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Literature summary for 5.6.2.2 extracted from

  • Bal, C.; Baldeyrou, B.; Moz, F.; Lansiaux, A.; Colson, P.; Kraus-Berthier, L.; Leonce, S.; Pierre, A.; Boussard, M.F.; Rousseau, A.; Wierzbicki, M.; Bailly, C.
    Novel antitumor indenoindole derivatives targeting DNA and topoisomerase II (2004), Biochem. Pharmacol., 68, 1911-1922.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
additional information cytotoxic effects of inhibitors on K562 and K562adr tumor cells, overview Homo sapiens
S35047 a phenyl derivative of 8-[2-(dialkylamino)ethoxy]-2,3-dimethoxy-5H-10H-indenol[1,2-b]indol-10-one-O-propynyl-oxime core structure, inhibition of topoisomerase II, intercalation with DNA causes cytoxic activity Homo sapiens
S35794 a derivative of 8-[2-(dialkylamino)ethoxy]-2,3-dimethoxy-5H-10H-indenol[1,2-b]indol-10-one-O-propynyl-oxime core structure, inhibition of topoisomerase II, intercalation with DNA causes cytoxic activity Homo sapiens
S36699 a derivative of 8-[2-(dialkylamino)ethoxy]-2,3-dimethoxy-5H-10H-indenol[1,2-b]indol-10-one-O-propynyl-oxime core structure, inhibition of topoisomerase II, intercalation with DNA causes cytoxic activity Homo sapiens
S36888 a derivative of 8-[2-(dialkylamino)ethoxy]-2,3-dimethoxy-5H-10H-indenol[1,2-b]indol-10-one-O-propynyl-oxime core structure, inhibition of topoisomerase II, intercalation with DNA causes cytoxic activity Homo sapiens
S36889 a derivative of 8-[2-(dialkylamino)ethoxy]-2,3-dimethoxy-5H-10H-indenol[1,2-b]indol-10-one-O-propynyl-oxime core structure, inhibition of topoisomerase II, intercalation with DNA causes cytoxic activity Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
K-562 cell chronic myeloid leukemia cell line Homo sapiens
-
K-562adr cell adriamycin-resistant K562 cell line Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
supercoiled pKMp27 DNA + ATP + H2O relaxation of supercoiled pKMp27 DNA Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
Topoisomerase II
-
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
7.1
-
in vivo cytotoxic assay at Homo sapiens
7.8
-
in vitro assay at Homo sapiens