Literature summary for 5.6.2.1 extracted from

Proszek, J.; Roy, A.; Jakobsen, A.K.; Fr?hlich, R.; Knudsen, B.R.; Stougaard, M.
Topoisomerase I as a biomarker: detection of activity at the single molecule level (2013), Sensors, 14, 1195-1207.

Search for more literature for 5.6.2.1

Application

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

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

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

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 and Products (Substrate)

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

Synonyms	Comment	Organism
hTopI	-	Homo sapiens
Topoisomerase I	-	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
7.5	-	assay at	Homo sapiens

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Release 2023.1 (January 2023)