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Literature summary for 1.14.13.148 extracted from

  • Henderson, M.C.; Siddens, L.K.; Morre, J.T.; Krueger, S.K.; Williams, D.E.
    Metabolism of the anti-tuberculosis drug ethionamide by mouse and human FMO1, FMO2 and FMO3 and mouse and human lung microsomes (2008), Toxicol. Appl. Pharmacol., 233, 420-427.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf9 insect cells Homo sapiens
expressed in Sf9 insect cells Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
Thiourea
-
Homo sapiens
Thiourea thiourea reduces ethionamide oxygenation to ethionamide S-oxide by an average of 73.5% in liver and 76.9% in lung Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.114
-
Ethionamide isozyme FMO3, at pH 9.5 and 37°C Mus musculus
0.336
-
Ethionamide isozyme FMO3, at pH 9.5 and 37°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-
microsome
-
Mus musculus
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P31513
-
-
Mus musculus P97501
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Mus musculus
-
liver FMO3 is the major hepatic isozyme in adults Homo sapiens
-
lung
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ethionamide + NADPH + H+ + O2
-
Homo sapiens ethionamide S-oxide + NADP+ + H2O
-
?
ethionamide + NADPH + H+ + O2
-
Mus musculus ethionamide S-oxide + NADP+ + H2O
-
?

Synonyms

Synonyms Comment Organism
flavin-containing monooxygenase
-
Homo sapiens
flavin-containing monooxygenase
-
Mus musculus
FMO3 isozyme Homo sapiens
FMO3 isozyme Mus musculus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.973
-
Ethionamide isozyme FMO3, at pH 9.5 and 37°C Homo sapiens
1.01
-
Ethionamide isozyme FMO3, at pH 9.5 and 37°C Mus musculus

Cofactor

Cofactor Comment Organism Structure
FAD
-
Homo sapiens
FAD
-
Mus musculus
NADPH required for activity Homo sapiens
NADPH required for activity Mus musculus

General Information

General Information Comment Organism
metabolism isoform FMO3 in human liver may contribute to the toxicity and/or affect efficacy of ethionamide administration Homo sapiens