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Literature summary for 3.4.21.21 extracted from

  • Soejima, K.; Mizuguchi, J.; Yuguchi, M.; Nakagaki, T.; Higashi, S.; Iwanaga, S.
    Factor VIIa modified in the 170 loop shows enhanced catalytic activity but does not change the zymogen-like property (2001), J. Biol. Chem., 276, 17229-17235.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
tissue factor activates Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant enzymes in CHO-K1 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
DELTA360-329 lower affinity for soluble tissue factor as compared to wild-type factor VIIa, 7fold smaller tissue factor-mediated acceleration of amidolytic activity compared to wild type factor VIIa Homo sapiens
additional information mutant enzyme which has all of the residues of the loop formed by a disulfide bond between Cys310 and Cys329 replaced with those of trypsin has lower affinity for soluble tissue factor as compared to wild-type enzyme, 2fold smaller tissue factor-mediated acceleration of amidolytic activity compared to wild type enzyme, the catalytic efficiencies of the mutant towards various chromogenic substrates are 2-18fold greater than those of the wild-type factor VIIa. As well as the wild-type enzyme the mutant exists predominantly in the zymogen-like state Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.25
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, plasma derived wild-type enzyme, activated by tissue factor Homo sapiens
1.43
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, activated wild-type enzyme, activated by tissue factor Homo sapiens
1.53
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, mutant enzyme DELTA360-329, without tissue factor Homo sapiens
1.73
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, mutant enzyme which has all of the residues of the loop formed by a disulfide bond between Cys310 and Cys329 replaced with those of trypsin, activated by tissue factor Homo sapiens
2.22
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, activated wild-type enzyme, without tissue factor Homo sapiens
2.82
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, plasma derived wild-type enzyme, without tissue factor Homo sapiens
2.98
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, mutant enzyme DELTA360-329, activated by tissue factor Homo sapiens
3.06
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, mutant enzyme which has all of the residues of the loop formed by a disulfide bond between Cys310 and Cys329 replaced with those of trypsin, without tissue factor Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
wild-type and mutant enzymes expressed in CHO-K1 cells 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.
benzoyl-Ile-Glu-gamma-methoxyglutamyl-Gly-Arg-p-nitroanilide + H2O i.e. S2222, 2% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens benzoyl-Ile-Glu-gamma-methoxyglutamyl-Gly-Arg + p-nitroaniline
-
?
benzyloxycarbonyl-D-Arg-Gly-Arg + H2O i.e. S2765, 6% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens ?
-
?
D-Ile-Pro-Arg-p-nitroanilide + H2O i.e. S2288, 68% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens D-Ile-Pro-Arg + p-nitroaniline
-
?
D-Phe-pipecolyl-Arg-p-nitroanilide + H2O i.e. S2238, 34% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens D-Phe-pipecolyl-Arg + p-nitroaniline
-
?
D-Pro-Phe-Arg-p-nitroanilide + H2O i.e. S2302, 12% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens D-Pro-Phe-Arg + p-nitroaniline
-
?
N-methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide + H2O i.e. chromozym X, 11% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens N-methoxycarbonyl-D-Nle-Gly-Arg + p-nitroaniline
-
?
N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide + H2O i.e. chromozym t-PA Homo sapiens N-methylsulfonyl-D-Phe-Gly-Arg + p-nitroaniline
-
?
pyroglutamyl-Gly-Arg-p-nitroanilide + H2O i.e. S2444, 2% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens pyroglutamyl-Gly-Arg + p-nitroaniline
-
?
pyroglutamyl-Phe-Lys-p-nitroanilide + H2O i.e. S2403, 1.4% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens pyroglutamyl-D-Phe-Gly-Arg + p-nitroaniline
-
?
pyroglutamyl-Pro-Arg-p-nitroanilide + H2O i.e. S2366, 38% of the activity with N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide, plasma-derived wild-type enzyme Homo sapiens pyroglutamyl-Pro-Arg + p-nitroaniline
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.59
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, mutant enzyme DELTA360-329, without tissue factor Homo sapiens
1.95
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, activated wild-type enzyme, without tissue factor Homo sapiens
3.29
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, plasma derived wild-type enzyme, without tissue factor Homo sapiens
7.81
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, mutant enzyme DELTA360-329, activated by tissue factor Homo sapiens
18.53
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, mutant enzyme which has all of the residues of the loop formed by a disulfide bond between Cys310 and Cys329 replaced with those of trypsin, without tissue factor Homo sapiens
20.98
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, mutant enzyme which has all of the residues of the loop formed by a disulfide bond between Cys310 and Cys329 replaced with those of trypsin, activated by tissue factor Homo sapiens
37.08
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, activated wild-type enzyme, activated by tissue factor Homo sapiens
44.2
-
D-Ile-Pro-Arg-p-nitroanilide pH 8.0, 30°C, plasma derived wild-type enzyme, activated by tissue factor Homo sapiens