Cloned (Comment) | Organism |
---|---|
expression in Pichia pastoris strain SMD 1168 Kex1- | Homo sapiens |
recombinant enzyme expression in Pichia pastoris strain SMD 1168 Kex1- endoplasmic reticulum membranes from a vector encoding (in 5'- to 3'-order): N-terminal alpha-mating factor from Saccharomyces cerevisiae, flag-tag epitope, His10-tag, Tev protease cleavage site, multiple cloning site, C-terminal Tev cleavage site, EGFP, Strep-tag II. The human VKORC1 DNA sequence is inserted into the multiple cloning site | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
warfarin | direct inhibition | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | VKORC1 kinetic modeling, overview | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
membrane | - |
Homo sapiens | 16020 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | Ca2+ might play a role in stabilizing the lipid membranes that surround the VKORC1 protein, but does not affect the DTT-driven enzyme activity | Homo sapiens | |
additional information | EGTA does not affect the DTT-driven enzyme activity | Homo sapiens | |
additional information | human VKOR enzymatic activity is not Ca2+-dependent, no effect by EGTA | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
2,3-epoxyphylloquinone + AH2 | Homo sapiens | - |
phylloquinone + A + ? | - |
? | |
2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O | Homo sapiens | - |
2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Reaction | Comment | Organism | Reaction ID |
---|---|---|---|
phylloquinone + a protein with a disulfide bond + H2O = 2,3-epoxyphylloquinone + a protein with reduced L-cysteine residues | bi bi ping-pong mechanism for VKORC1, kinetic modeling | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
2,3-epoxyphylloquinone + 1,4-dithiothreitol | - |
Homo sapiens | phylloquinone + oxidized dithiothreitol | - |
? | |
2,3-epoxyphylloquinone + AH2 | - |
Homo sapiens | phylloquinone + A + ? | - |
? | |
2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O | - |
Homo sapiens | 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol | - |
? | |
additional information | advantages and caveats of using the DTT-driven VKOR assay, overview | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
vitamin K 2,3-epoxide reductase complex subunit-1 | - |
Homo sapiens |
VKORC1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6 | 7 | - |
Homo sapiens |
7.6 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
dithiothreitol | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | VKORC1 kinetic model and derivation of the IC50-Ki transformation, overview | Homo sapiens | |
0.002633 | - |
warfarin | recombinant enzyme, pH 7.6, 30°C | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00099 | - |
at DTT concentration of over 1 mM, pH 7.6, 30°C | Homo sapiens | warfarin | |
0.00617 | - |
at DTT concentration of 0.1123 mM, pH 7.6, 30°C | Homo sapiens | warfarin | |
0.02363 | - |
at DTT concentration of 0.000296 mM, pH 7.6, 30°C | Homo sapiens | warfarin |
General Information | Comment | Organism |
---|---|---|
physiological function | vitamin K 2,3-epoxide reductase complex subunit 1 is an essential enzyme for proper function of blood coagulation | Homo sapiens |