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Literature summary extracted from
- Novel and specific inhibitors of a poxvirus type I topoisomerase (2006), Mol. Pharmacol., 69, 547-557.
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 5.6.2.1 | drug development | potential target for drug treatment against smallpox and molluscum contagiosum virus | Homo sapiens |
| 5.6.2.1 | drug development | potential target for drug treatment against smallpox and molluscum contagiosum virus | Vaccinia virus |
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 5.6.2.1 | - |
Vaccinia virus |
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 5.6.2.1 | Y274F | vaccinia topoisomerase mutant, lacks active site tyrosine nucleophile but binds to DNA containing specific recognition sequence, like wild type vTopo | Vaccinia virus |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 5.6.2.1 | 1,2'-binaphthalene-7',8-dicarboxylic acid | 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% | Vaccinia virus |  |
| 5.6.2.1 | 1,3-bis(4-amino-2-methylquinolin-6-yl)urea | IC90 (compound concentration at which 90% or higher inhibition is observed) 2 microM, using high-throughput screen, relaxation inhibition 40% | Vaccinia virus | |
| 5.6.2.1 | 1-(3,4-dihydroxybenzyl)isoquinoline-6,7-diol | IC90 (compound concentration at which 90% or higher inhibition is observed) 10 microM, using high-throughput screen, relaxation inhibition 80% | Vaccinia virus | |
| 5.6.2.1 | 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% | Vaccinia virus | |
| 5.6.2.1 | 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 | Homo sapiens | |
| 5.6.2.1 | 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% | Vaccinia virus | |
| 5.6.2.1 | 2-methylidenebutanedioic acid | IC90 (compound concentration at which 90% or higher inhibition is observed) 10 microM, using high-throughput screen, relaxation inhibition 100% | Vaccinia virus | |
| 5.6.2.1 | 2-[[2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-3,4-dihydro-2H-chromen-3-yl]oxy]-2-(3,4,5-trihydroxyphenyl)-3,4-dihydro-2H-chromene-3,4,5,7-tetrol | IC90 (compound concentration at which 90% or higher inhibition is observed) 0.5 microM, using high-throughput screen, relaxation inhibition 70%; IC90 (compound concentration at which 90% or higher inhibition is observed) 1 microM, using high-throughput screen, relaxation inhibition 100% | Vaccinia virus | |
| 5.6.2.1 | 4,4',4'',4'''-ethane-1,1,2,2-tetrayltetrakis(2,6-dichlorophenol) | IC90 (compound concentration at which 90% or higher inhibition is observed) 10 microM, using high-throughput screen, relaxation inhibition 60% | Vaccinia virus | |
| 5.6.2.1 | 4,4-bis(3,5-dibromo-4-hydroxyphenyl)pentanoic acid | IC90 (compound concentration at which 90% or higher inhibition is observed) 1 microM, using high-throughput screen, relaxation inhibition 100% | Vaccinia virus | |
| 5.6.2.1 | 4-[(2-carboxyphenyl)carbonyl]benzene-1,2-dicarboxylic acid | IC90 (compound concentration at which 90% or higher inhibition is observed) 1 microM, using high-throughput screen, relaxation inhibition 100% | Vaccinia virus | |
| 5.6.2.1 | 4-[(6-chloro-2-methoxyacridin-9-yl)amino]-2-[(4-methylpiperazin-1-yl)methyl]phenol | IC90 (compound concentration at which 90% or higher inhibition is observed) 100 microM, using high-throughput screen, relaxation inhibition 100% | Vaccinia virus | |
| 5.6.2.1 | 4-[[(2-fluorophenyl)carbamoyl]amino]benzenesulfonamide | IC90 (compound concentration at which 90% or higher inhibition is observed) 100 microM, using high-throughput screen, relaxation inhibition 40% | Vaccinia virus | |
| 5.6.2.1 | 4-[[2-(6-amino-8-oxo-1,2,3,4,5,8-hexahydropyrido[2,3-b]pyrazin-2-yl)ethyl]amino]benzoic acid | IC90 (compound concentration at which 90% or higher inhibition is observed) 100 microM, using high-throughput screen, relaxation inhibition 100% | Vaccinia virus | |
| 5.6.2.1 | 5,5'-(1,1'-dihydroxy-8,8'-dimethoxy-6,6'-dimethyl-2,2'-binaphthalene-4,4'-diyl)bis(1,3-dimethyl-1,2,3,4-tetrahydroisoquinoline-6,8-diol) | IC90 (compound concentration at which 90% or higher inhibition is observed) 10 microM, using high-throughput screen, relaxation inhibition 40% | Vaccinia virus | |
| 5.6.2.1 | 5-(2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyl-6-[(4-methylphenyl)sulfonyl]tetrahydrofuro[2,3-d][1,3]dioxole | shows significant inhibition of plasmid supercoil relaxation even at 100 nM concentrations. IC90 (compound concentration at which 90% or higher inhibition is observed) 1 microM, using high-throughput screen, relaxation inhibition 50% | Vaccinia virus | |
| 5.6.2.1 | 5-[[3-(dimethylamino)propyl]amino]-3-methylpyrimido[4,5-b]quinoline-2,4(3H,4aH)-dione | IC90 (compound concentration at which 90% or higher inhibition is observed) 5 microM, using high-throughput screen, relaxation inhibition 70% | Vaccinia virus | |
| 5.6.2.1 | 7,8-dimethoxy-2-pyridin-4-yl-4H-chromen-4-one | IC90 (compound concentration at which 90% or higher inhibition is observed) 10 microM, using high-throughput screen, relaxation inhibition 100% | Vaccinia virus | |
| 5.6.2.1 | biphenyl-3,4'-diylbis(arsonic acid) | shows significant inhibition of plasmid supercoil relaxation even at 100 nM concentrations. IC90 (compound concentration at which 90% or higher inhibition is observed) 0.1 microM, using high-throughput screen, relaxation inhibition 50% | Vaccinia virus | |
| 5.6.2.1 | dibiphenyl-4-yl(hydroxy)acetic acid | IC90 (compound concentration at which 90% or higher inhibition is observed) 1 microM, using high-throughput screen, relaxation inhibition 100% | Vaccinia virus | |
| 5.6.2.1 | dihydroxy[4-[(2-hydroxyethyl)sulfamoyl]phenyl]oxoantimonate(2-) | does not inhibit supercoil relaxation at 10 microM concentration. IC90 (compound concentration at which 90% or higher inhibition is observed) 5 microM, using high-throughput screen, relaxation inhibition 0% | Vaccinia virus | |
| 5.6.2.1 | additional information | biphenyl-3,4'-diylbis(arsonic acid) and 5-(2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyl-6-[(4-methylphenyl)sulfonyl]tetrahydrofuro[2,3-d][1,3]dioxole show no inhibition even at compound concentrations of 20 microM | Homo sapiens | |
| 5.6.2.1 | additional information | using molecular beacon assay for topo I to blindly screen a 1990-member small-molecule library and to identify several specific inhibitors of the poxvirus topoisomerase | Vaccinia virus | |
| 5.6.2.1 | N,N,N-trimethyl-1H-pyridazino[4,3-b][1,4]benzothiazin-3-aminium | IC90 (compound concentration at which 90% or higher inhibition is observed) 100 microM, using high-throughput screen, relaxation inhibition 50% | Vaccinia virus | |
| 5.6.2.1 | phenazine-2,7-diylbis(arsonic acid) | IC90 (compound concentration at which 90% or higher inhibition is observed) 100 microM, using high-throughput screen, relaxation inhibition 50% | Vaccinia virus | |
| 5.6.2.1 | [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 | Homo sapiens | |
| 5.6.2.1 | [3-[(E)-2-carboxyethenyl]phenyl](dihydroxy)oxoantimonate(2-) | shows significant inhibition of plasmid supercoil relaxation even at 100 nM concentrations. IC90 (compound concentration at which 90% or higher inhibition is observed) 0.1 microM, using high-throughput screen, relaxation inhibition 70% | Vaccinia virus | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 5.6.2.1 | Homo sapiens | - |
- |
- |
| 5.6.2.1 | Vaccinia virus | - |
- |
- |
Purification (Commentary)
| EC Number | Purification (Comment) | Organism |
|---|---|---|
| 5.6.2.1 | - |
Vaccinia virus |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 5.6.2.1 | DNA topoisomerase | - |
Homo sapiens |
| 5.6.2.1 | DNA topoisomerase | - |
Vaccinia virus |
| 5.6.2.1 | hTopo | - |
Homo sapiens |
| 5.6.2.1 | vTopo | closely related to the human type I topoisomerase (hTopo) | Vaccinia virus |
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