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Literature summary for 5.6.2.2 extracted from

  • Mudeppa, D.G.; Kumar, S.; Kokkonda, S.; White, J.; Rathod, P.K.
    Topoisomerase II from human malaria parasites expression, purification, and selective inhibition (2015), J. Biol. Chem., 290, 20313-20324 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in a wheat germ cell-free transcription-translation system Plasmodium falciparum

Protein Variants

Protein Variants Comment Organism
Y829A active-site mutant Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
Ciprofloxacin
-
Plasmodium falciparum
etoposide
-
Plasmodium falciparum
GSK299423
-
Plasmodium falciparum

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ 10 mM used in assay conditions Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + catenated kinetoplast DNA
-
Plasmodium falciparum ADP + phosphate + decatenated kinetoplast DNA
-
?
ATP + supercoiled pUC18 plasmid
-
Plasmodium falciparum ADP + phosphate + relaxed pUC18 plasmid
-
?

Synonyms

Synonyms Comment Organism
TOPOII
-
Plasmodium falciparum
Topoisomerase II
-
Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0006
-
at pH 8.0 and 26°C Plasmodium falciparum GSK299423
0.02
-
at pH 8.0 and 26°C Plasmodium falciparum etoposide
0.035
-
at pH 8.0 and 26°C Plasmodium falciparum Ciprofloxacin