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Literature summary for 3.4.21.5 extracted from

  • Tsiang, M.; Paborsky, L.R.; Li, W.X.; Jain, A.K.; Mao, C.T.; Dunn, K.E.; Lee, D.W.; Matsumura, S.Y.; Matteucci, M.D.; Coutre, S.E.; Leung, L.L.K.; Gibbs, C.S.
    Protein engineering thrombin for optimal specificity and potency of anticoagulant activity in vivo (1996), Biochemistry, 35, 16449-16457.
    View publication on PubMed
Search for more literature for 3.4.21.5

Protein Variants

Protein Variants Comment Organism
E229K the mutation shifts the substrate specificity of thrombin by 130fold to favor the activation of the anticoagulant substrate protein C over the procoagulant substrate fibrinogen. The mutant enzyme is also less effective in activating platelets, is resistant to inhibition by antithrombin III and displays a prolonged half-life in plasma Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
antithrombin III mutant enzymes E229A and E229K are not inhibited 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
0.00215
-
 protein C mutant enzyme E229K Homo sapiens
0.00295
-
 D-Phe-L-pipecolyl-L-Arg-4-nitroanilide wild-type enzyme Homo sapiens
0.00312
-
 protein C mutant enzyme E229W Homo sapiens
0.00316
-
 fibrinogen wild-type enzyme Homo sapiens
0.00319
-
 protein C wild-type enzyme Homo sapiens
0.0236
-
 fibrinogen mutant enzyme E229A Homo sapiens
0.038
-
 fibrinogen mutant enzyme E229K Homo sapiens
0.0502
-
 D-Phe-L-pipecolyl-L-Arg-4-nitroanilide mutant enzyme E229A Homo sapiens
0.0528
-
 fibrinogen mutant enzyme E229W Homo sapiens
0.0632
-
 D-Phe-L-pipecolyl-L-Arg-4-nitroanilide mutant enzyme E229K Homo sapiens

Organism

Organism UniProt Comment Textmining
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
-
 Homo sapiens ?
-
 ?
protein C + H2O the mutation E229K shifts the substrate specificity of thrombin by 130fold to favor the activation of the anticoagulant substrate protein C over the procoagulant substrate fibrinogen Homo sapiens ?
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.065
-
 protein C wild-type enzyme Homo sapiens
0.148
-
 protein C mutant enzyme E229W Homo sapiens
0.19
-
 protein C mutant enzyme E229A Homo sapiens
0.21
-
 protein C mutant enzyme E229K Homo sapiens
2.53
-
 fibrinogen mutant enzyme E229K Homo sapiens
3.12
-
 fibrinogen mutant enzyme E229W Homo sapiens
5.9
-
 fibrinogen wild-type enzyme Homo sapiens
7.88
-
 fibrinogen mutant enzyme E229A Homo sapiens