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Literature summary for 3.4.21.6 extracted from

  • Heran, C.; Morgan, S.; Kasiewski, C.; Bostwick, J.; Bentley, R.; Klein, S.; Chu, V.; Brown, K.; Colussi, D.; Czekaj, M.; Perrone, M.; Leadley, R.
    Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis (2000), Eur. J. Pharmacol., 389, 201-207.
    View publication on PubMed
Search for more literature for 3.4.21.6

Application

Application Comment Organism
pharmacology the enzyme is a target for development of antithrombotic drug therapy mechanism Homo sapiens
pharmacology the enzyme is a target for development of antithrombotic drug therapy mechanism Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate i.e. RPR208566, highly specific Homo sapiens
methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate i.e. RPR208566, inhibits thrombus formation in the rat artery model, highly specific Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
 Homo sapiens
-
-
extracellular
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
prothrombin + H2O Homo sapiens initial step in thrombus formation thrombin + ?
-
 ?
prothrombin + H2O Rattus norvegicus initial step in thrombus formation thrombin + ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
 male Spreague-Dawley
-

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
a
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Rattus norvegicus
a

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
 Rattus norvegicus
-
carotid artery
-
 Rattus norvegicus
-
commercial preparation
-
 Homo sapiens
-
plasma
-
 Homo sapiens
-
plasma
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
prothrombin + H2O
-
 Homo sapiens thrombin + ?
-
 ?
prothrombin + H2O
-
 Rattus norvegicus thrombin + ?
-
 ?
prothrombin + H2O initial step in thrombus formation Homo sapiens thrombin + ?
-
 ?
prothrombin + H2O initial step in thrombus formation Rattus norvegicus thrombin + ?
-
 ?

Synonyms

Synonyms Comment Organism
coagulation factor Xa
-
 Homo sapiens
coagulation factor Xa
-
 Rattus norvegicus
factor Xa
-
 Homo sapiens
factor Xa
-
 Rattus norvegicus
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 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens
37
-
 assay at Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000013
-
 methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[(3',4'-dimethoxybiphenyl-4-yl)carbonyl]amino}butanoate trifluoroacetate 37°C Homo sapiens