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Literature summary extracted from

  • De Cristofaro, R.; Akhavan, S.; Altomare, C.; Carotti, A.; Peyvandi, F.; Mannucci, P.M.
    A natural prothrombin mutant reveals an unexpected influence of A-chain structure on the activity of human alpha-thrombin (2004), J. Biol. Chem., 279, 13035-13043.
    View publication on PubMed

Cloned(Commentary)

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

Protein Variants

EC Number Protein Variants Comment Organism
3.4.21.5 additional information a natural deletion mutant DELTAK9 of prothrombin from 2 homozygous humans lacks Lys9 and Lys10 residues of the A-chain shows 18fold reduced activity with substrate D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide and 60fold reduced activity with fibrinopeptide A compared to the wild-type enzyme, mutant shows reduced sensitivity to antithrombin, and Na+, and a defective PARI receptor recognition, thus reduced platelet activation, alteration of A-and B-chain conformation, especially insertion loop 60, and the catalytic triad residues Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.5 antithrombin wild-type and mutant DELTAK9, the mutant shows 20fold lower susceptibility than the wild-type Homo sapiens
3.4.21.5 Bovine pancreatic trypsin inhibitor
-
 Homo sapiens
3.4.21.5 heparin from porcine intestinal mucosa, about 16.5 kDa Homo sapiens
3.4.21.5 N-alpha-(2-naphthylsulfonyl-glycyl)-4-amidinophenylalanine-piperidine i.e. alpha-NAPAP Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.5 additional information
-
 additional information kinetics Homo sapiens
3.4.21.5 0.0051
-
 Fibrinopeptide A pH 8.0, 25°C, wild-type enzyme Homo sapiens
3.4.21.5 0.0084
-
 PAR1 peptide pH 8.0, 25°C, wild-type enzyme Homo sapiens
3.4.21.5 0.013
-
 Fibrinopeptide A pH 8.0, 25°C, mutant DELTAK9 Homo sapiens
3.4.21.5 0.028
-
 PAR1 peptide pH 8.0, 25°C, mutant DELTAK9 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.5 Homo sapiens P00734
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
3.4.21.5 proteolytic modification activation of recombinant wild-type and mutant DELTAK9 prothrombins by Taipan snake venom treatment Homo sapiens

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.21.5 recombinant wild-type and mutant enzyme from CHO cells Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.5 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide + H2O i.e. S2238, synthetic chromogenic substrate Homo sapiens D-phenylalanyl-pipecolyl-L-arginine + 4-nitroaniline
-
 ?
3.4.21.5 fibrinogen + H2O proteolytic activation Homo sapiens fibrin + fibrinopeptide A + fibrinopeptide B
-
 ?
3.4.21.5 fibrinopeptide A + H2O
-
 Homo sapiens ?
-
 ?
3.4.21.5 additional information interaction with receptors glycoprotein Ibalpha GpIb and protease-activated receptor 1, i.e. PAR1, in platelet membrane Homo sapiens ?
-
 ?
3.4.21.5 PAR1 peptide + H2O protease-activated receptor I peptide fragment, amino acid sequence Homo sapiens ?
-
 ?
3.4.21.5 protein C + H2O
-
 Homo sapiens ?
-
 ?

Subunits

EC Number Subunits Comment Organism
3.4.21.5 More structure molecular modeling of mutant DELTAK9 enzyme Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
3.4.21.5 alpha-thrombin
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.21.5 25
-
 assay at Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.21.5 1.82
-
 Fibrinopeptide A pH 8.0, 25°C, mutant DELTAK9 Homo sapiens
3.4.21.5 2.94
-
 Fibrinopeptide A pH 8.0, 25°C, mutant DELTAK9 Homo sapiens
3.4.21.5 4.2
-
 PAR1 peptide pH 8.0, 25°C, mutant DELTAK9 Homo sapiens
3.4.21.5 45.3
-
 Fibrinopeptide A pH 8.0, 25°C, wild-type enzyme Homo sapiens
3.4.21.5 146
-
 PAR1 peptide pH 8.0, 25°C, wild-type enzyme Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.21.5 8
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
3.4.21.5 Thrombomodulin
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.5 0.00000066
-
 N-alpha-(2-naphthylsulfonyl-glycyl)-4-amidinophenylalanine-piperidine pH 8.0, 25°C, mutant DELTAK9 Homo sapiens
3.4.21.5 0.0000021
-
 N-alpha-(2-naphthylsulfonyl-glycyl)-4-amidinophenylalanine-piperidine pH 8.0, 25°C, wild-type enzyme Homo sapiens