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Literature summary extracted from

  • Verhoef, D.; Visscher, K.M.; Vosmeer, C.R.; Cheung, K.L.; Reitsma, P.H.; Geerke, D.P.; Bos, M.H.A.
    Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors (2017), Nat. Commun., 8, 528 .
    View publication on PubMedView publication on EuropePMC

Protein Variants

EC Number Protein Variants Comment Organism
3.4.21.6 F174A the mutant has about wild type activity Homo sapiens
3.4.21.6 Y99A the enzyme shows strongly reduced activity compared to the wild type enzyme Homo sapiens
3.4.21.6 Y99A/F174A the enzyme shows severely reduced activity compared to the wild type enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.6 antithrombin irreversible inhibition Homo sapiens
3.4.21.6 apixaban
-
 Homo sapiens
3.4.21.6 edoxaban
-
 Homo sapiens
3.4.21.6 recombinant tick saliva anticoagulant protein
-
 Homo sapiens
3.4.21.6 rivaroxaban
-
 Homo sapiens
3.4.21.6 TFPIalpha
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.6 0.026
-
 S-2765 wild type enzyme, at pH 7.5 and 25°C 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
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
3.4.21.6 glycoprotein
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.6 blood plasma
-
 Homo sapiens
-
3.4.21.6 HEK-293 cell
-
 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 + ?
-
 ?
3.4.21.6 S-2765 + H2O
-
 Homo sapiens Z-D-Arg-Gly-L-Arg + 4-nitroaniline
-
 ?

Subunits

EC Number Subunits Comment Organism
3.4.21.6 ? x * 59000, SDS-PAGE Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
3.4.21.6 blood coagulation factor Xa
-
 Homo sapiens
3.4.21.6 factor Xa
-
 Homo sapiens
3.4.21.6 FXa
-
 Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.21.6 21
-
 S-2765 wild type enzyme, at pH 7.5 and 25°C Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 0.0000007
-
 recombinant tick saliva anticoagulant protein wild type enzyme, at pH 7.5 and 25°C Homo sapiens
3.4.21.6 0.00000162
-
 TFPIalpha wild type enzyme, at pH 7.5 and 25°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.6 0.000002
-
 wild type enzyme, at pH 7.5 and 25°C Homo sapiens edoxaban
3.4.21.6 0.000005
-
 wild type enzyme, at pH 7.5 and 25°C Homo sapiens apixaban
3.4.21.6 0.000034
-
 mutant enzyme Y99A, at pH 7.5 and 25°C Homo sapiens apixaban
3.4.21.6 0.000045
-
 mutant enzyme F174A, at pH 7.5 and 25°C Homo sapiens apixaban
3.4.21.6 0.000616
-
 mutant enzyme Y99A/F174A, at pH 7.5 and 25°C Homo sapiens apixaban