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Literature summary extracted from

  • Nar, H.; Bauer, M.; Schmid, A.; Stassen, J.M.; Wienen, W.; Priepke, H.W.M.; Kauffmann, I.K.; Ries, U.J.; Hauel, N.H.
    Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors (2001), Structure, 9, 29-37.
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.21.6 chymotrypsin treated factor Xa, i.e. des-Gla(1-44), lacking the Gla domain, free or complexed with inhibitor BIBT0871, 3 mg/ml protein in 10 mM Tris-HCl, pH 7.5, 20 mM sodium chloride, 2 mM calcium chloride, equilibrated against 20% PEG 4000, 0.1 M malate/imidazole, 0.1 M sodium acetate, pH 6.0, some days, X-ray diffraction structure determination and analysis at 1.9-3.0 A, cocrystallization of factor Xa complexed with thrombin and inhibitor BIBR1109 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.6 BIBM1015 4-(1-methyl-benzimidazole-based inhibitor) Homo sapiens
3.4.21.6 BIBR1109 4-(1-methyl-benzimidazole-based inhibitor) Homo sapiens
3.4.21.6 BIBT0871 possesses a 1-methyl-benzimidazole scaffold placing the methyl substitutent into the S2-subsite, pyridinyl moiety interacts with F174, binding structure Homo sapiens
3.4.21.6 heparin inhibition via complex formation with and modulation of the activity of thrombin Homo sapiens
3.4.21.6 additional information binding mode of dual specific inhibitors, with a N-methyl-benzimidazole scaffold, of thrombin and factor Xa, overview 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 P00742 chymotrypsin treated factor Xa, i.e. des-Gla(1-44), lacking the Gla domain
-

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.6 commercial preparation
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

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

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 0.000015
-
 BIBM1015 pH 8.0, 37°C Homo sapiens
3.4.21.6 0.00004
-
 BIBR1109 pH 8.0, 37°C Homo sapiens
3.4.21.6 0.000057
-
 BIBT0871 pH 8.0, 37°C Homo sapiens