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Literature summary for 3.4.21.69 extracted from

  • Yang, L.; Bae, J.S.; Manithody, C.; Rezaie, A.R.
    Identification of a specific exosite on activated protein C for interaction with protease-activated receptor 1 (2007), J. Biol. Chem., 282, 25493-25500.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
vitamin K dependent on Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant enzymes in HEK-293 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
E167A site-directed mutagenesis, the surface loop residue mutation eliminates the cytoprotective signaling properties of APC without affecting its anticoagulant activity, inability of E167A to exhibit significant protective activity in response to TNF-alpha-induced inflammatory events in endothelial cells Homo sapiens
E170A site-directed mutagenesis, the surface loop residue mutation eliminates the cytoprotective signaling properties of APC without affecting its anticoagulant activity, inability of E170A to exhibit significant protective activity in response to TNF-alpha-induced inflammatory events in endothelial cells Homo sapiens
S195A site-directed mutagenesis, inactive mutant Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Protein C inhibitor inhibits wild-type enzyme and mutants E167A and E170A Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information steady-state kinetics Homo sapiens
0.234
-
SpPCa pH 7.4, 37°C, recombinant wild-type enzyme Homo sapiens
0.249
-
SpPCa pH 7.4, 37°C, recombinant mutant E167A Homo sapiens
0.258
-
SpPCa pH 7.4, 37°C, recombinant mutant E170A Homo sapiens

Localization

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

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
56000
-
x * 56000, SDS-PAGE Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
active factor Va + H2O Homo sapiens proteolytic inactivation inactive factor V + domain B
-
?
active factor VIIIa + H2O Homo sapiens proteolytic inactivation inactive factor VIII + domain B
-
?
protease activated receptor 1 + H2O Homo sapiens APC exhibits cytoprotective and antiinflammatory activity through the endothelial protein C receptor-dependent cleavage of protease activated receptor 1, PAR-1, on endothelial cells ?
-
?

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.
active factor Va + H2O proteolytic inactivation Homo sapiens inactive factor V + domain B
-
?
active factor Va + H2O proteolytic inactivation, the basic residues of two surface loops including those on 39 and the Ca2+-binding 70-80 loops constitute interactive sites for both factors Va and VIIIa, thereby mediating the interaction of APC specifically with these procoagulant cofactors Homo sapiens inactive factor V + domain B
-
?
active factor VIIIa + H2O proteolytic inactivation Homo sapiens inactive factor VIII + domain B
-
?
active factor VIIIa + H2O proteolytic inactivation, the basic residues of two surface loops including those on 39 and the Ca2+-binding 70-80 loops constitute interactive sites for both factors Va and VIIIa, thereby mediating the interaction of APC specifically with these procoagulant cofactors Homo sapiens inactive factor VIII + domain B
-
?
additional information the enzyme is a vitamin K-dependent serine protease Homo sapiens ?
-
?
protease activated receptor 1 + H2O APC exhibits cytoprotective and antiinflammatory activity through the endothelial protein C receptor-dependent cleavage of protease activated receptor 1, PAR-1, on endothelial cells Homo sapiens ?
-
?
protease activated receptor 1 + H2O activation, the basic residues of surface loops are indispensable for interaction with APC, also two acidic residues on helix-162, Glu167 and Glu170, on the protease domain of APC which are required for the protease interaction with PAR-1 Homo sapiens ?
-
?
S2238 + H2O a commercial chromogenic substrate Homo sapiens ?
-
?
SpPCa + H2O a commercial tripeptidyl chromogenic substrate Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
? x * 56000, SDS-PAGE Homo sapiens

Synonyms

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

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
anticoagulation assay at Homo sapiens
37
-
amidohydrolytic assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
33.1
-
SpPCa pH 7.4, 37°C, recombinant wild-type enzyme Homo sapiens
34
-
SpPCa pH 7.4, 37°C, recombinant mutant E167A Homo sapiens
35
-
SpPCa pH 7.4, 37°C, recombinant mutant E170A Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens