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Literature summary for 3.4.21.6 extracted from
- Probing the molecular basis of factor Xa specificity by mutagenesis of the serpin, antithrombin (2001), Biochim. Biophys. Acta, 1528, 167-176.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| antithrombin | i.e. HAT, serpin, human, recombinant from expression in human 293 cells, inhibition is increased by heparin | Homo sapiens | |
| antithrombin mutant HAT/Proth-1 | mutant of human antithrombin possessing factor Xa-cleavage site 1 from human thrombin, recombinant from expression in inhuman 293 cells, inactivation of factor Xa is 3-4fold more effective that with mutant HAT/Proth-2, increased inactivation by heparin and 300-500fold by pentasaccharide fragment of heparin | Homo sapiens | |
| antithrombin mutant HAT/Proth-2 | mutant of human antithrombin possessing factor Xa-cleavage site 2 from human thrombin, recombinant from expression in inhuman 293 cells, increased inactivation by heparin and 300-500fold by pentasaccharide fragment of heparin | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00023 | - |
prothrombin | prothrombinase complex, pH 7.4, 22°C | Homo sapiens | |
| 0.0088 | - |
prethrombin-2 | prothrombinase complex, pH 7.4, 22°C | 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 | - |
- |
- |
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, catalytic mechanism | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| prethrombin-2 + H2O | smallest zymogen form of thrombin containing only the factor Xa cleavage site 2 | Homo sapiens | thrombin-2 | - |
? | |
| prothrombin + H2O | - |
Homo sapiens | thrombin + ? | - |
? | |
| prothrombin + H2O | the cleavage site 2 is preferred to cleavage site 1 | Homo sapiens | thrombin + ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | Ca2+, factor Xa and factor Va are part of the prothrombinase enzyme complex | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| factor Xa | - |
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 | - |
room temperature, assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 19.6 | - |
prothrombin | prothrombinase complex, pH 7.4, 22°C | Homo sapiens | |
| 20.5 | - |
prethrombin-2 | prothrombinase complex, pH 7.4, 22°C | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| Factor Va | part of the prothrombinase enzyme complex | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inactivation kinetics of wild-type and mutant antithrombins | Homo sapiens |
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