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Literature summary for 3.4.21.5 extracted from

  • Gibbs, C.S.; Coutre, S.E.; Tsiang, M.; Li, W.X.; Jain, A.K.; Dunn, K.E.; Law, V.S.; Mao, C.T.; Matsumura, S.Y.; Mejza, S.J.; Paborsky, L.R.; Leung, L.L.K.
    Conversion of thrombin into an anticoagulant by protein engineering (1995), Nature, 378, 413-416.
    View publication on PubMed

Application

Application Comment Organism
medicine the enzyme can be engineered to function in vivo as a potent anticoagulant that may possess a superior therapeutic profile with reduced potential for bleeding complications Homo sapiens

Protein Variants

Protein Variants Comment Organism
E229A mutation substantially shifts thrombin's specificity in favour of the anticoagulant substrate, protein C Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.002
-
protein C mutant enzyme E229A Homo sapiens
0.00295
-
D-Phe-L-pipecolyl-L-Arg-4-nitroanilide wild-type enzyme Homo sapiens
0.0032
-
protein C wild-type enzyme Homo sapiens
0.00355
-
fibrinogen Aalpha chain wild-type enzyme Homo sapiens
0.0113
-
fibrinogen Aalpha chain mutant enzyme E229A Homo sapiens
0.0355
-
platelet thrombin receptor peptide wild-type enzyme Homo sapiens
0.0502
-
D-Phe-L-pipecolyl-L-Arg-4-nitroanilide mutant enzyme E229A Homo sapiens
0.181
-
platelet thrombin receptor peptide mutant enzyme E229A Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Fibrinogen + H2O Homo sapiens key regulator of blood coagulation ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification zymogen: prothrombin Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-Phe-L-pipecolyl-L-Arg-4-nitroanilide + H2O
-
Homo sapiens D-Phe-L-pipecolyl-L-Arg + 4-nitroaniline
-
?
Fibrinogen + H2O Aalpha chain Homo sapiens ?
-
?
Fibrinogen + H2O key regulator of blood coagulation Homo sapiens ?
-
?
fibrinogen Aalpha chain + H2O
-
Homo sapiens ?
-
?
platelet thrombin receptor peptide + H2O
-
Homo sapiens ?
-
?
protein C + H2O mutation E229A substantially shifts thrombin's specificity in favour of the anticoagulant substrate, protein C Homo sapiens ?
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.19
-
protein C mutant enzyme E229A Homo sapiens
0.65
-
protein C wild-type enzyme Homo sapiens
4.53
-
fibrinogen Aalpha chain mutant enzyme E229A Homo sapiens
25
-
platelet thrombin receptor peptide mutant enzyme E229A Homo sapiens
34
-
platelet thrombin receptor peptide wild-type enzyme Homo sapiens
38
-
D-Phe-L-pipecolyl-L-Arg-4-nitroanilide mutant enzyme E229A Homo sapiens
51
-
D-Phe-L-pipecolyl-L-Arg-4-nitroanilide wild-type enzyme Homo sapiens
57
-
fibrinogen Aalpha chain wild-type enzyme Homo sapiens