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Literature summary for 1.14.13.148 extracted from

  • Adali, O.; Carver, G.C.; Philpot, R.M.
    The effect of arginine-428 mutation on modulation of activity of human liver flavin monooxygenase 3 (FMO3) by imipramine and chlorpromazine (1999), Exp. Toxicol. Pathol., 51, 271-276.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
chlorpromazine the activity of the native enzyme is increased at 0.001-0.2 mM of chlorpromazine. Greatest activation is 85% when methimazole and chlorpromazine concentrations are 2 mM and 0.1 mM, respectively Homo sapiens
imipramine the activity of the native enzyme is increased at 0.05-0.75 mM of imipramine Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Homo sapiens

Protein Variants

Protein Variants Comment Organism
T428R methimazole activity of the mutant enzyme is stimulated (maximally 25% when the methimazole concentration is 2 mM) to the same extend of native enzyme up to an imipramine concentration of 3 mM. The activity of the mutant is inhibited at concentrations above 0.3 mM imipramine, 0.75 mM imipramine causes 93% inhibition of methimazole activity of the mutant enzyme. Chlorpromazine activates the mutant enzyme only at high substrate concentrations (0.1-2 mM) Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0285
-
Methimazole mutant enzyme, at pH and 37°C Homo sapiens
0.03
-
Methimazole native enzyme, at pH and 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
methimazole + NADPH + H+ + O2
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
EC 1.14.13.8 assigned to Homo sapiens
flavin monooxygenase 3
-
Homo sapiens
flavin-containing monooxygenase
-
Homo sapiens
FMO3
-
Homo sapiens

Cofactor

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