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Literature summary extracted from
- Factorising ligand affinity: a combined thermodynamic and crystallographic study of trypsin and thrombin inhibition (2001), J. Mol. Biol., 313, 593-614.
Crystallization (Commentary)
| EC Number | Crystallization (Comment) | Organism |
|---|---|---|
| 3.4.21.4 | vapour diffusion method, crystal structure of the enzyme in complex with 1b, 1cMe, 1d and 1dAc | Fusarium oxysporum |
| 3.4.21.5 | enzyme complexed with hirugen, 5.5 mg/ml in 24-30% PEG 4000, 0.1 M sodium phosphate, pH 7.3, 20°C, vapour diffusion method, single crystals are soaked overnight in 30% PEG 4000, 0.1 M sodium phosphate, pH 7.3, and 0.5 mg/ml inhibitor, X-ray diffraction structure determination and analysis | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.21.4 | CRC 220 | - |
Fusarium oxysporum |  |
| 3.4.21.4 | Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-4'-acetyl-piperazide | - |
Fusarium oxysporum | |
| 3.4.21.4 | Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-4'-methylpiperidide | - |
Fusarium oxysporum | |
| 3.4.21.4 | Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-D-pipecolic acid | - |
Fusarium oxysporum | |
| 3.4.21.4 | Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-D-pipecolic acid methyl ester | - |
Fusarium oxysporum | |
| 3.4.21.4 | Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-isopecotinic acid | - |
Fusarium oxysporum | |
| 3.4.21.4 | Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-isopecotinic acid methylester | - |
Fusarium oxysporum | |
| 3.4.21.4 | Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-piperazide | - |
Fusarium oxysporum | |
| 3.4.21.4 | napsagatran | - |
Fusarium oxysporum | |
| 3.4.21.4 | napsagatran ethylester | - |
Fusarium oxysporum | |
| 3.4.21.5 | CRC 220 | binding mode to the enzyme, crystal structure | Homo sapiens | |
| 3.4.21.5 | inogatran | binding mode to the enzyme, crystal structure | Homo sapiens | |
| 3.4.21.5 | melagatran | binding mode to the enzyme, crystal structure | Homo sapiens | |
| 3.4.21.5 | additional information | inhibition mechanism | Homo sapiens | |
| 3.4.21.5 | napsagatran | binding mode to the enzyme, crystal structure | Bos taurus | |
| 3.4.21.5 | napsagatran | binding mode to the enzyme, crystal structure | Homo sapiens | |
| 3.4.21.5 | napsagatran ethyl ester | binding mode to the enzyme, crystal structure | Bos taurus | |
| 3.4.21.5 | napsagatran ethyl ester | binding mode to the enzyme, crystal structure | 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 | thermodynamic analysis of enzyme structure | Homo sapiens | |
| 3.4.21.5 | additional information | - |
additional information | thermodynamic analysis of enzyme structure | Bos taurus |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.21.4 | Fusarium oxysporum | - |
- |
- |
| 3.4.21.5 | Bos taurus | P00735 | - |
- |
| 3.4.21.5 | Homo sapiens | - |
- |
- |
Purification (Commentary)
| EC Number | Purification (Comment) | Organism |
|---|---|---|
| 3.4.21.5 | - |
Bos taurus |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.4.21.5 | commercial preparation | - |
Homo sapiens | - |
Specific Activity [micromol/min/mg]
| EC Number | Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|---|
| 3.4.21.5 | 0.019 | - |
purified enzyme | Bos taurus |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.21.5 | additional information | determination of enzyme activity by active site titration with 4-nitrophenyl guanidino-benzoate | Bos taurus | ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.4.21.5 | alpha-thrombin | - |
Homo sapiens |
| 3.4.21.5 | alpha-thrombin | - |
Bos taurus |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.4.21.4 | 0.000021 | - |
Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-isopecotinic acid methylester | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.000042 | - |
Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-4'-methylpiperidide | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.000044 | - |
Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-4'-acetyl-piperazide | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.00012 | - |
Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-piperazide | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.00022 | - |
Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-isopecotinic acid | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.00041 | - |
CRC 220 | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.00066 | - |
Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-D-pipecolic acid | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.0011 | - |
Nalpha-(2-naphthylsulfonyl)-L-3-amidino-phenylalanine-D-pipecolic acid methyl ester | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.0116 | - |
napsagatran | - |
Fusarium oxysporum | |
| 3.4.21.4 | 0.03 | - |
napsagatran ethylester | - |
Fusarium oxysporum | |
| 3.4.21.5 | additional information | - |
additional information | inhibition kinetics for napsagatran and napsagatran ethyl ester in presence of NaCl or KCl and at 4 different temperatures | Bos taurus |
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