Abstract
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.
Keywords: APC, anti-coagulation, cytoprotection, animal injury models
Mini-Reviews in Medicinal Chemistry
Title: Activated Protein C: A Promising Drug with Multiple Effects?
Volume: 9 Issue: 5
Author(s): S.T. B.G. Loubele, H. M.H. Spronk and H. ten Cate
Affiliation:
Keywords: APC, anti-coagulation, cytoprotection, animal injury models
Abstract: 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.
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Cite this article as:
Loubele B.G. S.T., Spronk M.H. H. and Cate ten H., Activated Protein C: A Promising Drug with Multiple Effects?, Mini-Reviews in Medicinal Chemistry 2009; 9 (5) . https://dx.doi.org/10.2174/138955709788167547
DOI https://dx.doi.org/10.2174/138955709788167547 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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