Literature summary for 5.6.2.2 extracted from

Bandele, O.J.; Osheroff, N.
Bioflavonoids as poisons of human topoisomerase II alpha and II beta (2007), Biochemistry, 46, 6097-6108.

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Activating Compound

Activating Compound	Comment	Organism	Structure
apigenin	0.05 mM, 5fold increase in DNA-cleavage activity for isoform II beta, 2fold increase for isoform II alpha	Homo sapiens
etoposide	0.05 mM, 10fold increase in DNA-cleavage activity for isoform II beta, 6fold increase for isoform II alpha	Homo sapiens
genistein	0.05 mM, 8fold increase in DNA-cleavage activity for isoform II beta, 5fold increase for isoform II alpha	Homo sapiens
luteolin	0.05 mM, 7fold increase in DNA-cleavage activity for isoform II beta, 3fold increase for isoform II alpha	Homo sapiens
additional information	effect of flavones, flavonols, and isoflavones on DNA cleavage activity requires a 5-OH and a 4-OH group and is enhanced by the presence of additional hydroxyl groups on the pendant ring	Homo sapiens
myricetin	0.05 mM, 7fold increase in DNA-cleavage activity for isoform II beta, 4fold increase for isoform II alpha	Homo sapiens
quercetin	0.05 mM, 7fold increase in DNA-cleavage activity for isoform II beta, 4fold increase for isoform II alpha	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
apigenin	inhibition of enzyme-mediated religation of DNA	Homo sapiens
etoposide	inhibition of enzyme-mediated religation of DNA	Homo sapiens
genistein	inhibition of enzyme-mediated religation of DNA	Homo sapiens
luteolin	inhibition of enzyme-mediated religation of DNA	Homo sapiens
myricetin	inhibition of enzyme-mediated religation of DNA	Homo sapiens
quercetin	inhibition of enzyme-mediated religation of DNA	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	isoforms II alpha and II beta	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
CEM cell	leukemia cell	Homo sapiens	-

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Release 2023.1 (January 2023)