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Literature summary for 3.4.21.5 extracted from

  • De Cristofaro, R.; De Filippis, V.
    Interaction of the 268-282 region of glycoprotein Ibalpha with the heparin-binding site of thrombin inhibits the enzyme activation of factor VIII (2003), Biochem. J., 373, 593-601.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
glycoprotein Ibalpha(1-282) peptide binds to exosite II of the enzyme, inhibits activation of factor VIII to more than 70% Homo sapiens
glycoprotein Ibalpha(268-282) peptide binds to exosite II of the enzyme, inhibits activation of factor VIII and cleavage of factor VIII(341-376) peptide to more than 70% Homo sapiens
HD22 aptamer, mitogen Homo sapiens
sulfated glycoprotein Ibalpha(268-282) peptide sulfated at all tyrosine residues, binds to exosite II of the enzyme, inhibits activation of factor VIII and cleavage of factor VIII(341-376) peptide to more than 70% Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics Homo sapiens
0.112
-
factor VIII(341-376) peptide pH 7.5, 25°C Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
factor VIII + H2O Homo sapiens activation by cleavage of Arg372, Arg74, and Arg1689, plays a fundamental role in the amplification of the coagulation cascade ?
-
?
factor X + H2O Homo sapiens proteolytic activation factor Xa + propeptide
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
factor VIII + H2O activation by cleavage of Arg372, Arg74, and Arg1689 involving exosite II, the heparin binding site Homo sapiens ?
-
?
factor VIII + H2O activation by cleavage of Arg372, Arg74, and Arg1689, plays a fundamental role in the amplification of the coagulation cascade Homo sapiens ?
-
?
factor VIII(341-376) peptide + H2O cleavage of Arg372 involving exosite II, the heparin binding site Homo sapiens ?
-
?
factor X + H2O proteolytic activation Homo sapiens factor Xa + propeptide
-
?

Synonyms

Synonyms Comment Organism
alpha-thrombin
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3 6 factor VIII(341-376) peptide pH 7.5, 25°C Homo sapiens
3.24
-
factor VIII(341-376) peptide pH 7.5, 25°C 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
additional information
-
additional information inhibition kinetics Homo sapiens
0.000025
-
HD22 pH 8.0, 25°C Homo sapiens
0.0088
-
glycoprotein Ibalpha(1-282) peptide pH 8.0, 25°C Homo sapiens
0.054
-
glycoprotein Ibalpha(268-282) peptide pH 8.0, 25°C Homo sapiens