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Literature summary for 3.4.21.6 extracted from

  • Chu, V.; Brown, K.; Colussi, D.; Gao, J.; Bostwick, J.; Kasiewski, C.; Bentley, R.; Morgan, S.; Guertin, K.; Pauls, H.W.; Gong, Y.; Zulli, A.; Perrone, M.H.; Dunwiddie, C.T.; Leadley, R.J.
    Pharmacological characterization of a novel factor Xa inhibitor, FXV673 (2001), Thromb. Res., 103, 309-324.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester i.e. FXV673, highly specific fo factor Xa compared to other serine protesases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, inhibition of thrombus formation in vivo in the acute arterial and venous electrolytic injury canine model, no effect on platelet aggregation Canis lupus familiaris
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester i.e. FXV673, highly specific fo factor Xa compared to other serine proteases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation Homo sapiens
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester i.e. FXV673, highly specific fo factor Xa compared to other serine protesases, increases the coagulation time, inhibition kinetics of the enzyme complex bound factor Xa, no effect on platelet aggregation Oryctolagus cuniculus
EDTA
-
Canis lupus familiaris
EDTA
-
Homo sapiens
EDTA
-
Oryctolagus cuniculus

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Homo sapiens
-
-
extracellular
-
Oryctolagus cuniculus
-
-
extracellular
-
Canis lupus familiaris
-
-

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
mongrel dogs of either sex
-
Homo sapiens
-
-
-
Oryctolagus cuniculus
-
-
-

Reaction

Reaction Comment Organism Reaction ID
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Homo sapiens
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Oryctolagus cuniculus
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Canis lupus familiaris

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-
commercial preparation
-
Oryctolagus cuniculus
-
commercial preparation
-
Canis lupus familiaris
-
plasma
-
Homo sapiens
-
plasma
-
Oryctolagus cuniculus
-
plasma
-
Canis lupus familiaris
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
prothrombin + H2O
-
Homo sapiens thrombin + ?
-
?
prothrombin + H2O
-
Oryctolagus cuniculus thrombin + ?
-
?
prothrombin + H2O
-
Canis lupus familiaris thrombin + ?
-
?

Subunits

Subunits Comment Organism
More enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+ Homo sapiens
More enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+ Oryctolagus cuniculus
More enzyme is part of the prothrombinase enzyme complex including also factor Va, phospholipids and Ca2+ Canis lupus familiaris

Synonyms

Synonyms Comment Organism
factor Xa
-
Homo sapiens
factor Xa
-
Oryctolagus cuniculus
factor Xa
-
Canis lupus familiaris
FXa
-
Homo sapiens
FXa
-
Oryctolagus cuniculus
FXa
-
Canis lupus familiaris
More the enzyme belongs to the peptidase family S1, i.e. trypsin family Homo sapiens
More the enzyme belongs to the peptidase family S1, i.e. trypsin family Oryctolagus cuniculus
More the enzyme belongs to the peptidase family S1, i.e. trypsin family Canis lupus familiaris

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Canis lupus familiaris

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens
7.5
-
assay at Oryctolagus cuniculus
7.5
-
assay at Canis lupus familiaris

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000027
-
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester pH 7.5, 37°C Oryctolagus cuniculus
0.00000052
-
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester pH 7.5, 37°C Homo sapiens
0.00000141
-
2-(R)-(3-carbamimidoylbenzyl)-3-(R)-[4-(1-oxypyridin-4-yl)benzoylamino]-butyric acid methyl ester pH 7.5, 37°C Canis lupus familiaris