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Literature summary extracted from

  • Chu, V.; Brown, K.; Colussi, D.; Choi, Y.M.; Green, D.; Pauls, H.W.; Spada, A.P.; Perrone, M.H.; Leadley, R.J.; Dunwiddie, C.T.
    In vitro characterization of a novel factor Xa inhibitor, RPR 130737 (2000), Thromb. Res., 99, 71-82.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.21.6 Ca2+ required Homo sapiens
3.4.21.6 additional information formation of the prothrombinase enzyme complex increases the factor Xa activity by 300000fold, the complex includes phospholipids, Ca2+, factor Xa and factor Va Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.6 1,5-dansyl-Glu-Gly-Arg chloromethyl ketone slow binding inhibitor Homo sapiens
3.4.21.6 4-hydroxy-3-[2-oxo-3-(S)-(5-pyridin-3-yl-thiophene-2-sulfonylamino)-pyrrolidin-1-ylmethyl]-benzamidine i.e. RPR130737, highly specific inhibitor of factor Xa realtive to other serine proteases, reversible, fast binding, competitive active-site directed inhibitor Homo sapiens
3.4.21.6 DX-9065a fast-binding inhibitor Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.6 Homo sapiens
-
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
3.4.21.6 selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Homo sapiens
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.6 L-Arg-Gly-Arg-4-nitroanilide + H2O chromogenic synthetic substrate S2765 Homo sapiens L-Arg-Gly-Arg + 4-nitroaniline
-
 ?
3.4.21.6 prothrombin + H2O
-
 Homo sapiens thrombin + ?
-
 ?

Subunits

EC Number Subunits Comment Organism
3.4.21.6 More formation of the prothrombinase enzyme complex increases the factor Xa activity by 300000fold, the complex includes phospholipids, Ca2+, factor Xa and factor Va Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
3.4.21.6 More the enzyme belongs to the peptidase family S1, i.e. trypsin family Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.21.6 22
-
 room temperature, assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.21.6 7.5
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 0.0000024
-
 4-hydroxy-3-[2-oxo-3-(S)-(5-pyridin-3-yl-thiophene-2-sulfonylamino)-pyrrolidin-1-ylmethyl]-benzamidine pH 7.5, 22°C Homo sapiens