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Literature summary extracted from

  • Kruczynski, A.; Barret, J.M.; Van Hille, B.; Chansard, N.; Astruc, J.; Menon, Y.; Duchier, C.; Creancier, L.; Hill, B.T.
    Decreased nucleotide excision repair activity and alterations of topoisomerase IIalpha are associated with the in vivo resistance of a P388 leukemia subline to F11782, a novel catalytic inhibitor of topoisomerases I and II (2004), Clin. Cancer Res., 10, 3156-3168.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.6.2.2 DNA sequence determination and analysis of the P388/F11782 cell and the P338 cell enzymes Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.6.2.2 1,3-bis(2-chloroethyl)-1-nitroso-urea P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 5-fluorouracil P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 camptothecin P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 cisplatin P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 Colchicine P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 cyclophosphamide P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 etopophos P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 etoposide P388/F11782 cell enzyme, low inhibition Mus musculus
5.6.2.2 F11782 inhibition of the P388 cell enzyme, mechanism, in vitro resistance of the P388/F11782 cell enzyme to the inhibitor is not associated with a classic multidrug resistance profile, resistant cells show cross-resistance to merbarone and doxorubicin, resistance mechanism Mus musculus
5.6.2.2 irinotecan P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 methotrexate P388/F11782 cell enzyme, low inhibition Mus musculus
5.6.2.2 mitoxanthrone P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 additional information P388/F11782 cells, resistant to F11782, show cross-resistance to merbarone and doxorubicin Mus musculus
5.6.2.2 TAS-103 P388/F11782 cell enzyme, low inhibition Mus musculus
5.6.2.2 Teniposide P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 topotecan P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 vinblastine P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 vinflunine P388/F11782 cell enzyme, high inhibition Mus musculus
5.6.2.2 vinorelbine P388/F11782 cell enzyme, high inhibition Mus musculus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
5.6.2.2 Mg2+
-
 Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
5.6.2.2 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.6.2.2 P-388 cell F11782-resistant P388 leukemia subline P388/F11782, development of the F11782-resistant subclone of P338 leukemia cell line, the cells show reduced enzyme amount and activity Mus musculus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
5.6.2.2 additional information
-
 F11782-resistant cells show reduced enzyme amount and activity Mus musculus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.6.2.2 kinetoplast DNA + ATP + H2O decatenation of kinetoplast DNA Mus musculus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.6.2.2 topoisomerase IIalpha
-
 Mus musculus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
5.6.2.2 37
-
 assay at Mus musculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
5.6.2.2 8
-
 assay at Mus musculus

Cofactor

EC Number Cofactor Comment Organism Structure
5.6.2.2 ATP
-
 Mus musculus