Protein Variants | Comment | Organism |
---|---|---|
G372A | mutant G372A, both in the free and tissue factor-bound form, exhibit reduced cleavage of factor X and of D-Ile-Pro-Arg-4-nitroanilide (kcat increased compared to wild-type), and have increased Km values compared with wild-type FVIIa. Inhibition of mutant G372A +soluble tissue factor by 4-aminobenzamidine is characterized by a seven-fold higher Ki than obtained with wild-type. Crystallographic and modelling data suggest that the most active conformation of FVIIa depends on the backbone hydrogen bond between Gly372 and Arg315 in the 170 loop. Native and active site-inhibited mutant G372A binds soluble tissue factor with the same affinity as the corresponding forms of FVIIa | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-aminobenzamidine | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000012 | - |
Factor X | mutant G372A + lipidated tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
0.000015 | - |
Factor X | wild-type FVIIa + lipidated tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
0.0019 | - |
Factor X | wild-type FVIIa + soluble tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
0.003 | - |
Factor X | wild-type FVIIa, pH 7.4 | Homo sapiens | |
0.0032 | - |
Factor X | mutant G372A + soluble tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
0.0054 | - |
Factor X | mutant G372A, pH 7.4 | Homo sapiens | |
1.8 | - |
D-Ile-Pro-Arg-4-nitroanilide | wild-type FVIIa + soluble tissue factor for induced allosteric activation of factor VIIa | Homo sapiens | |
7.1 | - |
D-Ile-Pro-Arg-4-nitroanilide | mutant G372A + soluble tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
10 | - |
D-Ile-Pro-Arg-4-nitroanilide | wild-type FVIIa, pH 7.4 | Homo sapiens | |
14 | - |
D-Ile-Pro-Arg-4-nitroanilide | mutant G372A, pH 7.4 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P08709 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
D-Ile-Pro-Arg-4-nitroanilide + H2O | - |
Homo sapiens | D-Ile-Pro-Arg + 4-nitroaniline | - |
? | |
Factor X + H2O | - |
Homo sapiens | Factor Xa + ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
factor VIIa | - |
Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000007 | - |
Factor X | mutant G372A, pH 7.4 | Homo sapiens | |
0.000049 | - |
Factor X | wild-type FVIIa, pH 7.4 | Homo sapiens | |
0.00062 | - |
Factor X | mutant G372A + soluble tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
0.0021 | - |
Factor X | mutant G372A + lipidated tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
0.0027 | - |
Factor X | wild-type FVIIa + soluble tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
0.004 | - |
Factor X | wild-type FVIIa + lipidated tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.1 | - |
4-aminobenzamidine | wild-type + soluble tissue factor for induced allosteric activation of factor VIIa | Homo sapiens | |
0.7 | - |
4-aminobenzamidine | mutant G372 + soluble tissue factor for induced allosteric activation of factor VIIa | Homo sapiens |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0012 | - |
Factor X | mutant G372A, pH 7.4 | Homo sapiens | |
0.016 | - |
Factor X | wild-type FVIIa, pH 7.4 | Homo sapiens | |
0.19 | - |
Factor X | mutant G372A + soluble tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
1.4 | - |
Factor X | wild-type FVIIa + soluble tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
180 | - |
Factor X | mutant G372A + lipidated tissue factor for induced allosteric activation of factor VIIa, pH 7.4 | Homo sapiens | |
270 | - |
Factor X | wild-type FVIIa + lipidated tissue factor for induced allosteric activation of factor VIIa | Homo sapiens |