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Literature summary for 3.4.21.21 extracted from

  • Persson, E.; Olsen, O.H.
    Activation loop 3 and the 170 loop interact in the active conformation of coagulation factor VIIa (2009), FEBS J., 276, 3099-3109.
    View publication on PubMed

Protein Variants

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

Inhibitors Comment Organism Structure
4-aminobenzamidine
-
Homo sapiens

KM Value [mM]

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

Organism UniProt Comment Textmining
Homo sapiens P08709
-
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
factor VIIa
-
Homo sapiens

Turnover Number [1/s]

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

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Ki Value [mM]

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 [mM/s]

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