-yn-1-yl 3-amino-2,3,6-trideoxy-b-D-arabino-hexopyranoside
-
80.1% inhibition at 0.1 mM
3-[2-(furan-2-yl)-6-phenylpyridin-4-yl]phenol
-
48.8% inhibition at 0.1 mM
3-[2-phenyl-6-(thiophen-2-yl)pyridin-4-yl]phenol
-
9.1% inhibition at 0.1 mM
3-[2-phenyl-6-(thiophen-3-yl)pyridin-4-yl]phenol
-
6.9% inhibition at 0.1 mM
3-[4-phenyl-6-(thiophen-2-yl)pyridin-2-yl]phenol
-
51.2% inhibition at 0.1 mM
3-[4-phenyl-6-(thiophen-3-yl)pyridin-2-yl]phenol
-
75.8% inhibition at 0.1 mM
3-[6-(furan-2-yl)-4-phenylpyridin-2-yl]phenol
-
10.2% inhibition at 0.1 mM
4,11-bis([2-[(2-hydroxyethyl)amino]ethyl]amino)-1H-naphtho[2,3-f]indole-5,10-dione
-
-
4,11-bis[(2-aminoethyl)amino]-1H-naphtho[2,3-f]indole-5,10-dione
-
-
4,11-bis[[2-(dimethylamino)ethyl]amino]-1H-naphtho[2,3-f]indole-5,10-dione
-
-
4,11-bis{[2-(methylamino)ethyl]amino}-1H-naphtho[2,3-f]indole-5,10-dione
-
-
4,11-dihydroxy-3-[(4-methylpiperazin-1-yl)methyl]-1H-naphtho[2,3-f]indole-5,10-dione
-
-
4,4',4'',4'''-porphyrin-5,10,15,20-tetrayltetrabenzoic acid
-
-
4,4',4'',4'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis(4-methylmorpholin-4-ium) tetraiodide
-
-
4-(1H-benzo[d]imidazol-2-yl)phenol
-
-
4-(2-hydroxyethyl)-6-([2-[(2-hydroxyethyl)amino]ethyl]amino)-1,2,3,4-tetrahydronaphtho[2,3-f]quinoxaline-7,12-dione
-
-
4-(4,6-diphenylpyridin-2-yl)phenol
-
52.9% inhibition at 0.1 mM
4-(4-phenyl-2,3'-bipyridin-6-yl)phenol
-
44% inhibition at 0.1 mM
4-(5-chlorofuran-2-yl)-2-(3-chlorophenyl)-6-(3-methylthiophen-2-yl) pyridine
-
5.9% inhibition at 0.1 mM
4-(5-chlorofuran-2-yl)-2-(3-chlorophenyl)-6-(5-chlorothiophen-2-yl) pyridine
-
13% inhibition at 0.1 mM
4-(5-chlorofuran-2-yl)-2-(4-chlorophenyl)-6-(3-methylthiophen-2-yl) pyridine
-
5.1% inhibition at 0.1 mM
4-(5-chlorofuran-2-yl)-2-(5-chlorothiophen-2-yl)-6-(furan-2-yl) pyridine
-
23% inhibition at 0.1 mM
4-(5-chlorofuran-2-yl)-2-(5-chlorothiophen-2-yl)-6-p-tolylpyridine
-
14% inhibition at 0.1 mM
4-(5-chlorofuran-2-yl)-2-(furan-2-yl)-6-(3-methylthiophen-2-yl) pyridine
-
7.8% inhibition at 0.1 mM
4-(5-chlorofuran-2-yl)-6-(3-methylthiophen-2-yl)-2,3'-bipyridine
-
21% inhibition at 0.1 mM
4-(6-phenyl-2,4'-bipyridin-4-yl)phenol
-
57.5% inhibition at 0.1 mM
4-(furan-2-yl)-2-(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine
4-(furan-2-yl)-2-(thiophen-2-yl)-5H-chromeno [4,3-b]pyridine
-
9.2% inhibition at 0.1 mM
4-(furan-2-yl)-2-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
-
-
4-(furan-2-yl)-2-phenyl-5H-chromeno[4,3-b]pyridine
-
-
4-(furan-3-yl)-2-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
-
-
4-(furan-3-yl)-2-phenyl-5H-chromeno[4,3-b]pyridine
-
-
4-(furan-3-yl)-6-(thiophene-2-yl)-[2,4']-bipyridyl
-
shows moderate topoisomerase I inhibitory activities when compared to camptothecin
4-(furan-3-yl)-6-(thiophene-3-yl)-[2,4']-bipyridyl
-
shows moderate topoisomerase I inhibitory activities when compared to camptothecin
4-(pyridin-2-yl)-2-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
-
-
4-(pyridin-2-yl)-2-(thiophen-3-yl)-5H-chromeno[4,3-b]pyridine
-
3.3% inhibition at 0.1 mM
4-(thiophene-3-yl)-6-(thiophene-2-yl)-[2,2']-bipyridyl
-
shows significant topoisomerase I inhibitory activities at 20 microM and 100 microM concentration
4-(thiophene-3-yl)-6-(thiophene-2-yl)-[2,4']-bipyridyl
-
shows significant topoisomerase I inhibitory activities at 20 microM and 100 microM concentration
4-chloro-N-[5-imino-1-(quinoxalin-2-yl)-2,5-dihydro-1H-1,2,4-triazol-3-yl]-5-methyl-2-sulfanylbenzenesulfonamide
-
-
4-hydroxy-5-methoxy-1-nitroanthracene-9,10-dione
-
-
4-methyl-5H-isoindolo[2,1-a]quinoxalin-6-one
-
-
4-phenyl-2-(pyridin-2-yl)-5H-chromeno[4,3-b]pyridine
4-phenyl-2-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
4-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoic acid
-
-
4-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoic acid hydrochloride
-
-
4-[2-(furan-2-yl)-6-phenylpyridin-4-yl]phenol
-
5.0% inhibition at 0.1 mM
4-[4-phenyl-6-(thiophen-2-yl)pyridin-2-yl]phenol
-
4.9% inhibition at 0.1 mM
4-[4-phenyl-6-(thiophen-3-yl)pyridin-2-yl]phenol
-
20.4% inhibition at 0.1 mM
4-[5-(4-methyl-1-piperazinyl)-1H,1H'-2,5'-bibenzimidazol-2'-yl]phenol
-
Hoechst 33258
4-[6-(furan-2-yl)-4-phenylpyridin-2-yl]phenol
-
18.6% inhibition at 0.1 mM
4-[[(6-amino-3-methylpyrido[2,3-b]pyrazin-8-yl)amino]methyl]benzenesulfonamide
-
-
5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carbonitrile
-
-
5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylic acid
-
-
5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline-11-carbonitrile
-
-
5,12-dioxo-N-(2-(piperidin-1-yl)ethyl)-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
5,12-dioxo-N-(3-(piperidin-1-yl)propyl)-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
5,12-dioxo-N-(3-(pyrrolidin-1-yl)propyl)-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
5,12-dioxo-N-(3-phenylpropyl)-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
5,12-dioxo-N-phenethyl-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
5,9,11-trimethoxy-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
-
-
5-(4-ethylpiperazin-1-yl)-11H-indeno[1,2-c]isoquinolin-11-ol
-
-
5-(4-ethylpiperazin-1-yl)-11H-indeno[1,2-c]isoquinolin-11-one
-
-
5-(4-ethylpiperazin-1-yl)-11H-indeno[1,2-c]isoquinoline
-
-
5-(4-methyl-1,4-diazepan-1-yl)-11H-indeno[1,2-c]isoquinolin-11-one
-
-
5-(4-methyl-1,4-diazepan-1-yl)-11H-indeno[1,2-c]isoquinoline
-
-
5-(4-methylpiperazin-1-yl)-11H-indeno[1,2-c]isoquinolin-11-ol
-
-
5-(4-methylpiperazin-1-yl)-11H-indeno[1,2-c]isoquinolin-11-one
-
-
5-(4-methylpiperazin-1-yl)-11H-indeno[1,2-c]isoquinoline
-
-
5-(4-methylpiperazin-1-yl)-2-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H-benzo[d]imidazole
-
-
5-(butylamino)-11H-indeno[1,2-c]isoquinolin-11-one
-
-
5-(morpholin-4-yl)-11H-indeno[1,2-c]isoquinolin-11-ol
-
-
5-(morpholin-4-yl)-11H-indeno[1,2-c]isoquinolin-11-one
-
-
5-(morpholin-4-yl)-11H-indeno[1,2-c]isoquinolin-11-yl acetate
-
-
5-(morpholin-4-yl)-11H-indeno[1,2-c]isoquinoline
-
-
5-(piperazin-1-yl)-11H-indeno[1,2-c]isoquinolin-11-one
-
-
5-deoxy-5-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-arabinitol
-
-
5-phenyl-2'-(indolo-6-yl)bibenzimidazole
-
5P2'IBB
5-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoic acid
-
-
5-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoic acid hydrochloride
-
-
6'-(thiophene-2-yl)-[3,4',2',4'']-terpyridine
-
shows moderate topoisomerase I inhibitory activities when compared to camptothecin
6'-(thiophene-2-yl)-[4,2',4',4'']-terpyridine
-
shows moderate topoisomerase I inhibitory activities when compared to camptothecin
6-(1-hydroxypropan-2-yl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(2,3-dihydroxypropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(2-hydroxypropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-(1H-imidazol-1-yl)propyl)-8-methoxy-3-nitro-5Hindeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-amino-2-hydroxypropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-3-(methylamino)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline hydrochloride
-
-
6-(3-aminopropyl)-5,6-dihydro-9-methoxy-3-iodo-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
-
6-(3-aminopropyl)-7-methoxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-9-methoxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-azidopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
-
6-(3-bromopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
-
6-(3-homopiperazinyl-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-(3-hydroxy-2-oxopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-hydroxypropyl)-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-piperazinyl-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride
-
similar activity as the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-(3-thiazolylamino-1-propyl)-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-(4-methylpiperazin-1-yl)-2'-(4-(10-(prop-2-ynyloxy)-decyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
-
6-(4-methylpiperazin-1-yl)-2'-(4-(12-(prop-2-ynyloxy)-dodecyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
-
6-(4-methylpiperazin-1-yl)-2'-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
-
6-(4-methylpiperazin-1-yl)-2'-(4-(8-(prop-2-ynyloxy)-octyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
-
-
6-(4-methylpiperazin-1-yl)-2-(4-(2-(4-(oct-7-ynyl)-1H-1,2,3-triazol-1-yl)ethoxy)phenyl)-1H-benzo[d]imidazole
-
-
6-(4-methylpiperazin-1-yl)-2-[4-[(prop-2-yn-1-yl)oxy]phenyl]-1H-benzimidazole
-
-
6-(4-methylpiperazine-1-carbonyl)indolizino[2,3-g]quinoline-5,12-dione
-
-
6-(furan-2-yl)-4-(furan-3-yl)-[2,2']-bipyridyl
-
shows moderate topoisomerase I inhibitory activities when compared to camptothecin
6-(furan-2-yl)-4-(furan-3-yl)-[2,4']-bipyridyl
-
shows moderate topoisomerase I inhibitory activities when compared to camptothecin
6-(furan-2-yl)-4-(thiophene-2-yl)-[2,4']-bipyridyl
-
shows significant topoisomerase I inhibitory activities at 20 microM and 100 microM concentration
6-(furan-2-yl)-4-(thiophene-3-yl)-[2,4']-bipyridyl
-
shows moderate topoisomerase I inhibitory activities when compared to camptothecin
6-(furan-2-yl)-[3,4',2',4'']-terpyridine
-
shows significant topoisomerase I inhibitory activities at 20 microM and 100 microM concentration
6-(morpholine-4-carbonyl)indolizino[2,3-g]quinoline-5,12-dione
-
-
6-(piperidine-1-carbonyl)indolizino[2,3-g]quinoline-5,12-dione
-
-
6-acetyl-7-amino-indolizino[2,3-g]quinoline-5,12-dione
-
-
6-acetyl-7-bromo-indolizino[2,3-g]quinoline-5,12-dione
-
-
6-acetyl-7-chloro-indolizino[2,3-g]quinoline-5,12-dione
-
-
6-acetyl-7-fluoro-indolizino[2,3-g]quinoline-5,12-dione
-
-
6-acetyl-7-hydroxy-indolizino[2,3-g]quinoline-5,12-dione
-
-
6-acetylindolizino[2,3-g]quinoline-5,12-dione
-
-
6-methylindolizino[2,3-g]quinoline-5,12-dione
-
-
6-N-(1-hydroxymethyl-2-hydroxy)ethylamino-12,13-dihydro-2,10-dihydroxy-13-(beta-D-glucopyranosyl)-5H-indolo[2,3-a]-pyrrolo[3,4-c]-carbazole-5,6(6H)-dione
-
also effective against cancer cells with P-glycoprotein-mediated resistance to adriamycin or taxol
6-N-formylamino-12,13-dihydro-1,11-dihydroxy-13-(beta-D-glucopyranosyl)-5G-indolo(2,3-a)pyrrolo(3,4-c)carbarole-5,7(6H)-dione
-
more potent than camptothecin for inhibiting the top1-mediated religation step
6-[(2-chlorobenzyl)sulfanyl]-9-(beta-L-ribofuranosyl)-9H-purin-2-amine
-
-
6-[(2R)-1-hydroxypropan-2-yl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-[(2R)-2,3-dihydroxypropyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-[(2R)-2-hydroxypropyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-[(2S)-1-hydroxypropan-2-yl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-[(2S)-2,3-dihydroxypropyl]-2,3-dimethoxy-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-[(2S)-2,3-dihydroxypropyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-[(2S)-2-hydroxypropyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-[(3-morpholylethylamino)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoic acid
-
-
6-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoic acid hydrochloride
-
-
6-[3-(1H-imidazol-1-yl)propyl]-2,3-dimethoxy-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-[3-(1H-imidazol-1-yl)propyl]-2,3-dimethoxy-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
6-[3-(1H-imidazol-1-yl)propyl]-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione hydrochloride
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-[3-(1H-imidazol-1-yl)propyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-[3-(3-hydroxypiperidinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline hydrochloride
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-[3-(4-aminopiperidinyl)-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride
-
weak activity
6-[3-pyrazolyl-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
similar activity as the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
6-[3-[(2-hydroxyethyl)amino]propyl]-2,3-dimethoxy-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
6-[3-[2-(1,2,4)]-triazolyl-1-propyl]-5,6-dihydro-2,3-dimethoxy-8,9-methylenedioxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline hydrochloride
-
higher activity than the parent compound 2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
7-(2-furoyl)-10-methoxyhomocamptothecin
-
-
7-(2-naphthoyl)-10-methoxyhomocamptothecin
-
-
7-(2-thenoyl)-10-methoxyhomocamptothecin
-
-
7-(3,5-dimethylbenzoyl)-10-methoxyhomocamptothecin
-
-
7-(4-chlorbenzoyl)-10-methoxyhomocamptothecin
-
-
7-(4-fluorobenzoyl)-10-methoxyhomocamptothecin
-
-
7-(4-methoxylbenzoyl)-10-methoxyhomocamptothecin
-
-
7-(4-toluyl)-10-methoxyhomocamptothecin
-
-
7-(4-triflouromethylbenzoyl)-10-methoxyhomocamptothecin
-
-
7-benzoyl-10-methoxyhomocamptothecin
-
-
7-butyryl-10-methoxyhomocamptothecin
-
-
7-cyclohexyl-10-methoxyhomocamptothecin
-
-
7-cyclohexylcabonyl-10-methoxyhomocamptothecin
-
-
7-cyclopentyl-10-methoxyhomocamptothecin
-
-
7-cyclopentylcabonyl-10-methoxyhomocamptothecin
-
-
7-cyclopropylcabonyl-10-methoxyhomocamptothecin
-
-
7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxy-camptothecin
-
strong synergism between irinotecan and 5-fluorouracil
7-heptanoyl-10-methoxyhomocamptothecin
-
-
7-isobutyryl-10-methoxyhomocamptothecin
-
-
7-ketoroyleanone
-
diterpenoid from Orthosiphon wulfenioides
7-pentanoyl-10-methoxyhomocamptothecin
-
-
7-propionyl-10-methoxyhomocamptothecin
-
-
8,9-dimethoxy-5-(2-N,N-dimethylaminoethyl)-2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-one
-
i.e. ARC-111
8,9-dimethoxy-5-(2-N-methylaminoethyl)-2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-one
-
i.e. Genz-644282
8-bromo-9-cyano-7-(alpha-L-xylofuranosyl)-3,7-dihydroimidazo[1,2-c]pyrrolo[3,2-e]pyrimidin-4-ium
-
-
8-methoxy-6-(3-morpholinopropyl)-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
9,9'-[butane-1,4-diylbis(oxy)]bis(10-methoxy-5,6-dihydro[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium) dichloride
-
synthetic protoberberine alkaloid, highly active
9,9'-[ethane-1,2-diylbis(oxy)]bis(10-methoxy-5,6-dihydro[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium)dichloride
-
synthetic protoberberine alkaloid, highly active
9,9'-[heptane-1,7-diylbis(oxy)]bis(10-methoxy-5,6-dihydro[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium) dichloride
-
synthetic protoberberine alkaloid, highly active
9,9'-[hexane-1,6-diylbis(oxy)]bis(10-methoxy-5,6-dihydro[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium) dichloride
-
synthetic protoberberine alkaloid, highly active
9,9'-[pentane-1,5-diylbis(oxy)]bis(10-methoxy-5,6-dihydro[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium) dichloride
-
synthetic protoberberine alkaloid, highly active
9,9'-[propane-1,3-diylbis(oxy)]bis(10-methoxy-5,6-dihydro[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium) dichloride
-
synthetic protoberberine alkaloid, highly active. Strongly stabilize the enzyme-DNA binary complex at low concentration (50–100microM). From 0.1 to 1 mM, their ability to stabilize is weak
9-aminoacridine
-
acts as Top1 poison
9-O-(2-aminoethyl)berberine
-
synthetic protoberberine alkaloid
9-O-(2-hydroxyethyl)berberine
-
synthetic protoberberine alkaloid
9-O-[2-(1H-imidazol-1-yl)ethyl]berberine
-
synthetic protoberberine alkaloid
9-O-[2-(4-methylpiperazin-1-yl)ethyl]berberine
-
synthetic protoberberine alkaloid
actinomycin D
-
traps topoisomerase I-DNA covalent complexes
adriamycin
-
-
aesculioside IIa
-
-
aesculioside IIb
-
-
aesculioside IIc
-
-
aesculioside IId
-
-
aesculioside IIIa
-
-
aesculioside IIIb
-
-
aesculioside IIIc
-
-
aesculioside IIId
-
-
aesculioside IIIe
-
-
aesculioside IIIf
-
-
aesculioside IV-23C1
-
-
aesculioside IV-23D1
-
-
aesculioside IV-23E
-
-
aesculioside IVa
-
-
aesculioside IVb
-
-
aesculioside IVc
-
-
Aminocatechol A-3253
-
Candida enzyme is more susceptible than the human enzyme
amsacrine
-
-
antofine
-
alkaloid from Cynanchum komarovii
ARC-111
-
-
batracylin
-
-
belotecan
-
-
Berberine
berberrubine
-
natural protoberberine alkaloid
beta-lapachone
-
-
beta-octabromo-meso-tetra(4-carboxyl)phenyl porphyrin
-
-
beta-octaphenyl-meso-tetra(4-carboxyl)phenyl porphyrin
-
-
bis(2,2-dichloro-6-[[2-(hydroxy-kO)benzylidene]amino-kN]-4H-1,3,2-benzodioxastannin-4-onato)copper(2+)
-
-
bis(2-hydroxy-5-[[2-(hydroxy-kO)benzylidene]amino-kN]benzoato)copper(2+)
-
-
bis(5,6-dimethyl-1H-benzo[d]imidazol-2-yl)methane
-
-
bis(5-methyl-1H-benzo[d]imidazol-2-yl)methane
-
-
bulgarein
-
stabilize inactive Top1cc
calothrixins
-
weak inhibitors of Top1
camptothecin
camptothecine
-
-
camptothecins
-
-
chelerythrine
-
-
chrysin 6-C-beta-D-glucopyranosyl 8-C-alpha-L-arabinopyranoside
-
flavonoid from Scutellaria amoena
cis-2',5,7-trihydroxyflavanonol 3-O-beta-D-glucopyranoside
-
flavonoid from Scutellaria amoena
cisplatin
-
presence of DNA adducts of bifunctional antitumor cisplatin or monodentate [PtCl(dien)]Cl in the substrate DNA inhibits eukaryotic top1 action, the adducts of cisplatin being more effective
colcemid
-
microtubule inhibitor, arrests cells in M phase, followed by induction of apotosis, 1 and 5 ng/ml colcemid display only modest cytotoxic effects. 10, 50 and 100 ng/ml induce pronounced cell death as measured by flow cytometry analysis
coptisine
-
natural protoberberine alkaloid
coralyne
-
potent and selective Top1 inhibitor
corypalline
-
moderate inhibition
CPT-11
-
-
dehydrocavidine
-
moderate inhibition
dehydrocheilanthifoline
-
moderate inhibition
dehydrodiscretamine
-
moderate inhibition
diaqua(2,2'-diamino-4,4'-bi-1,3-thiazole)oxosulfato-vanadium(IV) tetrahydrate
-
-
-
diflomotecan
-
-
dihydrobenzo[a]acridines
-
-
-
dihydrotanshinone I
-
diterpenoid from Salvia castanea f. tomentos
diospyrin
-
promotes protein conformational changes that can affect the kinase activity of Top1 altering SR protein phosphorylation and alternative splicing
distamycin A
-
-
doxorubicin
ecteinascidin 743
-
-
edotecarin
-
-
epirubicin
-
-
erybraedin C
-
binds irreversibly to the enzyme alone, probably in proximity of the active site, without abolishing enzyme binding to the DNA
ethoxidine
-
-
ethyl 10-amino-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
-
-
ethyl 10-bromo-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
-
-
ethyl 10-chloro-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
-
-
ethyl 10-fluoro-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
-
-
ethyl 10-hydroxy-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
-
-
ethyl 10-methyl-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
-
-
ethyl 2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]acetate hydrochloride
-
-
ethyl 2-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]acetate
-
-
ethyl 5,12-dioxo-5,12-dihydroindolizino[2,3-g]isoquinoline-6-carboxylate
-
-
ethyl 5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
-
-
ethyl 5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate
-
-
ethyl 5,12-dioxo-5,12-dihydroindolizino[3,2-g]isoquinoline-11-carboxylate
-
-
ethyl 5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
-
-
ethyl 6,11-dioxo-6,11-dihydrobenzo[f]-pyrido[1,2-alpha]indole 12-carboxylate
-
-
ethyl 7-amino-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
-
-
ethyl 7-bromo-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
-
-
ethyl 7-chloro-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
-
-
ethyl 7-fluoro-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
-
-
ethyl 7-hydroxy-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
-
-
ethyl 7-methyl-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
-
-
evodiamine
-
EVO, an alkaloidal compound isolated from Evodia rutaecarpa, is able to inhibit supercoiled plasmid DNA relaxation catalyzed by TopI by stabilizing topoisomerase I-DNA cleavable complex
fagaronine
-
-
feruloyl agmatine
-
moderate inhibition
flavopiridol
-
-
fomitellic acid A
-
0.1 mM, 85% inhibition, IC50: 0.06 mM
fomitellic acid B
-
0.1 mM, 85% inhibition
gemcitabine
-
nucleoside analogue
GENZ-644282
-
-
gimatecan
-
-
glutathione S-transferase-Par-4
-
-
-
gold(III) complex
-
-
-
Heliquinomycin
-
at 0.1 mg/ml
heparin
-
-
Hoechst 33258
-
-
Hoechst 33342
-
-
homocamptothecin
-
-
indenoisoquinoline
-
-
indeno[1,2-c]isoquinolinone
-
-
indimitecan
-
-
indolizino[2,3-g]quinoline-5,12-dione
-
-
indolizino[3,2-g]quinoline-5,12-dione
-
-
indotecan
-
-
irinotecan
isodiospyrin
-
inhibits by direct binding to htopo I, inhibits relexation activity and kinase activity, antagonizes camptothecin-induced DNA cleavage by htopo I
IT-101
-
-
Jatrorrhizine
-
natural protoberberine alkaloid
jatrorubine
-
natural protoberberine alkaloid
JDC-108
-
-
KCl
-
above 100 mM
lamellarin D
-
stabilize inactive Top1cc
methyl (7aS,12aS)-5-methylidene-13-oxo-5,7a,12a,13-tetrahydro-7H-[1]benzofuro[3,2-c]benzo[g]chromene-9-carboxylate
-
-
methyl 2-(4-Hydroxyphenyl)-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazole-4-carboxylate
-
-
methyl 2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetate
-
-
methyl 2-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetate
-
-
methyl 3-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate
-
-
methyl 3-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate
-
-
methyl 3-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate
-
-
methyl 4-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate
-
-
methyl 4-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate
-
-
methyl 4-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate
-
-
methyl 5-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate
-
-
methyl 5-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate
-
-
methyl 5-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate
-
-
methyl 6-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoate
-
-
methyl 6-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoate
-
-
methyl N-[(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)acetyl]glycinate
-
-
methyl [[5-carbamoyl-6-(methylsulfanyl)-4-oxo-3-phenyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl]sulfanyl]acetate
-
-
monodentate [PtCl(diethylenetriamine)]Cl
-
presence of DNA adducts of bifunctional antitumor cisplatin or monodentate [PtCl(dien)]Cl in the substrate DNA inhibits eukaryotic top1 action, the adducts of cisplatin being more effective. Inhibition is markedly enhanced by camptothecin. Sequence preference of Pt-DNA adducts in the 161-bp substrate DNA fragment. Inhibition mechanism and interaction analysis, overview
