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Literature summary for 3.4.21.5 extracted from
- 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.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of wild-type and mutant enzymes in CHO cells | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| 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
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| antithrombin | wild-type and mutant DELTAK9, the mutant shows 20fold lower susceptibility than the wild-type | Homo sapiens | |
| Bovine pancreatic trypsin inhibitor | - |
Homo sapiens | |
| heparin | from porcine intestinal mucosa, about 16.5 kDa | Homo sapiens |  |
| N-alpha-(2-naphthylsulfonyl-glycyl)-4-amidinophenylalanine-piperidine | i.e. alpha-NAPAP | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetics | Homo sapiens | |
| 0.0051 | - |
Fibrinopeptide A | pH 8.0, 25°C, wild-type enzyme | Homo sapiens | |
| 0.0084 | - |
PAR1 peptide | pH 8.0, 25°C, wild-type enzyme | Homo sapiens | |
| 0.013 | - |
Fibrinopeptide A | pH 8.0, 25°C, mutant DELTAK9 | Homo sapiens | |
| 0.028 | - |
PAR1 peptide | pH 8.0, 25°C, mutant DELTAK9 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P00734 | - |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| proteolytic modification | activation of recombinant wild-type and mutant DELTAK9 prothrombins by Taipan snake venom treatment | Homo sapiens |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant wild-type and mutant enzyme from CHO cells | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide + H2O | i.e. S2238, synthetic chromogenic substrate | Homo sapiens | D-phenylalanyl-pipecolyl-L-arginine + 4-nitroaniline | - |
? | |
| fibrinogen + H2O | proteolytic activation | Homo sapiens | fibrin + fibrinopeptide A + fibrinopeptide B | - |
? | |
| fibrinopeptide A + H2O | - |
Homo sapiens | ? | - |
? | |
| additional information | interaction with receptors glycoprotein Ibalpha GpIb and protease-activated receptor 1, i.e. PAR1, in platelet membrane | Homo sapiens | ? | - |
? | |
| PAR1 peptide + H2O | protease-activated receptor I peptide fragment, amino acid sequence | Homo sapiens | ? | - |
? | |
| protein C + H2O | - |
Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | structure molecular modeling of mutant DELTAK9 enzyme | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| alpha-thrombin | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 25 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 1.82 | - |
Fibrinopeptide A | pH 8.0, 25°C, mutant DELTAK9 | Homo sapiens | |
| 2.94 | - |
Fibrinopeptide A | pH 8.0, 25°C, mutant DELTAK9 | Homo sapiens | |
| 4.2 | - |
PAR1 peptide | pH 8.0, 25°C, mutant DELTAK9 | Homo sapiens | |
| 45.3 | - |
Fibrinopeptide A | pH 8.0, 25°C, wild-type enzyme | Homo sapiens | |
| 146 | - |
PAR1 peptide | pH 8.0, 25°C, wild-type enzyme | Homo sapiens | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| Thrombomodulin | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00000066 | - |
N-alpha-(2-naphthylsulfonyl-glycyl)-4-amidinophenylalanine-piperidine | pH 8.0, 25°C, mutant DELTAK9 | Homo sapiens | |
| 0.0000021 | - |
N-alpha-(2-naphthylsulfonyl-glycyl)-4-amidinophenylalanine-piperidine | pH 8.0, 25°C, wild-type enzyme | Homo sapiens | |
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