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Literature summary for 3.4.21.6 extracted from

  • Toso, R.; Zhu, H.; Camire, R.M.
    The conformational switch from the factor X zymogen to protease state mediates exosite expression and prothrombinase assembly (2008), J. Biol. Chem., 283, 18627-18635.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
I16L mutation disrupts activation process of the factor X zymogen with alteration of active site function and impairment of Na+ and factor Va binding. Irreversible stabilization with L-Glu-Gly-L-Arg-chloromethyl ketone fully rescues factor Va binding. The Km value for prothrombin conversion for the mutant assembled into prothrombinase is unaltered, whereas the kcat is reduced 3- to 4fold Homo sapiens
V17A mutation disrupts activation process of the factor X zymogen with alteration of active site function and impairment of Na+ and factor Va binding. The Km value for prothrombin conversion for the mutant assembled into prothrombinase is unaltered, whereas the kcat is reduced 3- to 4fold Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
pefabloc
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00031
-
prothrombin prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
0.00035
-
prothrombin prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
0.00042
-
prothrombin prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
0.00047
-
prothrombin prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
0.0052
-
prethrombin-1 prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
0.0054
-
prethrombin-1 prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
0.0057
-
prethrombin-1 prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
0.0069
-
prethrombin-1 prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
0.072
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide native factor Xa, pH 7.5 Homo sapiens
0.089
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide recombinant factor Xa, pH 7.5 Homo sapiens
0.13
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
0.17
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
0.29
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
0.49
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
1.15
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide mutant I16L, pH 7.5 Homo sapiens
1.38
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide mutant V17A, pH 7.5 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide + H2O
-
Homo sapiens methoxycarbonylcyclohexyl-Gly-Gly-L-Arg + 4-nitroaniline
-
?
prethrombin-1 + H2O
-
Homo sapiens thrombin + ?
-
?
prothrombin + H2O
-
Homo sapiens thrombin + ?
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
6.5
-
prethrombin-1 prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
6.6
-
prethrombin-1 prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
10.3
-
prothrombin prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
14.8
-
prothrombin prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
17.5
-
prethrombin-1 prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
18.1
-
prethrombin-1 prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
32.3
-
prothrombin prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
33
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
40.4
-
prothrombin prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
58
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide mutant I16L, pH 7.5 Homo sapiens
72
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
73
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide mutant V17A, pH 7.5 Homo sapiens
91
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
140
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide native factor Xa, pH 7.5 Homo sapiens
140
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
210
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide recombinant factor Xa, pH 7.5 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00005
-
pefabloc prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
0.000053
-
pefabloc prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
0.000064
-
pefabloc native factor Xa, pH 7.5 Homo sapiens
0.00007
-
pefabloc recombinant factor Xa, pH 7.5 Homo sapiens
0.00021
-
pefabloc prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
0.00029
-
pefabloc prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
0.00169
-
pefabloc mutant V17A, pH 7.5 Homo sapiens
0.0017
-
pefabloc mutant I16L, pH 7.5 Homo sapiens