Information on EC 5.99.1.2 - DNA topoisomerase

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
5.99.1.2
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RECOMMENDED NAME
GeneOntology No.
DNA topoisomerase
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
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transesterification
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typ IB topoisomerases generate a tyrosyl-3'-phosphodiester. Recombinant MimiTopIB relaxes supercoiled DNA
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 5.99.1.3 DNA topoisomerase (ATP-hydrolysing).
CAS REGISTRY NUMBER
COMMENTARY hide
80449-01-0
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
a parasite of Acanthamoeba polyphaga
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
Bacillus cereus ATCC14579
ATCC14579
UniProt
Manually annotated by BRENDA team
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-
-
Manually annotated by BRENDA team
strain YIT4006
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Manually annotated by BRENDA team
strain YIT4006
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Manually annotated by BRENDA team
camptothecin producing plant
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
camptothecin non producing plant
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
gene topA
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Manually annotated by BRENDA team
contains two topoisomerase III genes
UniProt
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
strain FMC2
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Manually annotated by BRENDA team
strain FMC2
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Manually annotated by BRENDA team
strain NRRL B-11,022
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Manually annotated by BRENDA team
strain NRRL B-11,022
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Manually annotated by BRENDA team
Mus musculus BALB/c
male mice
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Manually annotated by BRENDA team
Erdman strain
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Manually annotated by BRENDA team
gene MtbTopA or Rv3646
UniProt
Manually annotated by BRENDA team
var. xanthi
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Manually annotated by BRENDA team
camptothecin non producing plant
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Manually annotated by BRENDA team
camptothecin producing plant has Top1s with point mutations that confer resistance to camptothecin, suggesting the effect of an endogenous toxic metabolite on the evolution of the target cellular component
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Manually annotated by BRENDA team
camptothecin producing plant
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
salmon
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Manually annotated by BRENDA team
Sea urchin
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Manually annotated by BRENDA team
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UniProt
Manually annotated by BRENDA team
strain M145
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Manually annotated by BRENDA team
E233, spontaneous uracil-auxotrophic mutant derived from Sulfolobus islandicus Rey15A
SwissProt
Manually annotated by BRENDA team
E233, spontaneous uracil-auxotrophic mutant derived from Sulfolobus islandicus Rey15A
SwissProt
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
in Ref. 21 steht nur Xenopus sp.
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Manually annotated by BRENDA team
inbred line Mo17, gene Top1
UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(TTA)35
?
show the reaction diagram
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trinucleotide repeat (TTA)35 lying in the intergenic region of chromosome XIII of Saccharomyces cerevisiae, between the RPM2 (RNase P mitochondrial 2) and PRE8 genes. This sequence contains the structural elements suitable to be susceptible to DNA topoisomerase I site-specific activity and to assemble nucleosomes. DNA topoisomerase I strongly recognizes the TTA repeats. The (TTA)35 repeat is engaged in a positioned nucleosome in vivo. DNA topoisomerase I efficiently reacts with the TTA repeat, the (TTA)35 sequence, the longest and most stable among the simple repeated sequences in Saccharomyces cerevisiae, is organized in a positioned nucleosome and this can possibly account for its high stability, in fact each nucleosome stores one negative supercoil, thus preventing DNA denaturation and induction of conformational alterations responsible for genetic instability. DNA topoisomerase I in vivo cleaves the (TTA)35 sequence after nucleosome removal, the positioned nucleosome on the (TTA)35 sequence represents a hindrance to the DNA topoisomerase I activity. This last conclusion, based on the glucose/galactose experiments, represents the first formal evidence that DNA topoisomerase I cannot react with nucleosomal DNA
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?
DNA
DNA
show the reaction diagram
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so-called suicide substrate, contains a htopoI preferential binding sequence and is designed to trap the liberated 5'-OH end
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?
Holliday Junction Substrate H1-4
?
show the reaction diagram
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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
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?
negatively supercoiled DNA
?
show the reaction diagram
negatively supercoiled DNA
relaxed DNA
show the reaction diagram
negatively supercoiled pHOTI plasmid DNA
?
show the reaction diagram
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?
negatively supercoiled plasmid pXXZ06 DNA
?
show the reaction diagram
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negatively supercoiled PUC18 DNA
?
show the reaction diagram
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unable to relax positively supercoiled DNA
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?
Nicked circular DNA
Large catenated DNA networks
show the reaction diagram
SF2/ASF protein + ATP
?
show the reaction diagram
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kinase activity
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?
supercoiled DNA
?
show the reaction diagram
supercoiled DNA
relaxed closed circular DNA
show the reaction diagram
supercoiled plasmid DNA pGEM-5T
?
show the reaction diagram
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relaxation
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?
