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Literature summary for 3.4.21.6 extracted from
- Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors (2017), Nat. Commun., 8, 528 .
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| F174A | the mutant has about wild type activity | Homo sapiens |
| Y99A | the enzyme shows strongly reduced activity compared to the wild type enzyme | Homo sapiens |
| Y99A/F174A | the enzyme shows severely reduced activity compared to the wild type enzyme | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| antithrombin | irreversible inhibition | Homo sapiens | |
| apixaban | - |
Homo sapiens |  |
| edoxaban | - |
Homo sapiens | |
| recombinant tick saliva anticoagulant protein | - |
Homo sapiens | |
| rivaroxaban | - |
Homo sapiens | |
| TFPIalpha | - |
Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.026 | - |
S-2765 | wild type enzyme, at pH 7.5 and 25°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 | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| glycoprotein | - |
Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| blood plasma | - |
Homo sapiens | - |
| HEK-293 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| prothrombin + H2O | - |
Homo sapiens | thrombin + ? | - |
? | |
| S-2765 + H2O | - |
Homo sapiens | Z-D-Arg-Gly-L-Arg + 4-nitroaniline | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| ? | x * 59000, SDS-PAGE | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| blood coagulation factor Xa | - |
Homo sapiens |
| factor Xa | - |
Homo sapiens |
| FXa | - |
Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 21 | - |
S-2765 | wild type enzyme, at pH 7.5 and 25°C | Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000007 | - |
recombinant tick saliva anticoagulant protein | wild type enzyme, at pH 7.5 and 25°C | Homo sapiens | |
| 0.00000162 | - |
TFPIalpha | wild type enzyme, at pH 7.5 and 25°C | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000002 | - |
wild type enzyme, at pH 7.5 and 25°C | Homo sapiens | edoxaban | |
| 0.000005 | - |
wild type enzyme, at pH 7.5 and 25°C | Homo sapiens | apixaban | |
| 0.000034 | - |
mutant enzyme Y99A, at pH 7.5 and 25°C | Homo sapiens | apixaban | |
| 0.000045 | - |
mutant enzyme F174A, at pH 7.5 and 25°C | Homo sapiens | apixaban | |
| 0.000616 | - |
mutant enzyme Y99A/F174A, at pH 7.5 and 25°C | Homo sapiens | apixaban | |
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