morpholinodoxorubicin
-
traps topoisomerase I-DNA covalent complexes
N,N',N'',N'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis(2-hydroxy-N,N-dimethylethanaminium) tetrabromide
-
-
N,N',N'',N'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis(N,N-dimethylanilinium) tetrabromide
-
-
N,N',N'',N'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis(N-ethyl-N-methylethanaminium) tetrabromide
-
-
N,N',N'',N'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis[2-hydroxy-N-(2-hydroxyethyl)-N-methylethanaminium] tetrabromide
-
-
N,N-diethyl-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N,N-diethyl-9-([2-(1H-indol-3-yl)ethyl]amino)acridine-3-carboxamide
-
-
N-(2-(1H-imidazol-1-yl)ethyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-(2-(4-methylpiperazin-1-yl)ethyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-(2-(dimethylamino)ethyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-(2-(pyrrolidin-1-yl)ethyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-(2-morpholinoethyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-(3-(4-methylpiperazin-1-yl)propyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-(3-(diethylamino)propyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-(3-(dimethylamino)propyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-(3-morpholinopropyl)-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-butyl-11H-indeno[1,2-c]isoquinolin-5-amine
-
-
N-ethyl-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxamide
-
-
N-[1-benzyl-2-(4-ethylpiperazin-1-yl)-2-oxoethyl]-2-(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)acetamide
-
-
N-[1-[(4-ethylpiperazin-1-yl)carbonyl]-3-methylbutyl]-2-(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)acetamide
-
-
N-[2-(Dimethylamino)ethyl]acridine-4-carboxamide
-
-
N-[2-(Dimethylamino)ethyl]carboxamide derivatives of fused tetracyclic quinolines and quinoxalines
-
-
-
N-[6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide
-
-
N-[6-(3-azidopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide
-
-
N-[6-(3-hydroxypropyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide
-
-
N-[9-acetyl-6-(benzylsulfanyl)-9H-purin-2-yl]acetamide
-
-
NaCl
-
above 100 mM
nick-containing oligonucleotides
-
inhibit DNA substrate relaxation. Synthesis of and enzyme inhibition by a series of oligonucleotides with various lengths that contain nick and topoisomerase I-binding sites, sequences, overview. The position of the nick as well as the length of the oligonucleotides are crucial factors for the inhibition of the nuclear enzyme
-
nick-containing oligonucleotides s
-
inhibit DNA substrate relaxation. Synthesis of and enzyme inhibition by a series of oligonucleotides with various lengths that contain nick and topoisomerase I-binding sites, sequences, overview. The position of the nick as well as the length of the oligonucleotides are crucial factors for the inhibition of the nuclear enzyme
-
nitidine
-
-
novobiocin
-
inhibits the ATPase activity
NSC 314622
-
cytotoxicity results of its direct action upon topoisomerase 1 in cells
NSC 725776
-
-
NSC 743400
-
-
NSC 88915
-
-
NSC-724998
-
-
NSC-725776
-
-
NU/ICRF 505
-
-
oleanderolide
-
-
oleanolic acid
-
-
oligo-1,3-thiazolecarboxamides
-
-
-
palmatine
palmatrubine
-
natural protoberberine alkaloid
Par-4
-
tumor suppressor protein, prostate apoptosis response-4, binds to TOP1, via its leucine zipper domain, and prevents TOP1 interaction with the DNA
-
Par-4-GFP
-
-
-
phthalascidin
-
-
platinum(II) complex
-
-
-
plukenetione A
-
can inhibit the unwinding activity of Top1
pyrazoloacridine
-
completely suppresses the ability of topoisomerase I to relax supercoiled DNA at a concentration of 0.008 mM, inhibits the enzyme without trapping cleavable complexes
saintopin
-
-
Selenite
-
selenite induces topoisomerase I-DNA complexes in K562 cells
SN-38
SN38
-
enzyme linker fluctuations can have an impact on SN38 binding by reducing the enzyme affinity for the drug. TOP1 mutations are involved in the development of SN38 resistance
SR proteins
-
inhibition of DNA nicking activity by SR proteins. Inhibition of the DNA nicking activity of Topo I by SRSF1 depends on RNA recognition motifs joined by a spacer, Topo I enzyme inhibition by spacer mutants, overview
-
ST1968
-
-
-
tafluposide
-
-
Tax oncoprotein
-
from HTLV-1, inhibits DNA binding of topoisomerase I, which is the first step of the reaction catalyzed by the enzyme
-
taxol
-
-
tert-butyl 3-(4-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]-imidazol-2-yl)phenoxy)propylcarbamate
-
-
thaspine
-
-
thiazole-containing oligopeptides
-
inhibitory effect increases with the number of thiazole units. Inhibitory properties of thiazole-containing oligopeptides containing 3 or 4 thiazole units are 3-10tímes better than those of distamycin A
-
thiocamptothecin
-
-
topopyrone
-
-
topopyrone A
-
-
topopyrone B
-
-
topopyrone C
-
-
topopyrone D
-
-
topotecan
Tumor necrosis factor alpha
-
TNFalpha induces receptor-mediated apotosis. Receptor-mediated apoptosis induced by TNFalpha results in a very strong htopoI damage response, further indicating a general involvement of htopoI in apoptosis
-
ursolic acid
-
complete inhibition above 0.2 mM, IC50: 0.25 mM
versixanthone G
-
-
versixanthone H
-
-
versixanthone I
-
-
versixanthone J
-
-
versixanthone K
-
-
versixanthone L
-
-
versixanthone M
-
-
vincristine
-
-
winchic acid
-
triterpenoid from Winchia calophylla
XMT-1001
-
-
zinc bis(2-[(E)-[(2,2-dichloro-4-oxo-4H-1,3,2-benzodioxastannin-6-yl)imino]methyl]phenolate)
-
-
zinc bis(2-[(E)-[(3-carboxy-4-hydroxyphenyl)imino]methyl]phenolate)
-
-
[2,2',2'',2''',2'''',2''''',2''''''-([24-((2-[diethyl(methyl)ammonio]ethyl)sulfanyl)-14,19-dihydro-29H,31H-tetrabenzoporphine-2,3,9,10,16,17,23-heptayl-k4N29,N30,N31,N32]heptasulfanediyl)heptakis(N,N,N-trimethylethanaminiumato)(2-)]zinc(8+) octaiodide
-
-
[3-[(E)-2-carboxyethenyl]phenyl](dihydroxy)oxoantimonate(2-)
-
partial or complete inhibition of hTopo is only observed at relatively high compound concentrations in the range 5 to 20 microM
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
D-galactose
-
D-glucose
-
1-ethylKuQuinone
-
synthesis of the pentacyclic-diquinoid synthetic compound, overview. It efficiently inhibits the cleavage step of the enzyme reaction fitting well into the catalytic site. When incubated with the binary topoisomerase-DNA cleaved complex, the compound helps the enzyme to remove itself from the cleaved DNA and close the DNA gap, increasing the religation rate. The compound also induces the religation of the stalled enzyme-camptothecin-DNA ternary complex. The religation enhancement is due to the presence on the compound of two oxygen atoms that act as hydrogen acceptors. This property facilitates the deprotonation of the 5 DNA end. Docking and molecular modeling, overview
antimycin A
-
-
BH3I-2'
-
-
glycerol
-
high concentrations increase the efficiency of the DNA relaxation reaction
histone H1
-
stimulates
-
Nonhistone HMG proteins
-
stimulates
-
tumor necrosis factor-related apoptosis-inducing ligand
-
TRAIL
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
additional information
-
kinetic analysis, overview
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000063
camptothecin
-
with 0.63 microM camptothecin or more numerous shifted htopoI bands detected
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.02149
tanshinone-1
Homo sapiens
at pH 8.0 and 37°C
0.00323
(S)-camptothecin
Homo sapiens
-
-
0.01029 - 0.0158
11-acetyl-10-amino-indolizino[3,2-g]quinoline-5,12-dione
0.0002 - 0.0124
11-acetyl-10-bromo-indolizino[3,2-g]quinoline-5,12-dione
0.0015 - 0.022
11-acetyl-10-chloro-indolizino[3,2-g]quinoline-5,12-dione
0.00139 - 0.0127
11-acetyl-10-fluoro-indolizino[3,2-g]quinoline-5,12-dione
0.0163
11-acetyl-10-hydroxy-indolizino[3,2-g]quinoline-5,12-dione
Homo sapiens
-
for GLC-82 cells
0.0014 - 0.01471
11-acetylindolizino[3,2-g]quinoline-5,12-dione
0.0055
11-hydroxy-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
Homo sapiens
-
-
0.0091
11-hydroxy-2-methyl-8-nitro-4H-naphtho[2,3-h]chromene-4,7,12-trione
Homo sapiens
-
-
0.00706
11-hydroxy-2-phenyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
Homo sapiens
-
-
0.0215
11-methylindolizino[3,2-g]quinoline-5,12-dione
Homo sapiens
-
for GLC-82 cells
0.00715
11-[2-(dimethylamino)ethoxy]-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
Homo sapiens
-
-
0.05
2'-[4-([6-[(but-3-yn-1-yl)oxy]hexyl]oxy)phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
Homo sapiens
-
IC50 above 0.05 mM, pH and temperature not specified in the publication
0.2541
2'-[4-[(but-3-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.05
2'-[4-[(heptadec-16-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
Homo sapiens
-
IC50 above 0.05 mM, pH and temperature not specified in the publication
0.05
2'-[4-[(hex-5-yn-1-yl)oxy]phenyl]-6-(4-methylpiperazin-1-yl)-1H,3'H-2,5'-bibenzimidazole
Homo sapiens
-
IC50 above 0.05 mM, pH and temperature not specified in the publication
0.05
2-(4-[[1-(6-azidohexyl)-1H-1,2,3-triazol-4-yl]methoxy]phenyl)-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
Homo sapiens
-
IC50 above 0.05 mM, pH and temperature not specified in the publication
0.00266 - 0.00511
2-(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)-N-[2-methyl-1-(morpholin-4-ylcarbonyl)propyl]acetamide
0.00126 - 0.00223
2-(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)-N-[3-methyl-1-[(4-methylpiperazin-1-yl)carbonyl]butyl]acetamide
0.00495
3,10-dibromo-11-hydroxy-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
Homo sapiens
-
-
0.0065
3-bromo-11-hydroxy-2-methyl-4H-naphtho[2,3-h]chromene-4,7,12-trione
Homo sapiens
-
-
0.0015
4,11-bis[(2-aminoethyl)amino]-1H-naphtho[2,3-f]indole-5,10-dione
Homo sapiens
-
IC50 values 0.0005 mM to 0.0015 mM for 4,11-bis([2-[(2-hydroxyethyl)amino]ethyl]amino)-1H-naphtho[2,3-f]indole-5,10-dione, 0.0015 mM to 0.0035 mM for 4,11-bis[[2-(methylamino)ethyl]amino]-1H-naphtho[2,3-f]indole-5,10-dione, above 0.0035 mM for 4,11-bis[[2-(dimethylamino)ethyl]amino]-1H-naphtho[2,3-f]indole-5,10-dione
0.01175
4,4',4'',4'''-porphyrin-5,10,15,20-tetrayltetrabenzoic acid
Homo sapiens
-
-
0.16
4-hydroxy-5-methoxy-1-nitroanthracene-9,10-dione
Homo sapiens
-
-
0.05
6-(4-methylpiperazin-1-yl)-2'-(4-(10-(prop-2-ynyloxy)-decyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
Homo sapiens
-
IC50 above 0.05 mM, pH and temperature not specified in the publication
0.05
6-(4-methylpiperazin-1-yl)-2'-(4-(12-(prop-2-ynyloxy)-dodecyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
Homo sapiens
-
IC50 above 0.05 mM, pH and temperature not specified in the publication
0.05
6-(4-methylpiperazin-1-yl)-2'-(4-(6-(prop-2-ynyloxy)-hexyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
Homo sapiens
-
IC50 above 0.05 mM, pH and temperature not specified in the publication
0.05
6-(4-methylpiperazin-1-yl)-2'-(4-(8-(prop-2-ynyloxy)-octyloxy)phenyl)-1H,3'H-2,5'-bibenzo[d]imidazole
Homo sapiens
-
IC50 above 0.05 mM, pH and temperature not specified in the publication
0.0122 - 0.0223
6-acetyl-7-amino-indolizino[2,3-g]quinoline-5,12-dione
0.00021 - 0.0117
6-acetyl-7-bromo-indolizino[2,3-g]quinoline-5,12-dione
