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Literature summary for 5.6.2.2 extracted from

  • Sorensen, T.K.; Grauslund, M.; Jensen, P.B.; Sehested, M.; Jensen, L.H.
    Separation of bisdioxopiperazine- and vanadate resistance in topoisomerase II (2005), Biochem. Biophys. Res. Commun., 334, 853-860.
    View publication on PubMed
Search for more literature for 5.6.2.2

Activating Compound

Activating Compound Comment Organism Structure
vanadate slight activation of mutant L169F Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
overexpression of wild-type and mutant enzymes in Saccharomyces cerevisiae strain JelDELTATop1 Homo sapiens

Protein Variants

Protein Variants Comment Organism
L169F site-directed mutagenesis, the mutant enzyme is highly resistant to vanadate, the mutant shows reduced DNA passage activity compared to the wild-type enzyme Homo sapiens
L169I site-directed mutagenesis, the mutant shows unaltered DNA passage activity and slightly reduced DNA hyperstimulation compared to the wild-type enzyme Homo sapiens
R162K site-directed mutagenesis, the mutant enzyme is highly resistant to vanadate, but shows only slightly reduced sensitivity to bisdioxopiperazine compared to wild-type enzyme, reduced DNA hyperstimulation and DNA passage activity compared to the wild-type enzyme compared to the wild-type enzyme Homo sapiens
R162Q site-directed mutagenesis, the mutant enzyme is highly resistant to vanadate, the mutant shows no DNA hyperstimulation, nearly no ATPase activity, and reduced DNA passage activity and DNA hyperstimulation compared to the wild-type enzyme Homo sapiens
Y165S site-directed mutagenesis, the mutant enzyme is highly resistant to vanadate, the mutant shows no DNA hyperstimulation, nearly no ATPase activity, and highly reduced DNA passage activity and DNA hyperstimulation compared to the wild-type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
bisdioxopiperazine inhibition of wild-type enzyme and mutant R162K, inhibition mechanism Homo sapiens
vanadate inhibition of wild-type enzyme, no inhibition of mutant R162K, R162Q and Y165S, inhibition mechanism Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.21
-
 DNA pH 7.7, 37°C, DNA passage, mutant R162Q Homo sapiens
0.3
-
 DNA pH 7.7, 37°C, DNA passage, mutant Y165S Homo sapiens
0.39
-
 DNA pH 7.7, 37°C, DNA passage, wild-type enzyme Homo sapiens
0.55
-
 DNA pH 7.7, 37°C, DNA passage, mutant L169I Homo sapiens
0.61
-
 DNA pH 7.7, 37°C, DNA passage, mutant R162K Homo sapiens
0.94
-
 DNA pH 7.7, 37°C, DNA passage, mutant L169F Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
KCl required for DNA passage activity Homo sapiens
Mg2+ required for ATPase and DNA passage activities Homo sapiens
NaCl required for DNA passage activity Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isozyme alpha
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 DNA hyperstimulation rates and ATPase activities of wild-type and mutant enzymes, overview Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dsDNA + ATP + H2O passage of dsDNA Homo sapiens ?
-
 ?
additional information the enzyme has intrinsic ATPase activity Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
Topoisomerase II
-
 Homo sapiens
topoisomerase IIalpha
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.6
-
 DNA pH 7.7, 37°C, DNA passage, mutant Y165S Homo sapiens
1.24
-
 DNA pH 7.7, 37°C, DNA passage, mutant R162Q Homo sapiens
1.65
-
 DNA pH 7.7, 37°C, DNA passage, mutant L169F Homo sapiens
1.8
-
 DNA pH 7.7, 37°C, DNA passage, mutant R162K Homo sapiens
3.33
-
 DNA pH 7.7, 37°C, DNA passage, mutant L169I Homo sapiens
3.38
-
 DNA pH 7.7, 37°C, DNA passage, wild-type enzyme Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 ATPase assay at Homo sapiens
7.7
-
 DNA passage assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens