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Literature summary for 5.6.2.2 extracted from

  • Insaf, S.; Danks, M.K.; Witiak, D.T.
    Structure-function analysis of DNA topoisomerase II inhibitors (1996), Curr. Med. Chem., 3, 437-466.
No PubMed abstract available
Search for more literature for 5.6.2.2

Activating Compound

Activating Compound Comment Organism Structure
additional information
-
 Homo sapiens
additional information modification by poly(ADP)ribosylation eukaryota
additional information casein kinase II and protein kinase C phosphorylate topoisomerase II. Phosphorylation produces a 2-3fold increase in the catalytic activity eukaryota

Application

Application Comment Organism
pharmacology antitumor effect of inhibitors Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
isoform IIalpha and isoform IIbeta Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4'-(9-acridinylamino)methansulfon-m-anisidide and related quinoline carboxamides eukaryota
Aclarubicin
-
 eukaryota
actinomycins
-
 Homo sapiens
Ametantrone
-
 eukaryota
aurintricarboxylic acid
-
 Homo sapiens
aurintricarboxylic acid
-
 Saccharomyces cerevisiae
Barminomycin-like anthracyclines
-
 Homo sapiens
Benzisoquinolinediones
-
 Homo sapiens
Bisantrene efficiency in patients with breast cancer and acute leukemia Homo sapiens
Bisdioxopiperazines
-
 eukaryota
Bisdioxopiperazines
-
 Mammalia
carminamycin
-
 eukaryota
daunorubicin
-
 eukaryota
Demethylepipodophyllotoxins
-
 eukaryota
doxorubicin
-
 Saccharomyces cerevisiae
ellipticines
-
 eukaryota
ellipticines
-
 Homo sapiens
fostriecin
-
 eukaryota
genistein
-
 eukaryota
idarubicin
-
 eukaryota
idarubicin
-
 Homo sapiens
isoflavones
-
 eukaryota
Merbarone
-
 eukaryota
Merocil
-
 Homo sapiens
Merodantoin
-
 Homo sapiens
Mitoxantrone
-
 eukaryota
additional information
-
 eukaryota
additional information antitumor effect of inhibitors Homo sapiens
additional information
-
 Saccharomyces cerevisiae
N-Trifluoroacetyldoxorubicin-14 valerate
-
 Homo sapiens
Pirarubicin
-
 eukaryota
Pirarubicin
-
 Homo sapiens
quinolones
-
 eukaryota

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information eukaryota enzyme plays a key role in DNA replication and transcription. Required for chromosome segregation during meiosis and mitosis ?
-
 ?
additional information Homo sapiens isoenzyme IIalpha is expressed at the highest level during rapid proliferation, isoenzyme IIbeta is expressed maximally in cells that have reached the plateau phase of growth ?
-
 ?

Organism

Organism UniProt Comment Textmining
eukaryota
-
-
-
Homo sapiens
-
 2 isoenzymes: IIalpha and IIbeta
-
Mammalia
-
-
-
Saccharomyces cerevisiae
-
-
-

Reaction

Reaction Comment Organism Reaction ID
ATP-dependent breakage, passage and rejoining of double-stranded DNA the catalytic cycle of topoisomerase II consists of 5 distinct steps: DNA binding, the pre-strand passage breakage-religation equilibrium, strand passage, the post-strand passage breakage-religation equilibrium and ATP hydrolysis/enzyme turnover eukaryota
a

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information
-
 Saccharomyces cerevisiae ?
-
 ?
additional information no formation of negative supercoils eukaryota ?
-
 ?
additional information enzyme plays a key role in DNA replication and transcription. Required for chromosome segregation during meiosis and mitosis eukaryota ?
-
 ?
additional information isoenzyme IIalpha is expressed at the highest level during rapid proliferation, isoenzyme IIbeta is expressed maximally in cells that have reached the plateau phase of growth Homo sapiens ?
-
 ?
network of DNA rings + ATP + H2O decatenation Mammalia monomeric DNA circles + ADP + phosphate
-
 ?
network of DNA rings + ATP + H2O decatenation eukaryota monomeric DNA circles + ADP + phosphate
-
 ?
network of DNA rings + ATP + H2O decatenation Homo sapiens monomeric DNA circles + ADP + phosphate
-
 ?
network of DNA rings + ATP + H2O decatenation Saccharomyces cerevisiae monomeric DNA circles + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O catenation Mammalia catenated DNA networks + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O catenation eukaryota catenated DNA networks + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O catenation Homo sapiens catenated DNA networks + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O catenation Saccharomyces cerevisiae catenated DNA networks + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O relaxation Mammalia relaxed DNA + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O relaxation eukaryota relaxed DNA + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O relaxation Homo sapiens relaxed DNA + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O relaxation Saccharomyces cerevisiae relaxed DNA + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O ATP-dependent relaxation of negative and positive supercoils eukaryota relaxed DNA + ADP + phosphate
-
 ?
supercoiled DNA + ATP + H2O under optimal conditions the enzyme relaxes all supercoils prior to dissociation of the enzyme from DNA eukaryota relaxed DNA + ADP + phosphate
-
 ?