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Literature summary for 5.6.2.2 extracted from
- Inhibition of Leishmania donovani promastigote DNA topoisomerase I and human monocyte DNA topoisomerases I and II by antimonial drugs and classical antitopoisomerase agents (2004), J. Parasitol., 90, 1155-1162.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| camptothecin | 34% inhibition at 0.5 mM | Homo sapiens |  |
| Hoechst 33258 | bis-imidazole derivative | Homo sapiens | |
| Hoechst 33342 | bis-imidazole derivative | Homo sapiens | |
| meglumine antimoniate | 14% inhibition at 0.0033 mM | Homo sapiens | |
| additional information | monocyte cytotoxic effects of inhibitors | Homo sapiens | |
| potassium antimonyl tartrate | 10% inhibition at 0.0033 mM | Homo sapiens | |
| sodium antimonyl(III) gluconate | IC50 is 0.0028 mM | Homo sapiens | |
| sodium stibogluconate | IC50 is 0.0027 mM | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| nucleus | - |
Homo sapiens | 5634 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| monocyte | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| kinetoplast DNA + ATP + H2O | decatenation of kinetoplast DNA | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| DNA topoisomerases II | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | dependent on | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0027 | - |
IC50 is 0.0027 mM | Homo sapiens | sodium stibogluconate | |
| 0.0028 | - |
IC50 is 0.0028 mM | Homo sapiens | sodium antimonyl(III) gluconate | |
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Release 2023.1 (January 2023)
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