0.00019 - 0.00783
6-acetyl-7-chloro-indolizino[2,3-g]quinoline-5,12-dione
0.00017 - 0.00526
6-acetyl-7-fluoro-indolizino[2,3-g]quinoline-5,12-dione
0.0176 - 0.02485
6-acetyl-7-hydroxy-indolizino[2,3-g]quinoline-5,12-dione
0.00086 - 0.00792
6-acetylindolizino[2,3-g]quinoline-5,12-dione
0.0122 - 0.0142
6-methylindolizino[2,3-g]quinoline-5,12-dione
0.109
aesculioside IIa
Homo sapiens
-
-
0.118
aesculioside IIb
Homo sapiens
-
-
0.111
aesculioside IIc
Homo sapiens
-
-
0.024
aesculioside IId
Homo sapiens
-
-
0.119
aesculioside IIIa
Homo sapiens
-
-
0.16
aesculioside IIIb
Homo sapiens
-
-
0.132
aesculioside IIIc
Homo sapiens
-
-
0.049
aesculioside IIId
Homo sapiens
-
-
0.045
aesculioside IIIe
Homo sapiens
-
-
0.054
aesculioside IIIf
Homo sapiens
-
-
0.053
aesculioside IV-23C1
Homo sapiens
-
-
0.027
aesculioside IV-23D1
Homo sapiens
-
-
0.033
aesculioside IV-23E
Homo sapiens
-
-
0.052
aesculioside IVa
Homo sapiens
-
-
0.036
aesculioside IVb
Homo sapiens
-
-
0.05
aesculioside IVc
Homo sapiens
-
-
0.00234
beta-octabromo-meso-tetra(4-carboxyl)phenyl porphyrin
Homo sapiens
-
-
0.0034
beta-octaphenyl-meso-tetra(4-carboxyl)phenyl porphyrin
Homo sapiens
-
-
0.025
camptothecin
Homo sapiens
-
at pH 7.5 and 25°C
0.00009 - 0.0002
epirubicin
0.019 - 0.0235
ethyl 10-amino-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
0.0011 - 0.0208
ethyl 10-bromo-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
0.0022 - 0.0199
ethyl 10-chloro-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
0.0012 - 0.0062
ethyl 10-fluoro-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
0.0233 - 0.0238
ethyl 10-hydroxy-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
0.00927 - 0.01165
ethyl 10-methyl-5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
0.00088 - 0.00096
ethyl 5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
0.0019 - 0.01445
ethyl 5,12-dioxo-5,12-dihydroindolizino[3,2-g]quinoline 11-carboxylate
0.01643 - 0.02341
ethyl 7-amino-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
0.002 - 0.0103
ethyl 7-bromo-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
0.0021 - 0.00737
ethyl 7-chloro-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
0.00137 - 0.00701
ethyl 7-fluoro-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
0.0072
ethyl 7-hydroxy-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
Homo sapiens
-
for GLC-82 cells
0.00022 - 0.0145
ethyl 7-methyl-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline 6-carboxylate
0.0018 - 0.0099
etoposide
0.00602
evodiamine
Homo sapiens
-
-
0.06
fomitellic acid A
Homo sapiens
-
0.1 mM, 85% inhibition, IC50: 0.06 mM
0.02286
Hoechst 33258
Homo sapiens
-
at pH 7.9 and 37°C
0.005
Hoechst 33342
Homo sapiens
-
IC50 above 0.05 mM, at pH 7.9 and 37°C
0.0115 - 0.01697
indolizino[2,3-g]quinoline-5,12-dione
0.0123 - 0.0202
indolizino[3,2-g]quinoline-5,12-dione
0.00668 - 0.00744
JDC-108
0.00213 - 0.00288
methyl N-[(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)acetyl]glycinate
0.00109 - 0.00288
N-[1-benzyl-2-(4-ethylpiperazin-1-yl)-2-oxoethyl]-2-(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)acetamide
0.00244 - 0.00794
N-[1-[(4-ethylpiperazin-1-yl)carbonyl]-3-methylbutyl]-2-(6-methyl-5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)acetamide
0.0000063
nick-containing oligonucleotide, nick-containing oligonucleotides
Homo sapiens
-
-
-
0.00002 - 0.047
NSC 725776
0.00006 - 0.047
NSC 743400
0.00002 - 0.0034
SN-38
0.0295
topopyrone C
Homo sapiens
-
-
0.00118
topotecan
Homo sapiens
-
-
0.25
ursolic acid
Homo sapiens
-
complete inhibition above 0.2 mM, IC50: 0.25 mM
additional information
additional information
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5
assay at
7.4
-
assay at
8.6
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
assay at
20
-
assay at
23
-
cleavage assay at
25
-
assay at
30
-
assay at
37 - 45
-
-
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25 - 37
-
The effects of ATP/Mg2+ and temperature on the ability of E1 to bind origin DNA in the presence and absence of Topo I is shown. Increasing amounts of E1 were incubated with radiolabeled PV origin DNA at 37°C or 25°C in the presence or absence of ATP/Mg2+
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
renal cancer cell line
Manually annotated by BRENDA team
-
renal cancer cell line
Manually annotated by BRENDA team
-
human immortalized epithelial cells
Manually annotated by BRENDA team
-
breast cancer cell line
Manually annotated by BRENDA team
-
Caco-2 cells have eight copies of the hTOPI gene, they show twofold more hTopI protein, and twofold higher activity of hTopI compared to HT-29 cells, but similar camptothecin sensitivity
Manually annotated by BRENDA team
-
renal cancer cell line
Manually annotated by BRENDA team
-
leukemia cell line
Manually annotated by BRENDA team
-
colon cancer cell line
Manually annotated by BRENDA team
-
from patients receiving adjuvant 5-fluorouracil-based chemotherapy
Manually annotated by BRENDA team
-
nonsmall cell lung cancer cell line
Manually annotated by BRENDA team
-
colon cancer cell line
Manually annotated by BRENDA team
-
human primary lung fibroblasts
Manually annotated by BRENDA team
-
htopoI obtained from HeLa S3 cells
Manually annotated by BRENDA team
-
bipotent hemopoietic stem cells
Manually annotated by BRENDA team
-
leukemia cell line
Manually annotated by BRENDA team
-
nonsmall cell lung cancer cell line
Manually annotated by BRENDA team
-
nonsmall cell lung cancer cell line
Manually annotated by BRENDA team
-
breast cancer cell line
Manually annotated by BRENDA team
-
a human cutaneous T cell lymphoma cell line
Manually annotated by BRENDA team
-
ovarian cancer cell line
Manually annotated by BRENDA team
-
colon cancer cell line
Manually annotated by BRENDA team
-
melanoma cancer cell line
Manually annotated by BRENDA team
-
melanoma cancer cell line
Manually annotated by BRENDA team
-
melanoma cancer cell line
Manually annotated by BRENDA team
-
melanoma cells
Manually annotated by BRENDA team
-
leukemia cell line
Manually annotated by BRENDA team
-
nonsmall cell lung cancer cell line
Manually annotated by BRENDA team
-
nonsmall cell lung cancer cell line
Manually annotated by BRENDA team
-
nonsmall cell lung cancer cell line
Manually annotated by BRENDA team
-
nonsmall cell lung cancer cell line
Manually annotated by BRENDA team
-
breast cancer cell line
Manually annotated by BRENDA team
-
ovarian cancer cell line
Manually annotated by BRENDA team
-
ovarian cancer cell line
Manually annotated by BRENDA team
-
ovarian cancer cell line
Manually annotated by BRENDA team
-
ovarian cancer cell line
Manually annotated by BRENDA team
-
renal carcinoma cells
Manually annotated by BRENDA team
-
renal cancer cell line
Manually annotated by BRENDA team
-
CNS cancer cell line
Manually annotated by BRENDA team
-
CNS cancercell line
Manually annotated by BRENDA team
-
CNS cancer cell line
Manually annotated by BRENDA team
-
melanoma cancer cell line
Manually annotated by BRENDA team
-
melanoma cancer cell line
Manually annotated by BRENDA team
-
melanoma cancer cell line
Manually annotated by BRENDA team
-
ovarian cancer cell line
Manually annotated by BRENDA team
-
renal cancer cell line
Manually annotated by BRENDA team
-
CNS cancer cell line
Manually annotated by BRENDA team
-
CNS cancer cell line
Manually annotated by BRENDA team
-
leukemia cell line
Manually annotated by BRENDA team
-
pancreatic cancer cells
Manually annotated by BRENDA team
-
colon cancer cell line
Manually annotated by BRENDA team
-
breast cancer cell line
Manually annotated by BRENDA team
-
renal cancer cell line
Manually annotated by BRENDA team
-
CNS cancer cell line
Manually annotated by BRENDA team
-
melanoma cancer cell line
Manually annotated by BRENDA team
-
renal cancer cell line
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
TOP1_HUMAN
765
0
90726
Swiss-Prot
other Location (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
100000
-
glycerol density gradient centrifugation, monomeric form
200000
-
gel filtration, dimeric form
70000
Western blot
91000
-
-
97000
-
-
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
-
2 * 100000, SDS-PAGE. DNA topoisomerase I exists largely in a monomeric form, but also has a minor population of the dimeric form
monomer
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
-
phorsphorylation by Top1 kinase29 is required for activity, inhibition o by diospyrin induces a 10fold increase in DNA breaks in Top1-proficient cells
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
crystal structures of two camptothecin-resistant forms of human topoisomerase I F361S at 2.6 A resolution and N722S at 2.3 A resolution. Cell dimensions for N722S are: a = 57.3 A, b = 116.3 A, c = 75.2 A, beta = 94.3°, space group P2(1). Cell dimensions for F361S are: a = 57.6 A, b = 115.6 A, c = 75.0 A, beta = 96.3 A
topo70 K532R/Y723F protein in complex with a 22-mer duplex DNA oligonucleotide, vapour diffusion at room. Cell dimensions: a = 56.9 A, b = 118.6 A, c = 71.7 A, beta = 98.3°
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
F361S
camptothecin-resistant enzyme form
F617N
site-directed mutagenesis
G622A
site-directed mutagenesis
I623V
site-directed mutagenesis
K532A
K532R
cleavage and religation activity of the mutant enzyme are reduced, cleavage is reduced to a greater extent than religation
K550Q
site-directed mutagenesis
K605Q
site-directed mutagenesis
K616M
site-directed mutagenesis
K616Q
site-directed mutagenesis
K616R
site-directed mutagenesis
L603V
site-directed mutagenesis
M621I
site-directed mutagenesis
M621S
site-directed mutagenesis
N618S
site-directed mutagenesis
N722S
camptothecin-resistant enzyme form, mutation leads to elimination of a water-mediated contact between the enzyme and topotecan
Q613R
site-directed mutagenesis
T729K
is resistant even at high concentration to camptothecin anti-cancer drug
T729P
mild reduction in drug sensitivity and in DNA binding
W203A/W205A/W206A
lacking processivity, exhibits resistance to camptothecin and is inactivated by urea. Indicates that the tryptophan anchor stabilizes the N-terminus of the functional domain and revents the loss of Top1 structure and function
Y552N
site-directed mutagenesis
Y612N
site-directed mutagenesis
Y723F
Y727F
catalytically inactive
A653P
-
known to be CPT resistant
Cropo4
-
chimeric enzyme, human topo I having residues 631-717 replaced by residues 314-317 of Cre
Cropo6
-
chimeric enzyme, human topo I having residues 631-717 replaced by residues 312-317 of Cre
Cropo8
-
chimeric enzyme, human topo I having residues 631-717 replaced by residues 312-319 of Cre
DELTA1-202
-
mutant enzyme is impaired in blunt end ligation but remains sensitive towards camptothecin in relaxation
DELTA191-206
-
mutant is distinguished from wild-type enzyme by a decreased relaxation rate at distributive and an increased rate under processive conditions. Mutant is strongly impaired in blunt end ligation and insensitive towards camptothecin in relaxation
E418K
-
the active site tyrosine. The Glu418Lys mutant is active and partially resistant to CPT in yeast cells expressed in yeast cells, display a camptothecin resistance that slowly decreases as a function of time
