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Literature summary for 3.4.21.6 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

Activating Compound Comment Organism Structure
Ca2+ required Homo sapiens
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

Inhibitors Comment Organism Structure
1,5-dansyl-Glu-Gly-Arg chloromethyl ketone slow binding inhibitor Homo sapiens
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
DX-9065a fast-binding inhibitor Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

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

Substrates and Products (Substrate)

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

Subunits

Subunits Comment Organism
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

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

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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