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Literature summary for 3.4.21.6 extracted from

  • Henry, B.L.; Desai, U.R.
    Sulfated low molecular weight lignins, allosteric inhibitors of coagulation proteinases via the heparin binding site, significantly alter the active site of thrombin and factor Xa compared to heparin (2014), Thromb. Res., 134, 1123-1129.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
additional information sulfated low-molecular weight lignins CDSO3, FDSO3, SDSO3, and unfractionated heparin inhibit thrombin and factor Xa through allosteric disruption of the catalytic apparatus, specifically through the catalytic step Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0013
-
D-phenylalanyl-L-pipecolyl-L-arginine-4-nitroanilide 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C Homo sapiens
0.0013
-
D-cyclohexyl-Gly-L-Pro-L-Arg-4-nitroanilide 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C Homo sapiens
0.0022
-
D-hexahydrotyrosol-L-Ala-L-Arg-4-nitroanilide 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C Homo sapiens
0.0045
-
N6-CBZ-D-Lys-L-Pro-L-Arg-4-nitroanilide 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C Homo sapiens
0.061
-
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg-4-nitroanilide 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1% (w/v) PEG 8000 at 25°C Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
prothrombin + H2O Homo sapiens
-
trhombin + ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-cyclohexyl-Gly-L-Pro-L-Arg-4-nitroanilide + H2O
-
Homo sapiens D-cyclohexyl-Gly-L-Pro-L-Arg + 4-nitroaniline
-
?
D-hexahydrotyrosol-L-Ala-L-Arg-4-nitroanilide + H2O
-
Homo sapiens D-hexahydrotyrosol-L-Ala-L-Arg + 4-nitroaniline
-
?
D-phenylalanyl-L-pipecolyl-L-arginine-4-nitroanilide + H2O
-
Homo sapiens D-phenylalanyl-L-pipecolyl-L-arginine + 4-nitroaniline
-
?
methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg-4-nitroanilide + H2O
-
Homo sapiens methoxycarbonyl-D-cyclohexylglycyl-Gly-L-Arg + 4-nitroaniline
-
?
N6-CBZ-D-Lys-L-Pro-L-Arg-4-nitroanilide + H2O
-
Homo sapiens N6-CBZ-D-Lys-L-Pro-L-Arg + 4-nitroaniline
-
?
prothrombin + H2O
-
Homo sapiens trhombin + ?
-
?

Synonyms

Synonyms Comment Organism
factor Xa
-
Homo sapiens
FXa
-
Homo sapiens