E710G
-
site-directed mutagenesis, the mutation is not detectable in tissue samples from colorectal cancer patients
G365C
-
camptothecin-resistant Top1(G365C) mutant
G717D
-
the mutant enzyme is no more sensitive to camptothecin than the wild type enzyme
hTopoI (deltaNL)
-
hTopoI deletion mutant. Considering the domain organization, hTopoI distinguishes itself from both Vaccinia virus TopoI and the tyrosine recombinases, by having rather extensive N-terminal and linker domains. Investigation of the resolution activity of hTopoI deleted in either one or both of these domains. Two hTopoI variants, hTopoI(deltaN) lacking aa 1-202, and hTopoI(deltaNL) lacking aa 1-202 and 660-688. Deleting the N-terminal and linker domains of hTopoI in order to mimic the domain organization of Vaccinia virus TopoI and the tyrosine recombinases inhibited resolution of the Holliday junction substrate. hTopoI(deltaNL) forms dimers
hTopoI(deltaN)
-
hTopoI deletion mutant. Considering the domain organization, hTopoI distinguishes itself from both Vaccinia virus TopoI and the tyrosine recombinases, by having rather extensive N-terminal and linker domains. Investigation of the resolution activity of hTopoI deleted in either one or both of these domains. Two hTopoI variants, hTopoI(deltaN) lacking aa 1-202, and hTopoI(deltaNL) lacking aa 1-202 and 660-688. Deleting the N-terminal and linker domains of hTopoI in order to mimic the domain organization of Vaccinia virus TopoI and the tyrosine recombinases inhibited resolution of the Holliday junction substrate. hTopoI(deltaNL) forms dimers
K681A
-
site-directed mutagenesis, the mutation of Lys681, located on the tip of the linker domain, dramatically reduces the religation rate, the equilibrium of the mutant is shifted toward cleavage when compared to the wild-type enzyme. Mutation of residue 681 from lysine to alanine does not cause alterations in the linker domain secondary structure, and the main chain conformation of the mutated residue does not significantly change in relation with the neighbor residues, when compared to the wild-type protein
L617I
-
site-directed mutagenesis, the mutation is not detectable in tissue samples from colorectal cancer patients
R364K/G717R
-
the mutations lead to resistance towards inhibitors SN-38 and NSC 743400
R621H
-
site-directed mutagenesis, the mutation is not detectable in tissue samples from colorectal cancer patients
S10A/S112A/S394A
-
triple mutant 3A
S10A/S21A/S112A/S394A
-
quadruple phosphomutant 4A
S21A
-
site-directed mutagenesis
T729A
-
mutations that confer camptothecin resistance, but do not interact directly with the drug or the DNA, oligonucleotide-directed mutagenesis
T729E
-
camptothecin resistance, remarkable defect in DNA binding, oligonucleotide-directed mutagenesis
T729K
-
camptothecin resistance, oligonucleotide-directed mutagenesis
T729P
-
oligonucleotide-directed mutagenesis
W205G
-
mutant is distinguished from wild-type enzyme by a decreased relaxation rate at distributive and an increased rate under processive conditions. Mutant is strongly impaired in blunt end ligation and insensitive towards camptothecin in relaxation
Y337F
-
mutant enzyme is still able to bind single-stranded DNA but is unable to cleave the DNA substrate because of the absence of the active Tyr337
Y723F
additional information
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
anti-FLAG M2 affinity gel column chromatography
chitin affinity chromatography followed by chromatography on hydroxyapatite
HiTrap Q HP column and SDS-PAGE
mutant enzymes
enzyme overexpressed in yeast
-
Human Topo I purified from extracts of baculovirus-infected Sf9 or Hi-5 cells
-
N-terminally epitope-tagged with sequence DYKDDDY, i.e. FLAG-tag, recombinant enzyme from Saccharomyces cerevisiae strain EKY3 by immunoaffinity chromatography
-
native enzyme partially from Hut 78 cells by nuclear extract preparation
-
phosphocellulose chromatography
-
phosphocellulose column chromatography and FLAG affinity column chromatography
-
recombinant His-tagged full-length enzyme and enzyme fragments from Saccharomyces cerevisiae by nickel affinity chromatography and cation exchange chromatography
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in insect cells
expression of mutant enzymes in Saccharomyces cerevisiae
BPV1 glutathione S-transferase (GST)-E1, BPV1 GST-E1 DBD, BPV1 E2, and the human papillomavirus type 11 (HPV11) GST-E1 truncation mutant (aa 589 to 649) expressed in Escherichia coli BL21(DE3)
-
EKY3 yeast cells
-
Escherichia coli competent cells BL21(DE3)pLysS, JM109
-
expressed in Pichia pastoris strains KM71H and X33
-
expressed in Pichia pastoris strains X33, GS115, SMD1168H and KM71H
-
expressed in Saccharomyces cerevisiae
-
expressed in Saccharomyces cerevisiae strain EKY3
-
expression in Saccharaomyces cerevisiae top1 null strain RS190
-
expression in Saccharomyces cerevisiae strain RS190
-
expression mutant cells of Saccharomyces cerevisiae
-
expression of FLAG-tagged K681A mutant enzyme in Saccharomyces cerevisiae
-
gene Top1, recombinant expression in Saccharomyces cerevisiae strain EKY3 from YCpGAL1-e-Top1 single copy plasmid, N-terminally epitope-tagged with sequence DYKDDDY
-
overexpressed in yeast
-
recombinant His-tagged full-length enzyme and enzyme fragments expression in Saccharomyces cerevisiae
-
Saccharomyces cerevisiae strains EKY2 (MATa, top1D) and EKY3(MATa, top1D)
-
transformed into the yeast Saccharomyces cerevisiae top1alpha strain RS190 by the lithium acetate procedure
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
the enzyme expression is transiently induced up to 11fold by interleukin-2 at 1000 U/ml after 10 h
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
diagnostics
-
the enzyme hTopI is a biomarker for camptothecin-based therapy at direct determination of the drug response level
drug development
medicine
-
the enzyme is an anti-cancer target
pharmacology
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Liu, L.F.
HeLa topoisomerase I
Methods Enzymol.
100
133-137
1983
Homo sapiens
Manually annotated by BRENDA team
Hyder, S.M.; Baldi, A.; Crespi, M.; Wittliff, J.L.
Rapid purification of topoisomerase I from human breast cancer cells by high-performance liquid chromatography
J. Chromatogr.
359
433-447
1986
Homo sapiens
Manually annotated by BRENDA team
Gellert, M.
DNA topoisomerases
Annu. Rev. Biochem.
50
879-910
1981
Anas platyrhynchos, Priestia megaterium, Bos taurus, Gallus gallus, Drosophila sp. (in: flies), Escherichia coli, Homo sapiens, Micrococcus luteus, Platyrrhini, Mus musculus, Rattus norvegicus, salmon, Echinoidea, Vaccinia virus, Xenopus laevis
Manually annotated by BRENDA team
Vosberg, H.P.
DNA topoisomerases: enzymes that control DNA conformation
Curr. Top. Microbiol. Immunol.
114
19-102
1985
Agrobacterium tumefaciens, Priestia megaterium, Bacteria, Bos taurus, Brassica oleracea, Drosophila sp. (in: flies), Escherichia coli, eukaryota, Avibacterium paragallinarum, Homo sapiens, Micrococcus luteus, Mus musculus, Rattus norvegicus, Salmonella enterica subsp. enterica serovar Typhimurium, Triticum aestivum, Trypanosoma cruzi, Ustilago maydis, Xenopus laevis
Manually annotated by BRENDA team
Suzuki, M.; Takagi, E.; Kojima, K.; Izuta, S.; Yoshida, S.
Rapid purification and structural study of DNA topoisomerase I from human Burkitt lymphoma Raji cells
J. Biochem.
106
742-744
1989
Homo sapiens
Manually annotated by BRENDA team
Knudsen, B.R.; Straub, T.; Boege, F.
Separation and functional analysis of eukaryotic DNA topoisomerases by chromatography and electrophoresis
J. Chromatogr.
684
307-321
1996
eukaryota, Homo sapiens
Manually annotated by BRENDA team
Chino, M.; Nishikawa, K.; Yamada, A.; Ohsone, M.; Sawa, T.; Hanaoka, F.; Ishizuka, M.; Takeuchi, T.
Effect of a novel antibiotic, heliquinomycin, on DNA helicase and cell growth
J. Antibiot.
51
480-486
1998
Homo sapiens
Manually annotated by BRENDA team
Guichard, S.; Hennebelle, I.; Bugat, R.; Canal, P.
Cellular interactions of 5-fluorouracil and the camptothecin analogue CPT-11 (irinotecan) in human colorectal carcinoma cell line
Biochem. Pharmacol.
55
667-676
1998
Homo sapiens
Manually annotated by BRENDA team
Deady, L.W.; Kaye, A.J.; Finlay, G.J.; Baguley, B.C.; Denny, W.A.
Synthesis and antitumor properties of N-[2-(dimethylamino)ethyl]carboxamide derivatives of fused tetracyclic quinolines and quinoxalines: a new class of putative topoisomerase inhibitors
J. Med. Chem.
40
2040-2046
1997
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Spicer, J.A.; Gamage, S.A.; Atwell, G.J.; Finlay, G.J.; Baguley, B.C.; Denny, W.A.
Structure-activity relationships for acridine-substituted analogues of the mixed topoisomerase I/II inhibitor N-[2-dimethylamino)ethyl]acridine-4-carboxamide
J. Med. Chem.
40
1919-1929
1997
Homo sapiens
Manually annotated by BRENDA team
Lanza, A.; Tornaletti, S.; Rodolfo, C.; Scanavini, M.C.; Pedrini, A.M.
Human DNA topoisomerase I-mediated cleavages stimulated by ultraviolet light-induced DNA damage
J. Biol. Chem.
271
6978-6986
1996
Homo sapiens
Manually annotated by BRENDA team
Fostel, J.; Montgomery, D.
Identification of the aminocatechol A-3253 as an in vitro poison of DNA topoisomerase I from Candida albicans
Antimicrob. Agents Chemother.
39
586-592
1995
Candida albicans, Homo sapiens
Manually annotated by BRENDA team
Bugreev, D.V.; Vasyutina, E.L.; Ryabinin, V.A.; Sinyakov, A.N.; Buneva, V.N.; Nevinsky, G.A.
Inhibition of human DNA topoisomerase I by new DNA minor groove ligands: derivatives of oligo-1,3-thiazolecarboxamides
Antisense Nucleic Acid Drug Dev.
11
137-147
2001
Homo sapiens
Manually annotated by BRENDA team
Michishita, E.; Nakabayashi, K.; Ogino, H.; Suzuki, T.; Fujii, M.; Ayusawa, D.
DNA topoisomerase inhibitors induce reversible senescence in normal human fibroblasts
Biochem. Biophys. Res. Commun.
253
667-671
1998
Homo sapiens
Manually annotated by BRENDA team
Mizushina, Y.; Iida, A.; Ohta, K.; Sugawara, F.; Sakaguchi, K.
Novel triterpenoids inhibit both DNA polymerase and DNA topoisomerase
Biochem. J.
350
757-763
2000
Homo sapiens
-
Manually annotated by BRENDA team
Ting, C.Y.; Hsu, C.T.; Hsu, H.T.; Su, J.S.; Chen, T.Y.; Tarn, W.Y.; Kuo, Y.H.; Whang-Peng, J.; Liu, L.F.; Hwang, J.
Isodiospyrin as a novel human DNA topoisomerase I inhibitor
Biochem. Pharmacol.
66
1981-1991
2003
Homo sapiens
Manually annotated by BRENDA team
Park, H.J.; Lee, H.J.; Lee, E.J.; Hwang, H.J.; Shin, S.H.; Suh, M.E.; Kim, C.; Kim, H.J.; Seo, E.K.; Lee, S.K.
Cytotoxicity and DNA topoisomerase inhibitory activity of benz[f]indole-4,9-dione analogs
Biosci. Biotechnol. Biochem.
67
1944-1949
2003
Homo sapiens
Manually annotated by BRENDA team
Meng, L.H.; Liao, Z.Y.; Pommier, Y.
Non-camptothecin DNA topoisomerase I inhibitors in cancer therapy
Curr. Top. Med. Chem.
3
305-320
2003
Homo sapiens
Manually annotated by BRENDA team
Hotoda, N.; Hanai, R.
Characterization of recombinant human DNA topoisomerase IIIalpha activity expressed in yeast
J. Biochem.
127
1109-1113
2000
Homo sapiens
Manually annotated by BRENDA team
Fleury, F.; Sukhanova, A.; Ianoul, A.; Devy, J.; Kudelina, I.; Duval, O.; Alix, A.J.; Jardillier, J.C.; Nabiev, I.