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
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
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TopR1 can relax negative supercoils without ATP, while the extent of positive supercoiling catalyzed by TopR1 is dependent on the stoichiometry, the ATP concentration, the NaCl concentration and the assay temperature
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?
supercoiled DNA
?
show the reaction diagram
additional information
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
cyclin
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additional information
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cu2+
can partially substitute for Mg2+
KCl
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maximal activity of wild-type enzyme at 150 mM, maximal activity of mutant enzyme N726D at 75-100 mM
NH4+
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stimulates
additional information
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(+)-cheilanthifoline
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very weak inhibition
(+)-isocorydine
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(-)-cavidine
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very weak inhibition
(-)-cryptotanshinone
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diterpenoid from Salvia castanea f. tomentos
(-)-pallidine
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comparable to camptothecin
(-)-scoulerine
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inhibition comparable to camptothecin
(-)-tetrahydropalmatine
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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
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-
(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
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(1-phenyl-ethylideneamino)-acetic acid
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0.05 mM, 53% vTopo RNase activity remaining, 10% cTopo relaxation activity remaining
(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
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(2-hydroxy-naphthalen-1-yl)-acetic acid
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0.05 mM, 48% vTopo RNase activity remaining
(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
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(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
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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
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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
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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
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20.2% inhibition at 0.1 mM; 8.2% inhibition at 0.1 mM
(2S,3S,6R)-2-methyl-6-(3-(2-phenyl-1-tosyl-1H-indol-3-yl)prop-2-ynyloxy)tetrahydro-2H-pyran-3-amine
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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
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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
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7.9% inhibition at 0.1 mM
(3-hydroxy-4-thiocyanato-benzylsulfanyl)-acetic acid
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0.05 mM, 45% vTopo RNase activity remaining
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(5Z,7E,9E,14Z,17Z)-icosa-5,7,9,14,17-pentaenoic acid
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(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)carbamic acid
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(6aR,11aS)-11-[(4-methylphenyl)sulfonyl]-6,6a,11,11a-tetrahydro-5H-benzo[a]carbazole
(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)acridin-3-yl)(4-methylpiperazin-1-yl)methanone
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(9-([2-(1H-indol-3-yl)ethyl]amino)acridin-4-yl)(4-methylpiperazin-1-yl)methanone
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(9-[(1-benzylpiperidin-4-yl)amino]acridin-3-yl)(4-methylpiperazin-1-yl)methanone
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(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
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(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
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(S)-camptothecin
1,1',1'',1'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis(1-methylpiperidinium) tetraiodide
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-
1,1',1'',1'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis[3-(ethoxycarbonyl)-1-methylpiperidinium] tetraiodide
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1,1',1'',1'''-[1,4-dihydroporphyrin-5,10,15,20-tetrayltetrakis(benzene-4,1-diylmethanediyl)]tetrakis[3-(hydroxymethyl)-1-methylpiperidinium] tetraiodide
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1,2'-binaphthalene-7',8-dicarboxylic acid
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does not inhibit supercoil relaxation at 10 microM concentration. IC90 (compound concentration at which 90% or higher inhibition is observed) 2 microM, using high-throughput screen, relaxation inhibition 0%
1,3-bis(4-amino-2-methylquinolin-6-yl)urea
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IC90 (compound concentration at which 90% or higher inhibition is observed) 2 microM, using high-throughput screen, relaxation inhibition 40%
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)
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1,5-dideoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-xylo-hexitol
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1-(3,4-dihydroxybenzyl)isoquinoline-6,7-diol
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IC90 (compound concentration at which 90% or higher inhibition is observed) 10 microM, using high-throughput screen, relaxation inhibition 80%
1-(alpha-L-idopyranosyl)-N-(2-methylbenzoyl)-5-(methylsulfanyl)-1H-1,2,4-triazol-3-amine
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1-deoxy-1-(3-nitro-5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-glucitol
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1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-allitol
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1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-arabinitol
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1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-galactitol
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1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-glucitol
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1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-mannitol
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1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-ribitol
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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
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1-ethyl-3-(6-aminobenzoimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naph- thyridin-4(1H)-one
