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Literature summary for 5.6.2.2 extracted from
- Synthesis, biological evaluation, and molecular docking study of 3-(3-heteroatom substituted-2-hydroxy-1-propyloxy) xanthone analogues as novel topoisomerase IIalpha catalytic inhibitor (2011), Eur. J. Med. Chem., 46, 1964-1971.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-hydroxy-3-(oxiran-2-ylmethoxy)-9H-xanthen-9-one | - |
Homo sapiens |  |
| 1-hydroxy-3-[2-hydroxy-3-(2-hydroxyethoxy)propoxy]-9H-xanthen-9-one | 89.25% inhibition at 0.1 mM | Homo sapiens | |
| 1-hydroxy-3-[2-hydroxy-3-(propylamino)propoxy]-9H-xanthen-9-one | 100% inhibition at 0.1 mM. ATPase inhibitory activity, molecular docking, overview. The compound shows a stable binding pattern to the ATP-binding domain of topo II | Homo sapiens | |
| 1-hydroxy-3-[2-hydroxy-3-[(2-hydroxyethyl)amino]propoxy]-9H-xanthen-9-one | 100% inhibition at 0.1 mM | Homo sapiens | |
| 1-hydroxy-3-[2-hydroxy-3-[(2-hydroxyethyl)sulfanyl]propoxy]-9H-xanthen-9-one | 63.75% inhibition at 0.1 mM | Homo sapiens | |
| 1-hydroxy-3-[2-hydroxy-3-[(3-hydroxypropyl)amino]propoxy]-9H-xanthen-9-one | 100% inhibition at 0.1 mM | Homo sapiens | |
| 1-hydroxy-3-[2-hydroxy-3-[(3-hydroxypropyl)sulfanyl]propoxy]-9H-xanthen-9-one | 68% inhibition at 0.1 mM | Homo sapiens | |
| 3-[3-[(2-chloroethyl)sulfanyl]-2-hydroxypropoxy]-1-hydroxy-9H-xanthen-9-one | 45.33% inhibition at 0.1 mM | Homo sapiens | |
| 3-[3-[bis(2-hydroxyethyl)amino]-2-hydroxypropoxy]-1-hydroxy-9H-xanthen-9-one | 100% inhibition at 0.1 mM | Homo sapiens | |
| camptothecin | - |
Homo sapiens | |
| etoposide | 77.7% inhibition at 0.1 mM | Homo sapiens | |
| additional information | molecular docking study, overview | Homo sapiens | |
| novobiocin | inhibits the ATPase activity | 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 | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| DU-145 cell | - |
Homo sapiens | - |
| HCT-116 cell | - |
Homo sapiens | - |
| HeLa cell | - |
Homo sapiens | - |
| HL-60 cell | - |
Homo sapiens | - |
| MDA-MB-231 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | substrate for DNA topo IIalpha is supercoiled pBR322 plasmid DNA | Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | topo II consists of an N-terminal ATP-binding domain, DNA binding/cleavage domain known as the central domain, and a C-terminal tail. The ATP-binding domain is conserved evolutionally and belongs to the GHKL family | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Topo IIalpha | - |
Homo sapiens |
| topoisomerase IIalpha | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at, topo IIalpha activity | Homo sapiens |
| 37 | - |
assay at, ATPase activity | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at, ATPase activity | Homo sapiens |
| 7.9 | - |
assay at, topo IIalpha activity | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | the ATP-binding domain is conserved evolutionally and belongs to the GHKL family | Homo sapiens | |
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