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Literature summary for 1.14.13.8 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
Search for more literature for 1.14.13.8

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
additional information no inhibition of S-oxygenation of ethionamide by SKF-525A Homo sapiens
additional information lack of inhibition of S-oxygenation of ethionamide by SKF-525A Mus musculus
Thiourea inhibits S-oxygenation of ethionamide Homo sapiens
Thiourea inhibits S-oxygenation of ethionamide; thiourea reduces ethionamide oxygenation to ethionamide S-oxide by an average of 73.5% in liver and 76.9% in lung; 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
0.104
-
 Ethionamide 37°C, isozyme FMO1 Mus musculus
0.104
-
 Ethionamide isozyme FMO1, at pH 9.5 and 37°C Mus musculus
0.105
-
 Ethionamide 37°C, isozyme FMO1 Homo sapiens
0.105
-
 Ethionamide isozyme FMO1, at pH 9.5 and 37°C Homo sapiens
0.114
-
 Ethionamide 37°C, isozyme FMO3 Mus musculus
0.261
-
 Ethionamide 37°C, isozyme FMO2 Homo sapiens
0.261
-
 Ethionamide isozyme FMO2, at pH 9.5 and 37°C Homo sapiens
0.336
-
 Ethionamide 37°C, isozyme FMO3 Homo sapiens
2.131
-
 Ethionamide 37°C, isozyme FMO2 Mus musculus
2.131
-
 Ethionamide isozyme FMO2, at pH 9.5 and 37°C Mus musculus

Localization

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ethionamide + NADPH + H+ + O2 Mus musculus ethionamide is a pro-drug requiring bioactivation to exert toxicity ethionamide S-oxide + NADP+ + H2O
-
 ?
ethionamide + NADPH + H+ + O2 Homo sapiens ethionamide is a pro-drug requiring bioactivation to exert toxicity ethionamide S-oxide + NADP+ + H2O
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens Q01740
-
-
Homo sapiens Q99518
-
-
Mus musculus
-
 Swiss/Webster mice
-
Mus musculus P50285
-
-
Mus musculus Q8K2I3
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Mus musculus
-
liver
-
 Homo sapiens
-
liver in human fetal liver, the major isozyme is FMO1 Homo sapiens
-
lung
-
 Mus musculus
-
lung
-
 Homo sapiens
-
lung isozyme FMO2 is expressed at high levels in lung Homo sapiens
-

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
-
 ?
ethionamide + NADPH + H+ + O2 ethionamide is a pro-drug requiring bioactivation to exert toxicity Mus musculus ethionamide S-oxide + NADP+ + H2O
-
 ?
ethionamide + NADPH + H+ + O2 ethionamide is a pro-drug requiring bioactivation to exert toxicity Homo sapiens ethionamide S-oxide + NADP+ + H2O
-
 ?
ethionamide + NADPH + H+ + O2 i.e. ETA, S-oxygenation by isozymes FMO1, FMO2, and FMO3 Mus musculus ethionamide S-oxide + NADP+ + H2O
-
 ?
ethionamide + NADPH + H+ + O2 i.e. ETA, S-oxygenation by isozymes FMO1, FMO2, and FMO3 Homo sapiens ethionamide S-oxide + NADP+ + H2O
-
 ?

Synonyms

Synonyms Comment Organism
flavin-containing monooxygenase
-
 Homo sapiens
flavin-containing monooxygenase
-
 Mus musculus
FMO1
-
 Mus musculus
FMO1
-
 Homo sapiens
FMO1 isozyme Homo sapiens
FMO1 isozyme Mus musculus
FMO2
-
 Mus musculus
FMO2
-
 Homo sapiens
FMO2 isozyme Homo sapiens
FMO2 isozyme Mus musculus
FMO3
-
 Mus musculus
FMO3
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Mus musculus
37
-
 assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.805
-
 Ethionamide 37°C, isozyme FMO2 Homo sapiens
0.805
-
 Ethionamide isozyme FMO2, at pH 9.5 and 37°C Homo sapiens
0.973
-
 Ethionamide 37°C, isozyme FMO3 Homo sapiens
1.01
-
 Ethionamide 37°C, isozyme FMO3 Mus musculus
1.5
-
 Ethionamide 37°C, isozyme FMO1 Homo sapiens
1.5
-
 Ethionamide isozyme FMO1, at pH 9.5 and 37°C Homo sapiens
4.52
-
 Ethionamide 37°C, isozyme FMO1 Mus musculus
4.52
-
 Ethionamide isozyme FMO1, at pH 9.5 and 37°C Mus musculus
9.45
-
 Ethionamide 37°C, isozyme FMO2 Mus musculus
9.45
-
 Ethionamide isozyme FMO2, at pH 9.5 and 37°C Mus musculus

Cofactor

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

General Information

General Information Comment Organism
metabolism the enzyme is involved in metabolism of the anti-tuberculosis drug ethionamide in lung and liver, overview Mus musculus
metabolism the enzyme is involved in metabolism of the anti-tuberculosis drug ethionamide in lung and liver, overview Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.0028
-
 Ethionamide 37°C, isozyme FMO3 Homo sapiens
0.0032
-
 Ethionamide 37°C, isozyme FMO2 Homo sapiens
0.0035
-
 Ethionamide 37°C, isozyme FMO2 Mus musculus
0.0088
-
 Ethionamide 37°C, isozyme FMO3 Mus musculus
0.014
-
 Ethionamide 37°C, isozyme FMO1 Homo sapiens
0.044
-
 Ethionamide 37°C, isozyme FMO1 Mus musculus