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Literature summary for 1.6.5.2 extracted from

  • Korashy, H.M.; Brocks, D.R.; El-Kadi, A.O.
    Induction of the NAD(P)H:quinone oxidoreductase 1 by ketoconazole and itraconazole: a mechanism of cancer chemoprotection (2007), Cancer Lett., 258, 135-143.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
actinomycin D treatment of the cells with actinomycin D alone for 6 h significantly inhibits the constitutive NQO1 mRNA level by approximately 80%. KTZ- and ITZ-mediated Nqo1 induction is completely inhibited Mus musculus
itraconazole induces NQO1 mRNA and enzymatic activity levels in a concentration- and time-dependent manner in wild-type but not aryl hydrocarbon receptor-deficient Hepa-1c1c7 cells. Increases NQO1 de novo RNA synthesis without significantly affecting the levels of existing RNA. 50 micromol shows maximum NQO1 mRNA induction Mus musculus
ketoconazole induces NQO1 mRNA and enzymatic activity levels in a concentration- and time-dependent manner in wild-type but not aryl hydrocarbon receptor-deficient Hepa-1c1c7 cells. Increases NQO1 de novo RNA synthesis without significantly affecting the levels of existing RNA. 25 micromol shows maximum NQO1 mRNA induction Mus musculus
additional information fluconazole does not induce NQO1 Mus musculus
sulforaphane at a concentration of 5 micromol significantly induces NQO1 mRNA in both wild-type and C12 cells Mus musculus

Application

Application Comment Organism
drug development ability of ketoconazole and itraconazole to induce NQO1 gene expression at the transcriptional level through an aryl hydrocarbon receptor-dependent mechanism Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
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-
-

Source Tissue

Source Tissue Comment Organism Textmining
Hepa-1c1c7 cell
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Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
NAD(P)H + H+ + oxidized 2,6-dichlorophenolindophenol
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Mus musculus NAD(P)+ + reduced 2,6-dichlorophenolindophenol
-
?

Synonyms

Synonyms Comment Organism
DT-diaphorase
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Mus musculus
NAD(P)H:quinone oxidoreductase 1
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Mus musculus
NQO1
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Mus musculus