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Literature summary for 3.4.21.69 extracted from
- Activated protein C mutant with minimal anticoagulant activity, normal cytoprotective activity, and preservation of thrombin activable fibrinolysis inhibitor-dependent cytoprotective functions (2007), J. Biol. Chem., 282, 33022-33033.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| stable, functional expression of wild-type and mutant enzymes in HEK-293 cells | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| R229A/R230A/K191A/K192A/K193A | site-directed mutagenesis, construction of an APC protease domain mutant, 5A-APC, the mutant has minimal anticoagulant activity but normal cytoprotective activities that are dependent on endothelial protein C receptor and protease-activated receptor-1 as compared to the wild-tpe enzyme, activation of thrombin activable fibrinolysis inhibitor is essentially unaffected by 5A-APC due to its low anticoagulant activity, a 1000fold higher concentration of 5A-APC is required to give a factor Va inactivation pattern similar to that of recombinant wild-type APC | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| extracellular | - |
Homo sapiens | - |
- |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | required | 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 | - |
? | |
| additional information | Homo sapiens | activated protein C reduces mortality in severe sepsis patients and exhibits beneficial effects in multiple animal injury models. APC anticoagulant activity involves inactivation of factors Va and VIIIa, whereas APC cytoprotective activities involve the endothelial protein C receptor and protease-activated receptor-1, PAR-1, anticoagulantly active APC inhibits secondary extended thrombin generation and concomitant thrombin dependent activation of thrombin activable fibrinolysis inhibitor in plasma, both recombinant wild-type and mutant APCs inhibit staurosporine-induced endothelial cell apoptosis | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| proteolytic modification | protein C is activated by thrombin | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| plasma | - |
Homo sapiens | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
measurements of modification of gene expression, APC cytoprotective activity, endothelial barrier protection, and anticoagulant activity, overview | 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, cleavage at Arg306 and Arg506 | Homo sapiens | inactive factor V + domain B | - |
? | |
| bradykinin + H2O | proteolytic inactivation | Homo sapiens | ? | - |
? | |
| additional information | activated protein C reduces mortality in severe sepsis patients and exhibits beneficial effects in multiple animal injury models. APC anticoagulant activity involves inactivation of factors Va and VIIIa, whereas APC cytoprotective activities involve the endothelial protein C receptor and protease-activated receptor-1, PAR-1, anticoagulantly active APC inhibits secondary extended thrombin generation and concomitant thrombin dependent activation of thrombin activable fibrinolysis inhibitor in plasma, both recombinant wild-type and mutant APCs inhibit staurosporine-induced endothelial cell apoptosis | Homo sapiens | ? | - |
? | |
| Z-Gly-Gly-Arg-7-amido-4-methylcoumarin + H2O | a fluorogenic substrate, S-2366 | 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 |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
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