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Literature summary for 5.6.2.2 extracted from
- A cysteine-reactive alkyl hydroquinone modifies topoisomerase IIalpha, enhances DNA breakage, and induces apoptosis in cancer cells (2012), Chem. Res. Toxicol., 25, 2340-2351.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 10'(Z),13'(E),15'(E)-heptadecatrienyl hydroquinone | i.e. HQ17(3), the cysteine-reactive alkyl hydroquinone modifies topoisomerase IIalpha, enhances DNA breakage, and induces apoptosis in cancer cells, it is attributed to topoisomerase IIalpha poisoning and the induction of oxidative damage. Irreversibly inhibits Topo IIalpha activity in vitro and is more cytotoxic in leukemia HL-60 cells than in Topo IIalpha-deficient variant HL-60/MX2 cell. HQ17(3) reacts with Cys427, Cys733, and Cys997 of recombinant Topo IIalpha in vitro, whereas it reacts with Cys427 of cellular Topo IIalpha in Huh7 hepatoma cells. The cells, HQ17(3) treatment causes prompt inhibition of DNA synthesis and consequently induces the expression of DNA damage-related genes DDIT3, GADD45A, and GADD45G. Topo IIalpha inhibition, apoptosis, and oxidative stress account for cytotoxicity caused by HQ17(3). Pretreatment of Huh7 cells with N-acetylcysteine partially attenuates mitochondrial membrane damage, DNA breakage, and caspase activation, but does not diminish HQ17(3)-induced cell death | Homo sapiens |  |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| nucleus | - |
Homo sapiens | 5634 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Homo sapiens | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 170000 | - |
- |
Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| HL-60 cell | - |
Homo sapiens | - |
| Huh-7 cell | a hepatocyte-derived cellular carcinoma cell line | Homo sapiens | - |
| additional information | no activity in HL-60/MX2 cells | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | DNA strand breakage formation in vitro assay using RF-f1p supercoiled DNA | 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 |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.9 | 8 | assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
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