Activated Protein C: A Promising Drug with Multiple Effects?

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.

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