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Literature summary for 1.14.13.8 extracted from
- Investigation of structure and function of a catalytically efficient variant of the human flavin-containing monooxygenase form 3 (2006), Drug Metab. Dispos., 34, 1995-2002.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of wild-type and mutant isozymes FMO1 and FMO3 as N-terminally maltose-binding-protein fusion and C-terminally His6-tagged proteins in Escherichia coli strain JM109 | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| H360P | site-directed mutagenesis of isozyme FMO1, the mutant shows altered thermal stability and highly increased activity with mercaptoimidazole and chlorpromazine compared to the wild-type FMO1 | Homo sapiens |
| L360A | site-directed mutagenesis of isozyme FMO3, the mutant shows altered thermal stability and reduced activity with mercaptoimidazole, chlorpromazine, and 10-[(N,N-dimethylaminopentyl)-2-(trifluoromethyl)]phenothiazine compared to the wild-type FMO3 | Homo sapiens |
| L360H | site-directed mutagenesis of isozyme FMO3, the mutant shows altered thermal stability and reduced activity with mercaptoimidazole, chlorpromazine, and 10-[(N,N-dimethylaminopentyl)-2-(trifluoromethyl)]phenothiazine compared to the wild-type FMO3 | Homo sapiens |
| L360P | site-directed mutagenesis of isozyme FMO3, the mutant shows altered thermal stability and increased activity with mercaptoimidazole, chlorpromazine, and 10-[(N,N-dimethylaminopentyl)-2-(trifluoromethyl)]phenothiazine compared to the wild-type FMO3 | Homo sapiens |
| L360Q | site-directed mutagenesis of isozyme FMO3, the mutant shows altered thermal stability and reduced activity with mercaptoimidazole, chlorpromazine, and 10-[(N,N-dimethylaminopentyl)-2-(trifluoromethyl)]phenothiazine compared to the wild-type FMO3 | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.018 | - |
mercaptoimidazole | pH 8.4, 37°C, recombinant wild-type His6-tagged MBT-fusion-FMO3 | Homo sapiens |  |
| 0.02 | - |
mercaptoimidazole | pH 8.4, 37°C, recombinant mutant H360P His6-tagged MBT-fusion-FMO1 | Homo sapiens | |
| 0.022 | - |
chlorpromazine | pH 8.4, 37°C, recombinant mutant H360P His6-tagged MBT-fusion-FMO1 | Homo sapiens | |
| 0.022 | - |
mercaptoimidazole | pH 8.4, 37°C, recombinant mutant L360Q His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
| 0.026 | - |
chlorpromazine | pH 8.4, 37°C, recombinant mutant L360P His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
| 0.028 | - |
chlorpromazine | pH 8.4, 37°C, recombinant mutant L360H His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
| 0.03 | - |
mercaptoimidazole | pH 8.4, 37°C, recombinant wild-type His6-tagged MBT-fusion-FMO1 | Homo sapiens | |
| 0.034 | - |
mercaptoimidazole | pH 8.4, 37°C, recombinant mutant L360P His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
| 0.038 | - |
mercaptoimidazole | pH 8.4, 37°C, recombinant mutant L360H His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
| 0.046 | - |
mercaptoimidazole | pH 8.4, 37°C, recombinant mutant L360A His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
| 0.058 | - |
chlorpromazine | pH 8.4, 37°C, recombinant wild-type His6-tagged MBT-fusion-FMO1 | Homo sapiens | |
| 0.061 | - |
chlorpromazine | pH 8.4, 37°C, recombinant wild-type His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
| 0.076 | - |
chlorpromazine | pH 8.4, 37°C, recombinant mutant L360Q His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
| 0.08 | - |
chlorpromazine | pH 8.4, 37°C, recombinant mutant L360A His6-tagged MBT-fusion-FMO3 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
isozymes FMO1 and FMO3 | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
substrate specificity of recombinant wild-type and mutant His6-tagged MBT-fusion-FMO3s, overview | Homo sapiens |
| 0.0046 | 0.0073 | recombinant wild-type and mutant His6-tagged MBT-fusion-FMO3s | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 10-[(N,N-dimethylaminopentyl)-2-(trifluoromethyl)]phenothiazine + NADPH + O2 | i.e. 5-DPT or diethylenetriaminepentaacetic acid | Homo sapiens | ? | - |
? | |
| chlorpromazine + NADPH + O2 | - |
Homo sapiens | chlorpromazine N-oxide + NADP+ + H2O | - |
? | |
| mercaptoimidazole + NADPH + O2 | - |
Homo sapiens | mercaptoimidazole S-oxide + NADP+ + H2O | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | molecular modeling of the FMO3 structure | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| FMO | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 3 | - |
assay at | Homo sapiens |
Temperature Stability [°C]
| Temperature Stability Minimum [°C] | Temperature Stability Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 40 | - |
in absence of NADPH, residue 360 is important for thermal stability, half-lives of wild-type and mutant isozymes FMO1 and FMO3, overview | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8.4 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| FAD | - |
Homo sapiens | |
| NADPH | - |
Homo sapiens | |
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