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Literature summary for 3.4.21.6 extracted from
- Role of basic residues of the autolysis loop in the catalytic function of factor Xa (2002), Biochemistry, 41, 6780-6788.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of wild-type and mutant zymogens in HEK293 cells, the enzyme is expressed with an introduced cleavage site for for furin-like processing enzymes which is required for expression of the enzyme and for processing of the zymgen to the mature enzyme | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| K147A | site-directed mutagenesis, reduced Km, reduced kcat compared to the wild-type enzyme for the synthetic substrate and for prothrombin as a substrate | Homo sapiens |
| R143A | site-directed mutagenesis, reduced Km, reduced kcat compared to the wild-type enzyme for the synthetic substrate and for prothrombin as a substrate | Homo sapiens |
| R150A | site-directed mutagenesis, reduced Km, reduced kcat compared to the wild-type enzyme for the synthetic substrate and for prothrombin as a substrate | Homo sapiens |
| R154A | site-directed mutagenesis, increased Km, increased kcat for the synthetic substrate, and reduced Km and kcat for prothrombin as a substrate compared to the wild-type enzyme | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| antithrombin | Arg150 of the autolysis loop is involved in specific interaction with the activated conformation of antithrombin | Homo sapiens | |
| tissue factor pathway inhibitor | i.e. TFPI, plasma fXa inhibitor | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | steady state kinetics | Homo sapiens | |
| 0.000018 | - |
prothrombin | recombinant mutant K147A, 22°C | Homo sapiens | |
| 0.000019 | - |
prothrombin | recombinant mutant R143A, 22°C | Homo sapiens | |
| 0.000023 | - |
prothrombin | recombinant mutant R154A, 22°C | Homo sapiens | |
| 0.000025 | - |
prothrombin | recombinant mutant R150A, 22°C | Homo sapiens | |
| 0.000027 | - |
prothrombin | recombinant wild-type enzyme, 22°C | Homo sapiens | |
| 0.000029 | - |
prothrombin | native wild-type enzyme, 22°C | Homo sapiens | |
| 0.065 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant R150A, 22°C | Homo sapiens |  |
| 0.068 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant R143A, 22°C | Homo sapiens | |
| 0.069 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant K147A, 22°C | Homo sapiens | |
| 0.083 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant wild-type enzyme, 22°C | Homo sapiens | |
| 0.09 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | native wild-type enzyme, 22°C | Homo sapiens | |
| 0.122 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant R154A, 22°C | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| extracellular | - |
Homo sapiens | - |
- |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | required | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| prothrombin + H2O | Homo sapiens | - |
thrombin + ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| proteolytic modification | processing and activation of the recombinant wild-type and mutant zymogens to mature enzymes by Russell's viper venom at 37°C and pH 7.4 | Homo sapiens |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant wild-type and mutant zymogens from expression in HEK293 cells, to homogeneity | Homo sapiens |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin | scutelarin has similar specificity, autolysis loop is formed by residues Arg143, Lys147, Arg150, and Arg154 | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | wild-type plasma factor Xa and factor X | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide + H2O | i.e. Spectrozyme FXa, synthetic chromogenic substrate | Homo sapiens | N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine + 4-nitroaniline | - |
? | |
| prothrombin + H2O | - |
Homo sapiens | thrombin + ? | - |
? | |
| prothrombin + H2O | coupled assay method with measurement of thrombin activity against sythetic chromogenic substrate S2238 | Homo sapiens | thrombin + ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | factor Xa is part of the prothrombinase complex with Ca2+, phospholipids and factor Va | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| factor X | zymogen | Homo sapiens |
| factor Xa | mature enzyme | Homo sapiens |
| fX | - |
Homo sapiens |
| FXa | - |
Homo sapiens |
| More | the enzyme belongs to the peptidase family S1, i.e. trypsin family | Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 22 | - |
assay at, room temperature | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 1.4 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant R143A, 22°C | Homo sapiens | |
| 16.9 | - |
prothrombin | recombinant mutant R154A, 22°C | Homo sapiens | |
| 17.2 | - |
prothrombin | recombinant mutant R143A, 22°C | Homo sapiens | |
| 19 | - |
prothrombin | recombinant mutant K147A, 22°C | Homo sapiens | |
| 21 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant R150A, 22°C | Homo sapiens | |
| 21.2 | - |
prothrombin | recombinant mutant R150A, 22°C | Homo sapiens | |
| 23 | - |
prothrombin | recombinant wild-type enzyme, 22°C | Homo sapiens | |
| 26.5 | - |
prothrombin | native wild-type enzyme, 22°C | Homo sapiens | |
| 55 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant K147A, 22°C | Homo sapiens | |
| 98.6 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant R143A, 22°C | Homo sapiens | |
| 121 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | native wild-type enzyme, 22°C | Homo sapiens | |
| 126.5 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant wild-type enzyme, 22°C | Homo sapiens | |
| 127 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant wild-type enzyme, 22°C | Homo sapiens | |
| 411 | - |
N-alpha-benzyloxycarbonyl-D-arginyl-glycyl-L-arginine-4-nitroanilide | recombinant mutant R154A, 22°C | Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00000009 | - |
tissue factor pathway inhibitor | recombinant mutant R150A, 22°C | Homo sapiens | |
| 0.00000011 | - |
tissue factor pathway inhibitor | recombinant wild-type enzyme, 22°C | Homo sapiens | |
| 0.00000014 | - |
tissue factor pathway inhibitor | recombinant mutant R143A, 22°C | Homo sapiens | |
| 0.00000015 | - |
tissue factor pathway inhibitor | native wild-type enzyme, 22°C | Homo sapiens | |
| 0.00000021 | - |
tissue factor pathway inhibitor | recombinant mutant R154A, 22°C | Homo sapiens | |
| 0.00000024 | - |
tissue factor pathway inhibitor | recombinant mutant K147A, 22°C | Homo sapiens |
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