Any feedback?
Literature summary for 5.6.2.2 extracted from
- Cytotoxicity and inhibitory properties against topoisomerase II of doxorubicin and its formamidine derivatives (2009), Acta Biochim. Pol., 56, 135-142.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | class of anthracyclines seems to be a good source for selection of anticancer drugs directed toward cancer cells with the developed multidrug resistance attributed to the presence of altered DNA topoisomerase II | Mus musculus |
| drug development | class of anthracyclines seems to be a good source for selection of anticancer drugs directed toward cancer cells with the developed multidrug resistance attributed to the presence of altered DNA topoisomerase II | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| doxorubicin | the presence of the formamidino group in the doxorubicin molecule reduced its ability to stimulate DNA cleavage by DNA topoisomerase II | Homo sapiens |  |
| doxorubicin | the presence of the formamidino group in the doxorubicin molecule reduced its ability to stimulate DNA cleavage by DNA topoisomerase II | Mus musculus | |
| etoposide | a DNA topoisomerase II trapping agent with cytotoxic effect | Mus musculus | |
| hexamethyleneimine | the presence of the formamidino group in the molecule reduced its ability to stimulate DNA cleavage byDNA topoisomerase II, which is not a primary cellular target for the compound | Homo sapiens | |
| hexamethyleneimine | the presence of the formamidino group in the molecule reduced its ability to stimulate DNA cleavage byDNA topoisomerase II, which is not a primary cellular target for the compound | Mus musculus | |
| ICRF-187 | - |
Mus musculus | |
| additional information | cytotoxic activity of anthracyclines toward cancer cells, mechanism of DNA break formation by anthracyclines, overview | Homo sapiens | |
| additional information | cytotoxic activity of anthracyclines toward L1210 cells, mechanism of DNA break formation by anthracyclines, and role of the stabilization of DNA topoisomerase II in the mechanism of cell killing by the anthracyclines, overview | Mus musculus | |
| morpholine | amine derivative of doxorubicin, the presence of the formamidino group in the molecule reduces its ability to stimulate DNA cleavage by DNA topoisomerase II, which is not a primary cellular target for the compound | Homo sapiens | |
| morpholine | amine derivative of doxorubicin, the presence of the formamidino group in the molecule reduces its ability to stimulate DNA cleavage by DNA topoisomerase II, which is not a primary cellular target for the compound | Mus musculus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| nucleus | - |
Mus musculus | 5634 | - |
| nucleus | - |
Homo sapiens | 5634 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Mus musculus | |
| Mg2+ | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| L-1210 cell | leukemia cell line | Mus musculus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | substrate is supercoiled pBR322 DNA | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Topoisomerase II | - |
Mus musculus |
| Topoisomerase II | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Mus musculus |
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Mus musculus |
| 7.5 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Mus musculus | |
| ATP | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000183 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells | Mus musculus | doxorubicin | |
| 0.0000244 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells | Mus musculus | morpholine | |
| 0.000026 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells in presence of inhibitor ICRF-187 | Mus musculus | morpholine | |
| 0.0000314 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells in presence of inhibitor ICRF-187 | Mus musculus | doxorubicin | |
| 0.0000908 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells in presence of inhibitor ICRF-187 | Mus musculus | hexamethyleneimine | |
| 0.0000908 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells in presence of inhibitor ICRF-187 | Mus musculus | hexamethyleneimin | |
| 0.000094 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells | Mus musculus | hexamethyleneimine | |
| 0.000094 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells | Mus musculus | hexamethyleneimin | |
| 0.000329 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells | Mus musculus | etoposide | |
| 0.000585 | - |
pH 7.5, 37°C, cytotoxicity assay in L1210 cells in presence of inhibitor ICRF-187 | Mus musculus | etoposide | |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