Molecular determinants of site-specific inhibition of human DNA topoisomerase I by fagaronine and ethoxidine. Relation to DNA binding
J. Biol. Chem.
275
3501-3509
2000
Homo sapiens
Manually annotated by BRENDA team
Rudolph, J.; Theis, H.; Hanke, R.; Endermann, R.; Johannsen, L.; Geschke, F.U.
seco-Cyclothialidines: new concise synthesis, inhibitory activity toward bacterial and human DNA topoisomerases, and antibacterial properties
J. Med. Chem.
44
619-626
2001
Bos taurus, Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
Holden, J.A.
Purification of DNA topoisomerase I from human placenta
Methods Mol. Biol.
94
213-222
1999
Homo sapiens
Manually annotated by BRENDA team
Goulaouic, H.; Roulon, T.; Flamand, O.; Grondard, L.; Lavelle, F.; Riou, J.F.
Purification and characterization of human DNA topoisomerase IIIalpha
Nucleic Acids Res.
27
2443-2450
1999
Homo sapiens
Manually annotated by BRENDA team
Suzuki, T.; Uchida-Toita, M.; Andoh, T.; Yoshida, M.
HTLV-1 tax oncoprotein binds to DNA topoisomerase I and inhibits its catalytic activity
Virology
270
291-298
2000
Homo sapiens
Manually annotated by BRENDA team
Rahier, N.J.; Eisenhauer, B.M.; Gao, R.; Thomas, S.J.; Hecht, S.M.
On the role of E-ring oxygen atoms in the binding of camptothecin to the topoisomerase I-DNA covalent binary complex
Bioorg. Med. Chem.
13
1381-1386
2005
Homo sapiens
Manually annotated by BRENDA team
Chillemi, G.; Redinbo, M.; Bruselles, A.; Desideri, A.
Role of the linker domain and the 203-214 N-terminal residues in the human topoisomerase I DNA complex dynamics
Biophys. J.
87
4087-4097
2004
Homo sapiens
Manually annotated by BRENDA team
Interthal, H.; Quigley, P.M.; Hol, W.G.; Champoux, J.J.
The role of lysine 532 in the catalytic mechanism of human topoisomerase I
J. Biol. Chem.
279
2984-2992
2004
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Frohlich, R.F.; Andersen, F.F.; Westergaard, O.; Andersen, A.H.; Knudsen, B.R.
Regions within the N-terminal domain of human topoisomerase I exert important functions during strand rotation and DNA binding
J. Mol. Biol.
336
93-103
2004
Homo sapiens
Manually annotated by BRENDA team
Chrencik, J.E.; Staker, B.L.; Burgin, A.B.; Pourquier, P.; Pommier, Y.; Stewart, L.; Redinbo, M.R.
Mechanisms of camptothecin resistance by human topoisomerase I mutations
J. Mol. Biol.
339
773-784
2004
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Mialon, A.; Sankinen, M.; Soderstrom, H.; Junttila, T.T.; Holmstrom, T.; Koivusalo, R.; Papageorgiou, A.C.; Johnson, R.S.; Hietanen, S.; Elenius, K.; Westermarck, J.
DNA topoisomerase I is a cofactor for c-Jun in the regulation of epidermal growth factor receptor expression and cancer cell proliferation
Mol. Cell. Biol.
25
5040-5051
2005
Homo sapiens
Manually annotated by BRENDA team
Chen, A.Y.; Shih, S.J.; Hsiao, M.; Rothenberg, M.L.; Prudhomme, M.
Induction of radiosensitization by indolocarbazole derivatives: the role of DNA topoisomerase I
Mol. Pharmacol.
66
553-560
2004
Homo sapiens
Manually annotated by BRENDA team
Soe, K.; Hartung, S.; Grosse, F.
Human topoisomerase I forms double cleavage complexes on natural DNA
Biochem. Biophys. Res. Commun.
349
178-185
2006
Homo sapiens
Manually annotated by BRENDA team
Gao, R.; Zhang, Y.; Dedkova, L.; Choudhury, A.K.; Rahier, N.J.; Hecht, S.M.
Effects of modification of the active site tyrosine of human DNA topoisomerase I
Biochemistry
45
8402-8410
2006
Homo sapiens
Manually annotated by BRENDA team
Reguera, R.M.; Redondo, C.M.; Gutierrez de Prado, R.; Perez-Pertejo, Y.; Balana-Fouce, R.
DNA topoisomerase I from parasitic protozoa: a potential target for chemotherapy
Biochim. Biophys. Acta
1759
117-131
2006
Homo sapiens, Leishmania donovani, Leishmania major, Mammalia, Plasmodium falciparum, Trypanosoma congolense, Trypanosoma cruzi, Trypanosoma brucei (Q581U8)
Manually annotated by BRENDA team
Christmann-Franck, S.; Fermandjian, S.; Mirambeau, G.; Der Garabedian, P.A.
Molecular modelling studies on the interactions of human DNA topoisomerase IB with pyridoxal-compounds
Biochimie
89
468-473
2007
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Basnet, A.; Thapa, P.; Karki, R.; Na, Y.; Jahng, Y.; Jeong, B.S.; Jeong, T.C.; Lee, C.S.; Lee, E.S.
2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship
Bioorg. Med. Chem.
15
4351-4359
2007
Homo sapiens
Manually annotated by BRENDA team
Qin, Y.; Pang, J.Y.; Chen, W.H.; Zhao, Z.Z.; Liu, L.; Jiang, Z.H.
Inhibition of DNA topoisomerase I by natural and synthetic mono- and dimeric protoberberine alkaloids
Chem. Biodivers.
4
481-487
2007
Homo sapiens
Manually annotated by BRENDA team
Nagarajan, M.; Morrell, A.; Antony, S.; Kohlhagen, G.; Agama, K.; Pommier, Y.; Ragazzon, P.A.; Garbett, N.C.; Chaires, J.B.; Hollingshead, M.; Cushman, M.
Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors
J. Med. Chem.
49
5129-5140
2006
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Nagarajan, M.; Morrell, A.; Ioanoviciu, A.; Antony, S.; Kohlhagen, G.; Agama, K.; Hollingshead, M.; Pommier, Y.; Cushman, M.
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles
J. Med. Chem.
49
6283-6289
2006
Homo sapiens
Manually annotated by BRENDA team
Hede, M.S.; Petersen, R.L.; Froehlich, R.F.; Krueger, D.; Andersen, F.F.; Andersen, A.H.; Knudsen, B.R.
Resolution of Holliday junction substrates by human topoisomerase I
J. Mol. Biol.
365
1076-1092
2007
Homo sapiens
Manually annotated by BRENDA team
Khan, Q.A.; Pilch, D.S.
Topoisomerase I-mediated DNA cleavage induced by the minor groove-directed binding of bibenzimidazoles to a distal site
J. Mol. Biol.
365
561-569
2007
Homo sapiens
Manually annotated by BRENDA team
Hu, Y.; Clower, R.V.; Melendy, T.
Cellular topoisomerase I modulates origin binding by bovine papillomavirus type 1 E1
J. Virol.
80
4363-4371
2006
Homo sapiens
Manually annotated by BRENDA team
Bond, A.; Reichert, Z.; Stivers, J.T.
Novel and specific inhibitors of a poxvirus type I topoisomerase
Mol. Pharmacol.
69
547-557
2006
Homo sapiens, Vaccinia virus
Manually annotated by BRENDA team
Koster, D.A.; Palle, K.; Bot, E.S.; Bjornsti, M.A.; Dekker, N.H.
Antitumour drugs impede DNA uncoiling by topoisomerase I
Nature
448
213-217
2007
Homo sapiens
Manually annotated by BRENDA team
Fiorani, P.; Chillemi, G.; Losasso, C.; Castelli, S.; Desideri, A.
The different cleavage DNA sequence specificity explains the camptothecin resistance of the human topoisomerase I Glu418Lys mutant
Nucleic Acids Res.
34
5093-5100
2006
Homo sapiens
Manually annotated by BRENDA team
Rockstroh, A.; Kleinert, A.; Kramer, M.; Grosse, F.; Soe, K.
Cellular stress triggers the human topoisomerase I damage response independently of DNA damage in a p53 controlled manner
Oncogene
26
123-131
2007
Homo sapiens
Manually annotated by BRENDA team
Laco, G.S.; Pommier, Y.
Role of a tryptophan anchor in human topoisomerase I structure, function and inhibition
Biochem. J.
411
523-530
2008
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Zhang, H.; Pommier, Y.
Mitochondrial topoisomerase I sites in the regulatory D-loop region of mitochondrial DNA
Biochemistry
47
11196-11203
2008
Homo sapiens (Q969P6), Homo sapiens
Manually annotated by BRENDA team
Froehlich, R.F.; Juul, S.; Nielsen, M.B.; Vinther, M.; Veigaard, C.; Hede, M.S.; Andersen, F.F.
Identification of a minimal functional linker in human topoisomerase I by domain swapping with Cre recombinase
Biochemistry
47
7127-7136
2008
Homo sapiens
Manually annotated by BRENDA team
Khopde, S.; Roy, R.; Simmons, D.T.
The binding of topoisomerase I to T antigen enhances the synthesis of RNA-DNA primers during simian virus 40 DNA replication
Biochemistry
47
9653-9660
2008
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Zhai, B.; Shuai, L.; Yang, L.; Weng, X.; Wu, L.; Wang, S.; Tian, T.; Wu, X.; Zhou, X.; Zheng, C.
Octa-substituted anionic porphyrins: topoisomerase I inhibition and tumor cell apoptosis induction
Bioconjug. Chem.
19
1535-1542
2008
Homo sapiens
Manually annotated by BRENDA team
Cheng, Y.; An, L.K.; Wu, N.; Wang, X.D.; Bu, X.Z.; Huang, Z.S.; Gu, L.Q.
Synthesis, cytotoxic activities and structure-activity relationships of topoisomerase I inhibitors: indolizinoquinoline-5,12-dione derivatives
Bioorg. Med. Chem.
16
4617-4625
2008
Homo sapiens
Manually annotated by BRENDA team
Dallavalle, S.; Gattinoni, S.; Mazzini, S.; Scaglioni, L.; Merlini, L.; Tinelli, S.; Beretta, G.L.; Zunino, F.
Synthesis and cytotoxic activity of a new series of topoisomerase I inhibitors
Bioorg. Med. Chem. Lett.
18
1484-1489
2008
Homo sapiens
Manually annotated by BRENDA team
Li, Z.; Zhai, F.; Zhao, L.; Guo, Q.; You, Q.
Design and synthesis of N-methylmaleimide indolocarbazole bearing modified 2-acetamino acid moieties as Topoisomerase I inhibitors
Bioorg. Med. Chem. Lett.
19
406-409
2009
Homo sapiens
Manually annotated by BRENDA team
Dezhenkova, L.G.; Susova, O.Y.; Shchekotikhin, A.E.; Preobrazhenskaya, M.N.; Shtil, A.A.
Naphtho[2,3-f]indole-5,10-dione aminoalkyl derivatives: a new class of topoisomerase I inhibitors
Bull. Exp. Biol. Med.
145
334-337
2008
Homo sapiens
Manually annotated by BRENDA team
Moulder, S.; Valkov, N.; Neuger, A.; Choi, J.; Lee, J.H.; Minton, S.; Munster, P.; Gump, J.; Lacevic, M.; Lush, R.; Sullivan, D.
Phase 2 study of gemcitabine and irinotecan in metastatic breast cancer with correlatives to determine topoisomerase I localization as a predictor of response
Cancer
113
2646-2654
2008
Homo sapiens
Manually annotated by BRENDA team
Ambrosini, G.; Seelman, S.L.; Qin, L.X.; Schwartz, G.K.
The cyclin-dependent kinase inhibitor flavopiridol potentiates the effects of topoisomerase I poisons by suppressing Rad51 expression in a p53-dependent manner
Cancer Res.
68
2312-2320
2008
Homo sapiens
Manually annotated by BRENDA team
Goswami, A.; Qiu, S.; Dexheimer, T.S.; Ranganathan, P.; Burikhanov, R.; Pommier, Y.; Rangnekar, V.M.
Par-4 binds to topoisomerase 1 and attenuates its DNA relaxation activity
Cancer Res.
68
6190-6198
2008
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Cheng, X.; Wang, D.; Jiang, L.; Yang, D.
DNA topoisomerase I inhibitory alkaloids from Corydalis saxicola
Chem. Biodivers.
