Cloned (Comment) | Organism |
---|---|
recombinant expression of His-tagged wild-type and mutant enzymes in Escherichia coli strain JM109 | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
E158K | naturally occuring mutation and site-directed mutagenesis, the mutant exhibits a significant increase in all the kinetic parameters measured with substrate tamoxifen with nearly two times faster clearance. The mutation has no effect on the clearance of GSK5182 | Homo sapiens |
E308G | naturally occuring mutation and site-directed mutagenesis, the mutant exhibits a significant increase in all the kinetic parameters measured with substrate clomiphene with nearly two times faster clearance. The mutation has no effect on the clearance of GSK5182 | Homo sapiens |
V257M | naturally occuring mutation and site-directed mutagenesis, residue V257 is not in the immediate vicinity of the active site and is part of the hFMO3 insert region in a loop that protrudes from the NADP+-binding domain across the FAD-binding domain, the mutant exhibits a significant increase in all the kinetic parameters measured with substrate clomiphene with nearly two times faster clearance, while the clearance with substrate tamoxifen is reduced. The mutation has no effect on the clearance of GSK5182 | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten steady-state kinetics | Homo sapiens | |
0.00156 | - |
tamoxifen | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
0.0025 | - |
tamoxifen | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens | |
0.00457 | - |
GSK5182 | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
0.0064 | - |
tamoxifen | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens | |
0.0081 | - |
tamoxifen | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens | |
0.00982 | - |
GSK5182 | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens | |
0.0183 | - |
clomiphene | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens | |
0.0205 | - |
clomiphene | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
0.0285 | - |
GSK5182 | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens | |
0.0332 | - |
clomiphene | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens | |
0.0444 | - |
clomiphene | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens | |
0.0587 | - |
GSK5182 | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
membrane | - |
Homo sapiens | 16020 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
clomiphene + NADPH + H+ + O2 | Homo sapiens | clomiphene is used in infertility medication | clomiphene N-oxide + NADP+ + H2O | - |
? | |
GSK5182 + NADPH + H+ + O2 | Homo sapiens | an antidiabetic lead molecule | GSK5182 N-oxide + NADP+ + H2O | - |
? | |
tamoxifen + NADPH + H+ + O2 | Homo sapiens | tamoxifen is used in breast cancer medication | tamoxifen N-oxide + NADP+ + H2O | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P31513 | - |
- |
Purification (Comment) | Organism |
---|---|
recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain JM109 by negative anionic exchange chromatography (the protein is not retained by the DEAE resin at pH 7.4) and nickel affinity chromatography, followed by ultrafiltration | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
clomiphene + NADPH + H+ + O2 | - |
Homo sapiens | clomiphene N-oxide + NADP+ + H2O | - |
? | |
clomiphene + NADPH + H+ + O2 | clomiphene is used in infertility medication | Homo sapiens | clomiphene N-oxide + NADP+ + H2O | - |
? | |
GSK5182 + NADPH + H+ + O2 | - |
Homo sapiens | GSK5182 N-oxide + NADP+ + H2O | - |
? | |
GSK5182 + NADPH + H+ + O2 | an antidiabetic lead molecule | Homo sapiens | GSK5182 N-oxide + NADP+ + H2O | - |
? | |
additional information | identification of GSK5182 N-oxide products by mass spectrometry | Homo sapiens | ? | - |
- |
|
tamoxifen + NADPH + H+ + O2 | - |
Homo sapiens | tamoxifen N-oxide + NADP+ + H2O | - |
? | |
tamoxifen + NADPH + H+ + O2 | tamoxifen is used in breast cancer medication | Homo sapiens | tamoxifen N-oxide + NADP+ + H2O | - |
? |
Subunits | Comment | Organism |
---|---|---|
? | x * 58700, SDS-PAGE | Homo sapiens |
More | the amino acid sequence of PtFMO contains some conserved sequences of FMO: NADPH- and FAD-binding domains | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
flavin-containing monooxygenase 3 | - |
Homo sapiens |
FMO3 | - |
Homo sapiens |
hFMO3 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0012 | - |
clomiphene | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens | |
0.0042 | - |
clomiphene | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens | |
0.005 | - |
clomiphene | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens | |
0.0063 | - |
tamoxifen | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens | |
0.0075 | - |
tamoxifen | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
0.01 | - |
clomiphene | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
0.01 | - |
tamoxifen | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens | |
0.0188 | - |
tamoxifen | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens | |
0.0193 | - |
GSK5182 | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
0.02 | - |
GSK5182 | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens | |
0.037 | - |
GSK5182 | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens | |
0.095 | - |
GSK5182 | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | - |
Homo sapiens | |
NADPH | - |
Homo sapiens |
Organism | Comment | pI Value Maximum | pI Value |
---|---|---|---|
Homo sapiens | isoelectric focusing | - |
8.52 |
General Information | Comment | Organism |
---|---|---|
additional information | enzyme hFMO3 structural modeling with NADP-binding domain and FAD-binding domain with bound cofactors, overview | Homo sapiens |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.151 | - |
clomiphene | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens | |
0.488 | - |
clomiphene | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
0.656 | - |
clomiphene | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens | |
0.946 | - |
clomiphene | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens | |
1.234 | - |
tamoxifen | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens | |
2.52 | - |
tamoxifen | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens | |
2.935 | - |
GSK5182 | recombinant mutant E308G, pH 7.4, 37°C | Homo sapiens | |
3.33 | - |
GSK5182 | recombinant mutant V257M, pH 7.4, 37°C | Homo sapiens | |
3.77 | - |
GSK5182 | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens | |
4.22 | - |
GSK5182 | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
4.81 | - |
tamoxifen | recombinant mutant E158K, pH 7.4, 37°C | Homo sapiens | |
53.19 | - |
tamoxifen | recombinant wild-type enzyme, pH 7.4, 37°C | Homo sapiens |