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1-ethyl-3-(6-aminobenzoimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridin-4(1H)-one
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1-ethyl-3-(6-aminobenzoimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
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1-ethyl-3-(6-chlorobenzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
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1-ethyl-3-(6-chlorobenzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
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1-ethyl-3-(6-nitrobenzimidazol-2-yl)-6-fluoro-7-(4-methyl-1-piperazinyl)-4(1H)-quinolone
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1-ethyl-3-(6-nitrobenzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
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1-ethyl-3-(6-nitrobenzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
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1-ethyl-3-(6-nitrobenzothiazol-2-yl)-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4(1H)-quinolone
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1-ethyl-3-(6-nitrobenzothiazol-2-yl)-6-fluoro-7-(4-methylpiperazin-1-yl)-4(1H)-quinolone
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1-ethyl-3-(6-nitrobenzothiazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
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1-ethyl-3-(6-nitrobenzothiazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone
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1-ethyl-3-(6-nitrobenzoxazol-2-yl)-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4(1H)-quinolone
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; interacts with DNA-Top I complex and induces cancer cell apoptosis to produce antitumor effects, in vivo inhibition of anchorage-dependent colony formation
1-ethyl-3-(6-nitrobenzoxazol-2-yl)-6-fluoro-7-(4-methylpiperazin-1-yl)-4(1H)-quinolone
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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
-
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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
-
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1-ethyl-3-(benzothiazol-2-yl)-6-fluoro-7-(4-methylpiperazin-1-yl)-4(1H)-quinolone
-
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1-ethyl-3-(benzothiazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-1,8-naphthyridine-4(1H)-one
-
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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
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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
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1-hydroxy-3-(oxiran-2-ylmethoxy)-9H-xanthen-9-one
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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-4-(5-phenyl-1H-pyrrol-2-yl)-butan-2-one
-
0.05 mM, 35% vTopo RNase activity remaining
-
1-hydroxy-8-methoxyanthracene-9,10-dione
-
-
1-[2-(dimethylamino)ethoxy]-8-methoxyanthracene-9,10-dione
-
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1-[2-(dimethylamino)ethyl]-3-[(4-methylphenyl)sulfonyl]-1H-pyrrolo[2,3-b]quinoxalin-2-amine
-
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1-[3-[(dicyclohexylamino)methyl]-2,4-dihydroxyphenyl]ethanone
-
IC90 (compound concentration at which 90% or higher inhibition is observed) 100 microM, using high-throughput screen, relaxation inhibition 50%
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
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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
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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
-
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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
-
-
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
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-
14-(10'-aminodecyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
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-
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
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-
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
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-
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
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-
14-(7'-aminoheptyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
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-
14-(8'-aminooctyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
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-
14-(9'-aminononyl-1'-aminomethyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trihydrochloride
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-
14-(N,N-dimethylaminomethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
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-
14-(N-ethanolaminomethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11one
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-
14-aminomethyl-12H-5,11a-diazadibenzo[b,h]fluoren-11-one dihydrochloride
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-
14-chloromethyl-12H-5,11a-diazadibenzo[b,h]fluoren-11-one
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-
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
-
-
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
17-beta-3-oxo-18-Norandrost-4-ene-17-carboxylic acid-4-bromo-benzene sulfonic acid ester
-
shows significant inhibition of plasmid supercoil relaxation even at 100 nM concentrations. IC90 (compound concentration at which 90% or higher inhibition is observed) 0.5 microM, using high-throughput screen, relaxation inhibition 50%
17beta-O-[N-(benzyl)carbomyl]-oleanolic acid
-
-
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
2,2'-bis(8-formyl-1,6,7-trihydroxy-5-isopropyl-3-methylnaphthalene)
-
i.e. gossypol, belongs to the class II compounds which interfere with the catalytic function of topoisomerases without generating strand breaks
-
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-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
-
-
2,3-dimethyl-5H-isoindolo[2,1-a]quinoxalin-6-one
-
-
2,4-di(furan-2-yl)-5H-chromeno[4,3-b]pyridine
-
; 46.4% inhibition at 0.1 mM#
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-(2-nitro-vinyl)-1H-indole
-
0.05 mM, 54% vTopo Rnase activity remaining
2-(4-chlorobenzyl)benzoxazole
-
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-(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-carbonyl)-3-(pyridin-2-ylamino)-acrylonitrile
-
0.05 mM, 28% vTopo RNase activity remaining; 0.05 mM, 7% vTopo RNase activity remaining, 2% cTopo relaxation activity remaining
-
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
-
; 11.5% inhibition at 0.1 mM
2-(furan-2-yl)-4-(pyridin-3-yl)-5H-chromeno[4,3-b]pyridine
-
; 41.6% inhibition at 0.1 mM
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
-
; 4.9% inhibition at 0.1 mM
2-(pyridin-2-yl)-4-(pyridin-3-yl)-5H-chromeno[4,3-b]pyridine
-
; 2.6% inhibition at 0.1 mM
2-(pyridin-2-yl)-4-(thiophen-2-yl)-5H-chromeno[4,3-b]pyridine
-
; 48.2% inhibition at 0.1 mM
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