Activated Protein C: A Promising Drug with Multiple Effects?
| Autor: | Henri M. H. Spronk, Sarah T.B.G. Loubele, H. ten Cate |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Drug
Cells media_common.quotation_subject Mutant Inflammation Drug Discovery Animals Humans Medicine media_common Pharmacology Endothelial protein C receptor business.industry Anticoagulants General Medicine In vitro Enzyme Activation Cytoprotection Apoptosis Immunology Cancer research Animal studies medicine.symptom business Protein C Signal Transduction medicine.drug |
| Zdroj: | Mini-Reviews in Medicinal Chemistry. 9:620-626 |
| ISSN: | 1389-5575 |
| DOI: | 10.2174/138955709788167547 |
| Popis: | The anti-coagulant activated protein C (APC) can exert direct effects on cells, including cytoprotective functions involving apoptosis and inflammation mechanisms. These cytoprotective properties of APC require the presence of protease-activated receptor-1 (PAR-1) and endothelial protein C receptor (EPCR) resulting in inhibition of inflammatory gene expression and down-regulation of p53 and Bax. Several in vitro and animal studies have documented such cytoprotective properties of APC. The first evidence for a cytoprotective role of APC in a clinical setting came from the PROWESS trial in which APC administration reduced mortality rates in severe sepsis patients. However, although APC certainly has the potential to be used in a broader range of clinical settings it is thwarted by the associated risk of bleeding. Further research within this area towards improved therapeutics of specific APC mutants has taken place. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|