Literature summary for 5.6.2.2 extracted from

Pitts, S.L.; Jablonksy, M.J.; Duca, M.; Dauzonne, D.; Monneret, C.; Arimondo, P.B.; Anklin, C.; Graves, D.E.; Osheroff, N.
Contributions of the D-ring to the activity of etoposide against human topoisomerase IIalpha: potential interactions with DNA in the ternary enzyme-drug-DNA complex (2011), Biochemistry, 50, 5058-5066.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression of topoisomerase IIalpha in Saccharomyces cerevisiae	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
etoposide	etoposide is a widely prescribed anticancer drug that stabilizes covalent topoisomerase II-cleaved DNA complexes. The drug contains a polycyclic ring system, a glycosidic moiety at C4, and a pendant ring at C1. Interactions between topoisomerase IIalpha and etoposide in the binary enzyme-drug complex are mediated by substituents on the A-, B-, and E-rings of etoposide. The D-ring alterations all decrease the ability of etoposide to enhance DNA cleavage mediated by the enzyme in vitro and in cultured cells, and also weaken etoposide binding in the ternary enzyme-drug-DNA complex and altered sites of enzyme-mediated DNA cleavage. NMR spectroscopic interaction analysis, overview	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	required	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	cleavage of negatively supercoiled pBR322 plasmid DNA by topoisomerase IIalpha	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
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
6.9	-	assay at	Homo sapiens

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Release 2023.1 (January 2023)