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Literature summary for 3.4.21.5 extracted from

  • Qureshi, S.H.; Yang, L.; Manithody, C.; Iakhiaev, A.V.; Rezaie, A.R.
    Mutagenesis studies toward understanding allostery in thrombin (2009), Biochemistry, 48, 8261-8270.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.5

Activating Compound

Activating Compound Comment Organism Structure
additional information thrombomodulin has no effect on the conformation of the catalytic residue of thrombin Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
wild type and mutant enzymes are expressed as prethrombin-2 zymogens in baby hamster kidney cells using the pNUT-PL2 expression/purification vector system Homo sapiens

Protein Variants

Protein Variants Comment Organism
E217C/K224C mutant in which the 225-loop of the Na+-binding site is stabilized by an engineered disulfide bond, the activity of the mutant is dramatically impaired, though thrombomodulin interacts with this mutant with more than 20fold elevated KD to partially restore its activity, the mutant exhibits about 2-3fold higher KD for interaction with Na+ and does not clot fibrinogen or activated protein C in the presence of thrombomodulin Homo sapiens
R67C/I82C mutant in which the 70-80 loop of exosite-1 is stabilized by an engineered disulfide bond, mutant does not bind thrombomodulin and exhibits a normal amidolytic activity. The mutant exhibits about 2-3fold higher KD for interaction with Na+ and does not clot fibrinogen or activated protein C in the presence of thrombomodulin Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0039
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide wild type enzyme, in Tris-HCl (pH 7.5) with 1.0 M NaCl and dithiothreitol, at 22°C Homo sapiens
0.0059
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme R67C/I82C, in Tris-HCl (pH 7.5) with 0.2 M NaCl, at 22°C Homo sapiens
0.0059
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide wild type enzyme, in Tris-HCl (pH 7.5) with 0.2 M NaCl, at 22°C Homo sapiens
0.0064
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide wild type enzyme, in Tris-HCl (pH 7.5) with 0.2 M NaCl and dithiothreitol, at 22°C Homo sapiens
0.0088
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide wild type enzyme, in Tris-HCl (pH 7.5) with 0.2 M choline chloride, at 22°C Homo sapiens
0.0106
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme R67C/I82C, in Tris-HCl (pH 7.5) with 0.2 M choline chloride, at 22°C Homo sapiens
0.0287
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme E217C/K224C, in Tris-HCl (pH 7.5) with 1.0 M NaCl and dithiothreitol, at 22°C Homo sapiens
0.062
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme E217C/K224C, in Tris-HCl (pH 7.5) with 0.2 M NaCl, at 22°C Homo sapiens
0.0956
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme E217C/K224C, in Tris-HCl (pH 7.5) with 0.2 M NaCl and dithiothreitol, at 22°C Homo sapiens
0.298
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme E217C/K224C, in Tris-HCl (pH 7.5) with 0.2 M choline chloride, at 22°C Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Na+ the catalytic residue of thrombin is modulated by Na+ Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
activated protein C + H2O Homo sapiens
-
 ?
-
 ?
fibrinogen + H2O Homo sapiens
-
 fibrin + fibrinopeptide A + fibrinopeptide B
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
activated protein C + H2O
-
 Homo sapiens ?
-
 ?
D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide + H2O D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide is S2238 Homo sapiens D-phenylalanyl-pipecolyl-L-arginine + 4-nitroaniline
-
 ?
fibrinogen + H2O
-
 Homo sapiens fibrin + fibrinopeptide A + fibrinopeptide B
-
 ?

Synonyms

Synonyms Comment Organism
alpha-thrombin
-
 Homo sapiens
fibrinogenase
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.11
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme E217C/K224C, in Tris-HCl (pH 7.5) with 0.2 M choline chloride, at 22°C Homo sapiens
0.32
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme E217C/K224C, in Tris-HCl (pH 7.5) with 0.2 M NaCl, at 22°C Homo sapiens
15.8
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide wild type enzyme, in Tris-HCl (pH 7.5) with 0.2 M choline chloride, at 22°C Homo sapiens
21.2
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme R67C/I82C, in Tris-HCl (pH 7.5) with 0.2 M choline chloride, at 22°C Homo sapiens
41.2
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme E217C/K224C, in Tris-HCl (pH 7.5) with 0.2 M NaCl and dithiothreitol, at 22°C Homo sapiens
46.6
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide wild type enzyme, in Tris-HCl (pH 7.5) with 0.2 M NaCl and dithiothreitol, at 22°C Homo sapiens
47.9
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme E217C/K224C, in Tris-HCl (pH 7.5) with 1.0 M NaCl and dithiothreitol, at 22°C Homo sapiens
55.5
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide wild type enzyme, in Tris-HCl (pH 7.5) with 1.0 M NaCl and dithiothreitol, at 22°C Homo sapiens
75
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide wild type enzyme, in Tris-HCl (pH 7.5) with 0.2 M NaCl, at 22°C Homo sapiens
84.4
-
 D-phenylalanyl-pipecolyl-L-arginine-4-nitroanilide mutant enzyme R67C/I82C, in Tris-HCl (pH 7.5) with 0.2 M NaCl, at 22°C Homo sapiens