Application | Comment | Organism |
---|---|---|
medicine | the activated protein C exhibits anti-inflammatory and cytoprotective properties, which may contribute to the beneficial effect of APC in treating severe sepsis patients, a higher incidence of bleeding because of its anticoagulant function is a major drawback of APC as an effective anti-inflammatory drug | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
R67C/R82C | site-directed mutagenesis, construction of a protein C variant in which an engineered disulfide bond between two beta-sheets stabilizes the functionally critical Ca2+-binding 70-80 loop of the molecule. The 70-80 loop of this mutant no longer binds Ca2+, and the activation of the mutant by thrombin is enhanced 60-80fold independently of thrombomodulin, the anticoagulant activity of the activated protein C mutant is nearly eliminated. The endothelial protein C receptor- and protease activated receptor-1-dependent protective signaling properties of the mutant are minimally altered compared to the wild-type enzyme. The mutant loses its ability to interact with the procoagulant cofactors but not with the protective signaling molecules. The binding of EPCR is 2fold reduced compared to the wild-type enzyme | Homo sapiens |
S195A | site-directed mutagenesis, inactive mutant | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
extracellular | activated protein C | Homo sapiens | - |
- |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | required, calcium enhances the amidolytic activity of APC by 2fold, the Ca2+ and Na+ metal ion-binding sites are linked energetically | Homo sapiens | |
Na+ | the amidolytic activity of APC is strictly dependent on Na+, the Ca2+ and Na+ metal ion-binding sites are linked energetically | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
active factor Va + H2O | Homo sapiens | proteolytic inactivation requires interactions with both EPCR and PAR-1 | inactive factor V + domain B | - |
? | |
additional information | Homo sapiens | in addition to an anticoagulant activity, activated protein C also exhibits anti-inflammatory and cytoprotective properties, but can cause bleeding because of its anticoagulant function, the cytoprotective activity of APC is mediated through inhibition of caspase-3 activity | ? | - |
? | |
protease activated receptor 1 + H2O | Homo sapiens | activation | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
glycoprotein | different variants | Homo sapiens |
proteolytic modification | the protein C zymogen is activate through cleavage by thrombin in a Ca2+-dependent manner, thrombin acts in complex with the required thrombomodulin, the reaction is is markedly stimulated by endothelial protein C receptor | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
plasma | activated protein C | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
active factor Va + H2O | proteolytic inactivation requires interactions with both EPCR and PAR-1 | Homo sapiens | inactive factor V + domain B | - |
? | |
additional information | in addition to an anticoagulant activity, activated protein C also exhibits anti-inflammatory and cytoprotective properties, but can cause bleeding because of its anticoagulant function, the cytoprotective activity of APC is mediated through inhibition of caspase-3 activity | Homo sapiens | ? | - |
? | |
protease activated receptor 1 + H2O | activation | Homo sapiens | ? | - |
? | |
protease activated receptor 1 + H2O | activation, cleavage at Arg41 | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Activated protein C | - |
Homo sapiens |
APC | - |
Homo sapiens |