5
1335-1344
2008
Homo sapiens
Manually annotated by BRENDA team
Han, H.J.; Tan, N.H.; Zeng, G.Z.; Fan, J.T.; Huang, H.Q.; Ji, C.J.; Jia, R.R.; Zhao, Q.S.; Zhang, Y.J.; Hao, X.J.; Wang, L.Q.
Natural inhibitors of DNA topoisomerase I with cytotoxicities
Chem. Biodivers.
5
1364-1368
2008
Homo sapiens
Manually annotated by BRENDA team
Beretta, G.L.; Perego, P.; Zunino, F.
Targeting topoisomerase I: molecular mechanisms and cellular determinants of response to topoisomerase I inhibitors
Expert Opin. Ther. Targets
12
1243-1256
2008
Homo sapiens
Manually annotated by BRENDA team
Lopez-Lazaro, M.; Willmore, E.; Elliott, S.L.; Austin, C.A.
Selenite induces topoisomerase I and II-DNA complexes in K562 leukemia cells
Int. J. Cancer
123
2217-2221
2008
Homo sapiens
Manually annotated by BRENDA team
Lebedeva, N.; Rechkunova, N.; Boiteux, S.; Lavrik, O.
Trapping of human DNA topoisomerase I by DNA structures mimicking intermediates of DNA repair
IUBMB Life
60
130-134
2008
Homo sapiens
Manually annotated by BRENDA team
Hackbarth, J.S.; Galvez-Peralta, M.; Dai, N.T.; Loegering, D.A.; Peterson, K.L.; Meng, X.W.; Karnitz, L.M.; Kaufmann, S.H.
Mitotic phosphorylation stimulates DNA relaxation activity of human topoisomerase I
J. Biol. Chem.
283
16711-16722
2008
Homo sapiens
Manually annotated by BRENDA team
Sordet, O.; Goldman, A.; Redon, C.; Solier, S.; Rao, V.A.; Pommier, Y.
Topoisomerase I requirement for death receptor-induced apoptotic nuclear fission
J. Biol. Chem.
283
23200-23208
2008
Homo sapiens
Manually annotated by BRENDA team
Gul, H.I.; Cizmecioglu, M.; Zencir, S.; Gul, M.; Canturk, P.; Atalay, M.; Topcu, Z.
Cytotoxic activity of 4-hydroxychalcone derivatives against Jurkat cells and their effects on mammalian DNA topoisomerase I
J. Enzyme Inhib. Med. Chem.
24
804-807
2009
Homo sapiens
Manually annotated by BRENDA team
Alpan, A.S.; Zencir, S.; Zupko, I.; Coban, G.; Rethy, B.; Gunes, H.S.; Topcu, Z.
Biological activity of bis-benzimidazole derivatives on DNA topoisomerase I and HeLa, MCF7 and A431 cells
J. Enzyme Inhib. Med. Chem.
24
844-849
2009
Homo sapiens
Manually annotated by BRENDA team
Diana, P.; Martorana, A.; Barraja, P.; Montalbano, A.; Dattolo, G.; Cirrincione, G.; Dallacqua, F.; Salvador, A.; Vedaldi, D.; Basso, G.; Viola, G.
Isoindolo[2,1-a]quinoxaline derivatives, novel potent antitumor agents with dual inhibition of tubulin polymerization and topoisomerase I
J. Med. Chem.
51
2387-2399
2008
Homo sapiens
Manually annotated by BRENDA team
Cinelli, M.A.; Morrell, A.; Dexheimer, T.S.; Scher, E.S.; Pommier, Y.; Cushman, M.
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors
J. Med. Chem.
51
4609-4619
2008
Homo sapiens (P11387)
Manually annotated by BRENDA team
Losasso, C.; Cretaio, E.; Fiorani, P.; DAnnessa, I.; Chillemi, G.; Benedetti, P.
A single mutation in the 729 residue modulates human DNA topoisomerase IB DNA binding and drug resistance
Nucleic Acids Res.
36
5635-5644
2008
Homo sapiens
Manually annotated by BRENDA team
Chillemi, G.; DAnnessa, I.; Fiorani, P.; Losasso, C.; Benedetti, P.; Desideri, A.
Thr729 in human topoisomerase I modulates anti-cancer drug resistance by altering protein domain communications as suggested by molecular dynamics simulations
Nucleic Acids Res.
36
5645-5651
2008
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Sirikantaramas, S.; Yamazaki, M.; Saito, K.
Mutations in topoisomerase I as a self-resistance mechanism coevolved with the production of the anticancer alkaloid camptothecin in plants
Proc. Natl. Acad. Sci. USA
105
6782-6786
2008
Catharanthus roseus, Ophiorrhiza pumila, Camptotheca acuminata, Ophiorrhiza liukiuensis, Ophiorrhiza japonica, Homo sapiens (P11387), Homo sapiens, Arabidopsis thaliana (P30181)
Manually annotated by BRENDA team
Pham, M.H.; Kondapalli, N.; Reckord, C.L.; Foglesong, P.D.
Interleukin-2 induces the activities of DNA topoisomerase I and DNA topoisomerase II in HuT 78 cells
Biochem. Biophys. Res. Commun.
390
577-580
2009
Homo sapiens
Manually annotated by BRENDA team
Lebedeva, N.A.; Rechkunova, N.I.; Agama, K.; Pommier, Y.; Lavrik, O.I.
Interaction of DNA topoisomerase 1 with DNA intermediates and proteins of base excision repair
Biochemistry (Moscow)
74
1278-1284
2009
Homo sapiens
Manually annotated by BRENDA team
Lee, S.H.; Van, H.T.; Yang, S.H.; Lee, K.T.; Kwon, Y.; Cho, W.J.
Molecular design, synthesis and docking study of benz[b]oxepines and 12-oxobenzo[c]phenanthridinones as topoisomerase 1 inhibitors
Bioorg. Med. Chem. Lett.
19
2444-2447
2009
Homo sapiens (P11387)
Manually annotated by BRENDA team
Galvez-Peralta, M.; Hackbarth, J.S.; Flatten, K.S.; Kaufmann, S.H.; Hiasa, H.; Xing, C.; Ferguson, D.M.
On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents
Bioorg. Med. Chem. Lett.
19
4459-4462
2009
Homo sapiens
Manually annotated by BRENDA team
Chua, S.; Quek, N.; Li, M.; Ng, M.; Yuan, W.; Chua, M.; Guo, J.; Koh, L.; Ye, R.; Li, T.
Nick-containing oligonucleotides as human topoisomerase I inhibitors
Bioorg. Med. Chem. Lett.
19
618-623
2009
Homo sapiens
Manually annotated by BRENDA team
Cho, H.J.; Jung, M.J.; Kwon, Y.; Na, Y.
Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors
Bioorg. Med. Chem. Lett.
19
6766-6769
2009
Homo sapiens
Manually annotated by BRENDA team
Wang, P.; Ownby, S.; Zhang, Z.; Yuan, W.; Li, S.
Cytotoxicity and inhibition of DNA topoisomerase I of polyhydroxylated triterpenoids and triterpenoid glycosides
Bioorg. Med. Chem. Lett.
20
2790-2796
2010
Homo sapiens
Manually annotated by BRENDA team
Cinelli, M.A.; Cordero, B.; Dexheimer, T.S.; Pommier, Y.; Cushman, M.
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships
Bioorg. Med. Chem.
17
7145-7155
2009
Homo sapiens (P11387)
Manually annotated by BRENDA team
Thapa, P.; Karki, R.; Thapa, U.; Jahng, Y.; Jung, M.J.; Nam, J.M.; Na, Y.; Kwon, Y.; Lee, E.S.
2-Thienyl-4-furyl-6-aryl pyridine derivatives: synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study
Bioorg. Med. Chem.
18
377-386
2010
Homo sapiens
Manually annotated by BRENDA team
Kostopoulos, I.; Karavasilis, V.; Karina, M.; Bobos, M.; Xiros, N.; Pentheroudakis, G.; Kafiri, G.; Papakostas, P.; Vrettou, E.; Fountzilas, G.
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
9
339-348
2009
Homo sapiens
Manually annotated by BRENDA team
Shuai, L.; Wang, S.; Zhang, L.; Fu, B.; Zhou, X.
Cationic porphyrins and analogues as new DNA topoisomerase I and II inhibitors
Chem. Biodivers.
6
827-837
2009
Homo sapiens
Manually annotated by BRENDA team
Eisenreich, A.; Bogdanov, V.Y.; Zakrzewicz, A.; Pries, A.; Antoniak, S.; Poller, W.; Schultheiss, H.P.; Rauch, U.
Cdc2-like kinases and DNA topoisomerase I regulate alternative splicing of tissue factor in human endothelial cells
Circ. Res.
104
589-599
2009
Homo sapiens
Manually annotated by BRENDA team
You, Q.D.; Li, Z.Y.; Huang, C.H.; Yang, Q.; Wang, X.J.; Guo, Q.L.; Chen, X.G.; He, X.G.; Li, T.K.; Chern, J.W.
Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification
J. Med. Chem.
52
5649-5661
2009
Homo sapiens
Manually annotated by BRENDA team
Song, Y.; Shao, Z.; Dexheimer, T.S.; Scher, E.S.; Pommier, Y.; Cushman, M.
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors
J. Med. Chem.
53
1979-1989
2010
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Chan, A.; Chang, W.; Chen, L.; Lee, C.; Chen, C.; Lin, C.; Hwang, J.
Evodiamine stabilizes topoisomerase I-DNA cleavable complex to inhibit topoisomerase I activity
Molecules
14
1342-1352
2009
Homo sapiens
Manually annotated by BRENDA team
Tuduri, S.; Crabbe, L.; Conti, C.; Tourriere, H.; Holtgreve-Grez, H.; Jauch, A.; Pantesco, V.; De Vos, J.; Thomas, A.; Theillet, C.; Pommier, Y.; Tazi, J.; Coquelle, A.; Pasero, P.
Topoisomerase I suppresses genomic instability by preventing interference between replication and transcription
Nat. Cell Biol.
11
1315-1324
2009
Homo sapiens
Manually annotated by BRENDA team
Malina, J.; Vrana, O.; Brabec, V.
Mechanistic studies of the modulation of cleavage activity of topoisomerase I by DNA adducts of mono- and bi-functional PtII complexes
Nucleic Acids Res.
37
5432-5442
2009
Homo sapiens
Manually annotated by BRENDA team
Fiorani, P.; Tesauro, C.; Mancini, G.; Chillemi, G.; D'Annessa, I.; Graziani, G.; Tentori, L.; Muzi, A.; Desideri, A.
Evidence of the crucial role of the linker domain on the catalytic activity of human topoisomerase I by experimental and simulative characterization of the Lys681Ala mutant
Nucleic Acids Res.
37
6849-6858
2009
Homo sapiens
Manually annotated by BRENDA team
Szklarczyk, O.; Staron, K.; Cieplak, M.
Native state dynamics and mechanical properties of human topoisomerase I within a structure-based coarse-grained model
Proteins
77
420-431
2009
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Capranico, G.; Marinello, J.; Baranello, L.
Dissecting the transcriptional functions of human DNA topoisomerase I by selective inhibitors: implications for physiological and therapeutic modulation of enzyme activity
Biochim. Biophys. Acta
1806
240-250
2010
Homo sapiens
Manually annotated by BRENDA team
Karki, R.; Thapa, P.; Kang, M.J.; Jeong, T.C.; Nam, J.M.; Kim, H.L.; Na, Y.; Cho, W.J.; Kwon, Y.; Lee, E.S.
Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines
Bioorg. Med. Chem.
18
3066-3077
2010
Homo sapiens
Manually annotated by BRENDA team
Khadka, D.B.; Le, Q.M.; Yang, S.H.; Van, H.T.; Le, T.N.; Cho, S.H.; Kwon, Y.; Lee, K.T.; Lee, E.S.; Cho, W.J.
Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase I inhibitors
Bioorg. Med. Chem.
19
1924-1929
2011
Homo sapiens
Manually annotated by BRENDA team
Shi, W.; Marcus, S.L.; Lowary, T.L.
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.
19
603-612
2011
Homo sapiens
Manually annotated by BRENDA team
Jeong, B.; Choi, H.; Thapa, P.; Karki, R.; Lee, E.; Nam, J.; Na, Y.; Ha, E.; Kwon, Y.; Lee, E.
Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of rigid analogues of 2,4,6-trisubstituted pyridine containing 5,6-dihydrobenzo[h]quinoline moiety
Bull. Korean Chem. Soc.
32
303-306
2011
Homo sapiens
-
Manually annotated by BRENDA team
Kurtzberg, L.S.; Roth, S.; Krumbholz, R.; Crawford, J.; Bormann, C.; Dunham, S.; Yao, M.; Rouleau, C.; Bagley, R.G.; Yu, X.J.; Wang, F.; Schmid, S.M.; Lavoie, E.J.; Teicher, B.A.
Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment
Clin. Cancer Res.
17
2777-2787
2011
Homo sapiens, Mus musculus, Mus musculus BALB/c
Manually annotated by BRENDA team
Arlt, M.F.; Glover, T.W.
Inhibition of topoisomerase I prevents chromosome breakage at common fragile sites
DNA Repair
9
678-689
2010
Homo sapiens
Manually annotated by BRENDA team
Jun, K.Y.; Lee, E.Y.; Jung, M.J.; Lee, O.H.; Lee, E.S.; Park Choo, H.Y.; Na, Y.; Kwon, Y.
Synthesis, biological evaluation, and molecular docking study of 3-(3-heteroatom substituted-2-hydroxy-1-propyloxy) xanthone analogues as novel topoisomerase IIalpha catalytic inhibitor
Eur. J. Med. Chem.
46
1964-1971
2011
Homo sapiens
Manually annotated by BRENDA team
Thapa, U.; Thapa, P.; Karki, R.; Yun, M.; Choi, J.H.; Jahng, Y.; Lee, E.; Jeon, K.H.; Na, Y.; Ha, E.M.; Cho, W.J.; Kwon, Y.; Lee, E.S.
Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship
Eur. J. Med. Chem.
46
3201-3209
2011
Homo sapiens
Manually annotated by BRENDA team
Peterson, K.E.; Cinelli, M.A.; Morrell, A.E.; Mehta, A.; Dexheimer, T.S.; Agama, K.; Antony, S.; Pommier, Y.; Cushman, M.
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity
J. Med. Chem.
54
4937-4953
2011
Homo sapiens
Manually annotated by BRENDA team
Arjmand, F.; Muddassir, M.
Design and synthesis of heterobimetallic topoisomerase I and II inhibitor complexes: In vitro DNA binding, interaction with 5'-GMP and 5'-TMP and cleavage studies
J. Photochem. Photobiol. B
101
37-46
2010
Homo sapiens
Manually annotated by BRENDA team
Gentry, A.C.; Juul, S.; Veigaard, C.; Knudsen, B.R.; Osheroff, N.
The geometry of DNA supercoils modulates the DNA cleavage activity of human topoisomerase I
Nucleic Acids Res.
39
1014-1022
2011
Homo sapiens
Manually annotated by BRENDA team
Ishikawa, T.; Krzysko, K.A.; Kowalska-Loth, B.; Skrajna, A.M.; Czubaty, A.; Girstun, A.; Cieplak, M.K.; Lesyng, B.; Staron, K.
Activities of topoisomerase I in its complex with SRSF1
Biochemistry
51
1803-1816
2012
Homo sapiens
Manually annotated by BRENDA team
Ashour, A.; El-Sharkawy, S.; Amer, M.; Abdel Bar, F.; Katakura, Y.; Miyamoto, T.; Toyota, N.; Bang, T.H.; Kondo, R.; Shimizu, K.
Rational design and synthesis of topoisomerase I and II inhibitors based on oleanolic acid moiety for new anti-cancer drugs
Bioorg. Med. Chem.
22
211-220
2014
Homo sapiens
Manually annotated by BRENDA team
Arno, B.; Coletta, A.; Tesauro, C.; Zuccaro, L.; Fiorani, P.; Lentini, S.; Galloni, P.; Conte, V.; Floris, B.; Desideri, A.
A small organic compound enhances the religation reaction of human topoisomerase I and identifies crucial elements for the religation mechanism
Biosci. Rep.
33
e00025
2013
Homo sapiens
Manually annotated by BRENDA team
Liu, W.; Zhu, L.; Guo, W.; Zhuang, C.; Zhang, Y.; Sheng, C.; Cheng, P.; Yao, J.; Wang, W.; Dong, G.; Wang, S.; Miao, Z.; Zhang, W.
Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors
Eur. J. Med. Chem.
46
2408-2414
2011
Homo sapiens
Manually annotated by BRENDA team
Conda-Sheridan, M.; Reddy, P.V.; Morrell, A.; Cobb, B.T.; Marchand, C.; Agama, K.; Chergui, A.; Renaud, A.; Stephen, A.G.; Bindu, L.K.; Pommier, Y.; Cushman, M.
Synthesis and biological evaluation of indenoisoquinolines that inhibit both tyrosyl-DNA phosphodiesterase I (Tdp1) and topoisomerase I (Top1)
J. Med. Chem.
56
182-200
2013
Homo sapiens
Manually annotated by BRENDA team
Gongora, C.; Vezzio-Vie, N.; Tuduri, S.; Denis, V.; Causse, A.; Auzanneau, C.; Collod-Beroud, G.; Coquelle, A.; Pasero, P.; Pourquier, P.; Martineau, P.; Del Rio, M.
New topoisomerase I mutations are associated with resistance to camptothecin
Mol. Cancer
10
64
2011
Homo sapiens
Manually annotated by BRENDA team
Laco, G.S.
Evaluation of two models for human topoisomerase I interaction with dsDNA and camptothecin derivatives
PLoS ONE
6
e24314
2011
Homo sapiens
Manually annotated by BRENDA team
Drwal, M.N.; Agama, K.; Wakelin, L.P.; Pommier, Y.; Griffith, R.
Exploring DNA topoisomerase I ligand space in search of novel anticancer agents
PLoS ONE
6
e25150
2011
Homo sapiens
Manually annotated by BRENDA team
Douarre, C.; Sourbier, C.; Dalla Rosa, I.; Brata Das, B.; Redon, C.E.; Zhang, H.; Neckers, L.; Pommier, Y.
Mitochondrial topoisomerase I is critical for mitochondrial integrity and cellular energy metabolism
PLoS ONE
7
e41094
2012
Homo sapiens
Manually annotated by BRENDA team
Cortopassi, W.A.; Penna-Coutinho, J.; Aguiar, A.C.; Pimentel, A.S.; Buarque, C.D.; Costa, P.R.; Alves, B.R.; Franca, T.C.; Krettli, A.U.
Theoretical and experimental studies of new modified isoflavonoids as potential inhibitors of topoisomerase I from Plasmodium falciparum
PLoS ONE
9
e91191
2014
Homo sapiens, Plasmodium falciparum
Manually annotated by BRENDA team
Proszek, J.; Roy, A.; Jakobsen, A.K.; Fr?hlich, R.; Knudsen, B.R.; Stougaard, M.
Topoisomerase I as a biomarker: detection of activity at the single molecule level
Sensors
14
1195-1207
2013
Homo sapiens
Manually annotated by BRENDA team
Tian, Q.T.; Ding, C.Y.; Song, S.S.; Wang, Y.Q.; Zhang, A.; Miao, Z.H.
New tanshinone I derivatives S222 and S439 similarly inhibit topoisomerase I/II but reveal different p53-dependency in inducing G2/M arrest and apoptosis
Biochem. Pharmacol.
154
255-264
2018
Homo sapiens (P11387)
Manually annotated by BRENDA team
de Oliveira Figueiredo, P.; Perdomo, R.T.; Garcez, F.R.; de Fatima Cepa Matos, M.; de Carvalho, J.E.; Garcez, W.S.
Further constituents of Galianthe thalictroides (Rubiaceae) and inhibition of DNA topoisomerases I and IIalpha by its cytotoxic beta-carboline alkaloids
Bioorg. Med. Chem. Lett.
24
1358-1361
2014
Homo sapiens
Manually annotated by BRENDA team
Puc, J.; Kozbial, P.; Li, W.; Tan, Y.; Liu, Z.; Suter, T.; Ohgi, K.A.; Zhang, J.; Aggarwal, A.K.; Rosenfeld, M.G.
Ligand-dependent enhancer activation regulated by topoisomerase-I activity
Cell
160
367-380
2015
Homo sapiens
Manually annotated by BRENDA team
Ang, R.; Teoh, L.; Chan, M.; Miswan, N.; Khoo, B.
Comparing the expression of human DNA topoisomerase I in KM71H and X33 strains of Pichia pastoris
Electron. J. Biotechnol.
21
9-17
2016
Homo sapiens
-
Manually annotated by BRENDA team
Yu, L.M.; Zhang, X.R.; Li, X.B.; Yang, Y.; Wei, H.Y.; He, X.X.; Gu, L.Q.; Huang, Z.S.; Pommier, Y.; An, L.K.
Synthesis and biological evaluation of 6-substituted indolizinoquinolinediones as catalytic DNA topoisomerase I inhibitors
Eur. J. Med. Chem.
101
525-533
2015
Homo sapiens
Manually annotated by BRENDA team
Wu, G.; Qi, X.; Mo, X.; Yu, G.; Wang, Q.; Zhu, T.; Gu, Q.; Liu, M.; Li, J.; Li, D.
Structure-based discovery of cytotoxic dimeric tetrahydroxanthones as potential topoisomerase I inhibitors from a marine-derived fungus
Eur. J. Med. Chem.
148
268-278
2018
Homo sapiens
Manually annotated by BRENDA team
Kumar, A.; Bora, U.
Molecular docking studies of curcumin natural derivatives with DNA topoisomerase I and II-DNA complexes
Interdiscip. Sci. Comput. Life Sci.
6
285-291
2014
Homo sapiens (P11387)
Manually annotated by BRENDA team
Wright, C.M.; van der Merwe, M.; DeBrot, A.H.; Bjornsti, M.A.
DNA topoisomerase I domain interactions impact enzyme activity and sensitivity to camptothecin
J. Biol. Chem.
290
12068-12078
2015
Homo sapiens
Manually annotated by BRENDA team
Jensen, N.F.; Agama, K.; Roy, A.; Smith, D.H.; Pfister, T.D.; R?mer, M.U.; Zhang, H.L.; Doroshow, J.H.; Knudsen, B.R.; Stenvang, J.; Bruenner, N.; Pommier, Y.
Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a new pair of resistance-associated mutations
J. Exp. Clin. Cancer Res.
35
56
2016
Homo sapiens
Manually annotated by BRENDA team
Castelli, S.; Gonalves, M.; Katkar, P.; Stuchi, G.; Couto, R.; Petrilli, H.; da Costa Ferreira, A.
Comparative studies of oxindolimine-metal complexes as inhibitors of human DNA topoisomerase IB
J. Inorg. Biochem.
186
85-94
2018
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Ranjan, N.; Story, S.; Fulcrand, G.; Leng, F.; Ahmad, M.; King, A.; Sur, S.; Wang, W.; Tse-Dinh, Y.C.; Arya, D.P.
Selective inhibition of Escherichia coli RNA and DNA topoisomerase I by Hoechst 33258 derived mono- and bisbenzimidazoles
J. Med. Chem.
60
4904-4922
2017
Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
D'Alfonso, A.; Di Felice, F.; Carlini, V.; Wright, C.M.; Hertz, M.I.; Bjornsti, M.A.; Camilloni, G.
Molecular mechanism of DNA topoisomerase I-dependent rDNA silencing Sir2p recruitment at ribosomal genes
J. Mol. Biol.
428
4905-4916
2016
Saccharomyces cerevisiae, Homo sapiens (P11387), Homo sapiens, Saccharomyces cerevisiae W303-1A
Manually annotated by BRENDA team
Xin, L.T.; Liu, L.; Shao, C.L.; Yu, R.L.; Chen, F.L.; Yue, S.J.; Wang, M.; Guo, Z.L.; Fan, Y.C.; Guan, H.S.; Wang, C.Y.
Discovery of DNA topoisomerase I inhibitors with low-cytotoxicity based on virtual screening from natural products
Mar. Drugs
15
pii: E217
2017
Homo sapiens (P11387), Homo sapiens
Manually annotated by BRENDA team
Chan, M.K.; Lim, S.K.; Miswan, N.; Chew, A.L.; Noordin, R.; Khoo, B.Y.
Expression of stable and active human DNA topoisomerase I in Pichia pastoris
Protein Expr. Purif.
141
52-62
2018
Homo sapiens
Manually annotated by BRENDA team
Gokduman, K.
Strategies targeting DNA topoisomerase I in cancer chemotherapy camptothecins, nanocarriers for camptothecins, organic non-camptothecin compounds and metal complexes
Curr. Drug Targets
17
1928-1939
2016
Homo sapiens
Manually annotated by BRENDA team
Manzo, S.G.; Hartono, S.R.; Sanz, L.A.; Marinello, J.; De Biasi, S.; Cossarizza, A.; Capranico, G.; Chedin, F.
DNA topoisomerase I differentially modulates R-loops across the human genome
Genome Biol.
19
100
2018
Homo sapiens
Manually annotated by BRENDA team