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Literature summary for 3.4.21.69 extracted from

  • Nicolaes, G.A.; Bock, P.E.; Segers, K.; Wildhagen, K.C.; Dahlbaeck, B.; Rosing, J.
    Inhibition of thrombin formation by active site mutated (S360A) activated protein C (2010), J. Biol. Chem., 285, 22890-22900.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.69

Activating Compound

Activating Compound Comment Organism Structure
Phospholipid
-
 Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of the mutant zymogen protein C(S360A) in HEK-293 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
S360A the active site mutant lacks proteolytic activity but exhibits anticoagulant activity. APC(S360A), and not its zymogen protein C(S360A), expresses anticoagulant activities by competing with activated coagulation factors X and IX for binding to FVa and FVIIIa, respectively. APC(S360A) binding to FVa is critically dependent upon the presence of Arg506 and not Arg306. Inhibition of FVIIIa activity by APC(S360A) is 100fold less efficient than inhibition of FVa. Binding of APC(S360A) to FVa is almost completely dependent on Arg506 interacting with APC(S360A) to form a nonproductive Michaelis complex. No binding to the substrate FVa Gln506 mutant Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information binding of APC(S360A) to FVa is not affected by protein S Homo sapiens
prothrombin inhibits the binding of APC(S360A) to FVa Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Factor Va + H2O Homo sapiens activated protein C downregulates thrombin formation through proteolytic inactivation of factor Va by cleavage at Arg506 and Arg306. Docking of APC to FVa and FVIIIa constitutes the first step in the inactivation of the cofactor ?
-
 ?
Factor VIIIa + H2O Homo sapiens activated protein C downregulates thrombin formation through proteolytic inactivation of factor VIIIa by cleavage at Arg336 and Arg56. Docking of APC to FVa and FVIIIa constitutes the first step in the inactivation of the cofactor ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-Phe-Pip-Arg-4-nitroanilide + H2O S-2238 Homo sapiens D-Phe-Pip-Arg + 4-nitroaniline
-
 ?
Factor Va + H2O activated protein C downregulates thrombin formation through proteolytic inactivation of factor Va by cleavage at Arg506 and Arg306. Docking of APC to FVa and FVIIIa constitutes the first step in the inactivation of the cofactor Homo sapiens ?
-
 ?
Factor VIIIa + H2O activated protein C downregulates thrombin formation through proteolytic inactivation of factor VIIIa by cleavage at Arg336 and Arg56. Docking of APC to FVa and FVIIIa constitutes the first step in the inactivation of the cofactor Homo sapiens ?
-
 ?
pyroGlu-Pro-Arg-4-nitroanilide + H2O S-2366 Homo sapiens pyroGlu-Pro-Arg + 4-nitroaniline
-
 ?

Synonyms

Synonyms Comment Organism
Activated protein C
-
 Homo sapiens
APC
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

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

General Information

General Information Comment Organism
physiological function activated protein C downregulates thrombin formation through proteolytic inactivation of factor Va and factor VIIIa, the anticoagulant activity may be important for in vivo regulation of thrombin formation Homo sapiens