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Literature summary for 3.4.21.5 extracted from
- Multiple inhibitory kinetics reveal an allosteric interplay among thrombin functional sites (2015), Thromb. Res., 135, 212-216.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
- |
Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| antithrombin III | pseudo-complete inhibition, noncompetitive | Homo sapiens | |
| argatroban | complete inhibition, noncompetitive | Homo sapiens |  |
| bivalirudin | complete inhibition, noncompetitive | Homo sapiens | |
| GPRP | pseudo-complete inhibition, noncompetitive | Homo sapiens | |
| heparin | partial inhibition, noncompetitive | Homo sapiens | |
| hirugen | complete inhibition, noncompetitive | Homo sapiens | |
| additional information | investigation on the effect of thrombin inhibitors on fibrinogen hydrolysis using a turbidimetric assay. There is a close relation between binding and inhibitory modes of the thrombin ligands. Active site- and exosite I-targeted ligands are able to inhibit fibrinogen hydrolysis completely. Macromolecular ligands affect fibrinogen hydrolysis in a competitive manner due to creation of the interacting area comparable to the thrombin-fibrinogen one. Low-molecular ligands probably form nonproductive complex interfering the appropriate orientation of substrate on the thrombin. Exosite II-targeted ligands are capable for only partial inhibition, indicating the fine tuning of the thrombin enzymatic activity via allosteric effects | Homo sapiens | |
| Phe-Pro-Arg-chloromethyl ketone | complete inhibition, noncompetitive | Homo sapiens | |
| Toggle-25 t | partial inhibition, noncompetitive | Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| fibrinogen + H2O | - |
Homo sapiens | fibrin + fibrinopeptide A + fibrinopeptide B | - |
? | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000014 | - |
antithrombin III | pH 7.4, 37°C | Homo sapiens | |
| 0.00000175 | - |
bivalirudin | pH 7.4, 37°C | Homo sapiens | |
| 0.0000064 | - |
argatroban | pH 7.4, 37°C | Homo sapiens | |
| 0.00001 | - |
Toggle-25 t | pH 7.4, 37°C | Homo sapiens | |
| 0.0000208 | - |
Phe-Pro-Arg-chloromethyl ketone | pH 7.4, 37°C | Homo sapiens | |
| 0.0015 | - |
hirugen | pH 7.4, 37°C | Homo sapiens | |
| 0.00265 | - |
heparin | pH 7.4, 37°C | Homo sapiens | |
| 0.027 | - |
GPRP | pH 7.4, 37°C | Homo sapiens | |
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Release 2023.1 (January 2023)
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