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Literature summary for 5.6.2.2 extracted from
- High-yield production and characterization of biologically active GST-tagged human topoisomerase IIalpha protein in insect cells for the development of a high-throughput assay (2011), Protein Expr. Purif., 76, 165-172.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of GST-tagged isozyme topo2alpha in Spodoptera frugiperda Sf9 cells using the baculovirus transfection system | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| Ciprofloxacin | a topoisomerase II inhibitor | Homo sapiens |  |
| etoposide | a topoisomerase IIalpha inhibitor | Homo sapiens | |
| quercetin | a topoisomerase IIalpha inhibitor | Homo sapiens | |
| suramin | a topoisomerase IIalpha inhibitor | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000012 | - |
Supercoiled DNA | pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| nucleus | - |
Homo sapiens | 5634 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P11388 | topoisomerase IIalpha | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant GST-tagged isozyme topo2alpha from Sf9 insect cells by nuclei preparation, glutathione affinity chromatography, and gel filtration | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| supercoiled DNA + ATP + H2O | substrate is supercoiled scpBR322 plasmid DNA. Topo2a creates transient breaks in supercoiled DNA in an ATP-dependent manner resulting in DNA relaxation | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| topo2alpha | - |
Homo sapiens |
| topoisomerase IIalpha | - |
Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
DNA relaxation and ATPase assays at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | dependent on | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0003 | - |
inhibition of DNA relaxation activity, pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens | suramin | |
| 0.0036 | - |
inhibition of ATPase activity, pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens | quercetin | |
| 0.021 | - |
inhibition of ATPase activity, pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens | suramin | |
| 0.021 | - |
inhibition of ATPase activity, pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens | etoposide | |
| 0.0277 | - |
inhibition of DNA relaxation activity, pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens | quercetin | |
| 0.0589 | - |
inhibition of DNA relaxation activity, pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens | etoposide | |
| 0.1695 | - |
inhibition of DNA relaxation activity, pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens | Ciprofloxacin | |
| 0.797 | - |
inhibition of ATPase activity, pH 8.0, temperature not specified in the publication, recombinant topo2alpha | Homo sapiens | Ciprofloxacin | |
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