Application | Comment | Organism |
---|---|---|
diagnostics | the enzyme hTopI is a biomarker for camptothecin-based therapy at direct determination of the drug response level | Homo sapiens |
drug development | the enzyme is often upregulated in cancer cells, and it is a target for chemotherapeutic drugs of the camptothecin family | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
camptothecin | response to camptothecin-based treatment is dependent on hTopI activity, and reduction in activity as well as mutations in hTopI result in camptothecin resistance | Homo sapiens | |
additional information | the detection method termed rolling circle enhanced enzyme activity detection allows measurement of hTopI cleavage-religation activity at the single molecule level, and may be used to detect posttranslational enzymatic differences influencing camptothecin response | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
Caco-2 cell | Caco-2 cells have eight copies of the hTOPI gene, they show twofold more hTopI protein, and twofold higher activity of hTopI compared to HT-29 cells, but similar camptothecin sensitivity | Homo sapiens | - |
HT-29 cell | HT-29 cells have five copies of the hTOPI gene, they show twofold less hTopI protein, and twofold lower activity of hTopI compared to Caco-2 cells, but similar camptothecin sensitivity | Homo sapiens | - |
additional information | the enzyme is often upregulated in cancer cells and overexpressed in a wide range of cancers | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | enzyme substrates are S(hTopI)Id16, S(PosC)Id33, and fluorescently labeled detection oligonucleotides ID16-TAMRA and ID33-6FAM | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
hTopI | - |
Homo sapiens |
Topoisomerase I | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |