Activated Protein C: A Promising Drug with Multiple Effects?

Author(s): S.T. B.G. Loubele, H. M.H. Spronk, H. ten Cate.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 9 , Issue 5 , 2009

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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

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Article Details

VOLUME: 9
ISSUE: 5
Year: 2009
Page: [620 - 626]
Pages: 7
DOI: 10.2174/138955709788167547
Price: $58

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