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Literature summary 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

EC Number Protein Variants Comment Organism
3.4.21.6 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
3.4.21.6 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

EC Number Inhibitors Comment Organism Structure
3.4.21.6 pefabloc
-
Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.6 0.00031
-
prothrombin prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 0.00035
-
prothrombin prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.00042
-
prothrombin prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.00047
-
prothrombin prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 0.0052
-
prethrombin-1 prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.0054
-
prethrombin-1 prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.0057
-
prethrombin-1 prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 0.0069
-
prethrombin-1 prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 0.072
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.089
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.13
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.17
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.29
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 0.49
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 1.15
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 1.38
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide mutant V17A, pH 7.5 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.6 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.6 blood plasma
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.21.6 6.5
-
prethrombin-1 prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 6.6
-
prethrombin-1 prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 10.3
-
prothrombin prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 14.8
-
prothrombin prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 17.5
-
prethrombin-1 prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 18.1
-
prethrombin-1 prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 32.3
-
prothrombin prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 33
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 40.4
-
prothrombin prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 58
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 72
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 73
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 91
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 140
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 140
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 210
-
methoxycarbonylcyclohexyl-Gly-Gly-L-Arg-4-nitroanilide recombinant factor Xa, pH 7.5 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 0.00005
-
pefabloc prothrombinase assembled with recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.000053
-
pefabloc prothrombinase assembled with native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.000064
-
pefabloc native factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.00007
-
pefabloc recombinant factor Xa, pH 7.5 Homo sapiens
3.4.21.6 0.00021
-
pefabloc prothrombinase assembled with mutant I16L, pH 7.5 Homo sapiens
3.4.21.6 0.00029
-
pefabloc prothrombinase assembled with mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 0.00169
-
pefabloc mutant V17A, pH 7.5 Homo sapiens
3.4.21.6 0.0017
-
pefabloc mutant I16L, pH 7.5 Homo sapiens