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Literature summary 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

Activating Compound

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

Application

EC Number Application Comment Organism
5.6.2.2 pharmacology antitumor effect of inhibitors Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.6.2.2 isoform IIalpha and isoform IIbeta Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.6.2.2 4'-(9-acridinylamino)methansulfon-m-anisidide and related quinoline carboxamides eukaryota
5.6.2.2 Aclarubicin
-
 eukaryota
5.6.2.2 actinomycins
-
 Homo sapiens
5.6.2.2 Ametantrone
-
 eukaryota
5.6.2.2 aurintricarboxylic acid
-
 Homo sapiens
5.6.2.2 aurintricarboxylic acid
-
 Saccharomyces cerevisiae
5.6.2.2 Barminomycin-like anthracyclines
-
 Homo sapiens
5.6.2.2 Benzisoquinolinediones
-
 Homo sapiens
5.6.2.2 Bisantrene efficiency in patients with breast cancer and acute leukemia Homo sapiens
5.6.2.2 Bisdioxopiperazines
-
 Mammalia
5.6.2.2 Bisdioxopiperazines
-
 eukaryota
5.6.2.2 carminamycin
-
 eukaryota
5.6.2.2 daunorubicin
-
 eukaryota
5.6.2.2 Demethylepipodophyllotoxins
-
 eukaryota
5.6.2.2 doxorubicin
-
 Saccharomyces cerevisiae
5.6.2.2 ellipticines
-
 Homo sapiens
5.6.2.2 ellipticines
-
 eukaryota
5.6.2.2 fostriecin
-
 eukaryota
5.6.2.2 genistein
-
 eukaryota
5.6.2.2 idarubicin
-
 Homo sapiens
5.6.2.2 idarubicin
-
 eukaryota
5.6.2.2 isoflavones
-
 eukaryota
5.6.2.2 Merbarone
-
 eukaryota
5.6.2.2 Merocil
-
 Homo sapiens
5.6.2.2 Merodantoin
-
 Homo sapiens
5.6.2.2 Mitoxantrone
-
 eukaryota
5.6.2.2 additional information antitumor effect of inhibitors Homo sapiens
5.6.2.2 additional information
-
 Saccharomyces cerevisiae
5.6.2.2 additional information
-
 eukaryota
5.6.2.2 N-Trifluoroacetyldoxorubicin-14 valerate
-
 Homo sapiens
5.6.2.2 Pirarubicin
-
 Homo sapiens
5.6.2.2 Pirarubicin
-
 eukaryota
5.6.2.2 quinolones
-
 eukaryota

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.6.2.2 additional information eukaryota enzyme plays a key role in DNA replication and transcription. Required for chromosome segregation during meiosis and mitosis ?
-
 ?
5.6.2.2 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

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

Reaction

EC Number Reaction Comment Organism Reaction ID
5.6.2.2 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)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.6.2.2 additional information
-
 Saccharomyces cerevisiae ?
-
 ?
5.6.2.2 additional information no formation of negative supercoils eukaryota ?
-
 ?
5.6.2.2 additional information enzyme plays a key role in DNA replication and transcription. Required for chromosome segregation during meiosis and mitosis eukaryota ?
-
 ?
5.6.2.2 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 ?
-
 ?
5.6.2.2 network of DNA rings + ATP + H2O decatenation Mammalia monomeric DNA circles + ADP + phosphate
-
 ?
5.6.2.2 network of DNA rings + ATP + H2O decatenation eukaryota monomeric DNA circles + ADP + phosphate
-
 ?
5.6.2.2 network of DNA rings + ATP + H2O decatenation Homo sapiens monomeric DNA circles + ADP + phosphate
-
 ?
5.6.2.2 network of DNA rings + ATP + H2O decatenation Saccharomyces cerevisiae monomeric DNA circles + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O catenation Mammalia catenated DNA networks + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O catenation eukaryota catenated DNA networks + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O catenation Homo sapiens catenated DNA networks + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O catenation Saccharomyces cerevisiae catenated DNA networks + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O relaxation Mammalia relaxed DNA + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O relaxation eukaryota relaxed DNA + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O relaxation Homo sapiens relaxed DNA + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O relaxation Saccharomyces cerevisiae relaxed DNA + ADP + phosphate
-
 ?
5.6.2.2 supercoiled DNA + ATP + H2O ATP-dependent relaxation of negative and positive supercoils eukaryota relaxed DNA + ADP + phosphate
-
 ?
5.6.2.2 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
-
 ?