Target intelligence / Profile preview

Endothelial protein C receptor (EPCR) (EPCR)

Target
EPCR
Molecular classification
Receptor, MHC class I-like protein, CD antigen
01

Overview

The Endothelial protein C receptor (EPCR) is a Type I transmembrane glycoprotein primarily expressed on the surface of large vessel endothelial cells [1]. It plays a critical role in the protein C anticoagulant pathway by binding Protein C and presenting it to the thrombin-thrombomodulin complex, which significantly accelerates the generation of Activated Protein C (APC) [2]. In the context of xenotransplantation, human EPCR is expressed as a transgene on porcine endothelium to overcome molecular incompatibilities between pig and human coagulation systems, thereby preventing the rapid development of consumptive coagulopathy and thrombotic microangiopathy in the graft [3, 4]. Beyond its anticoagulant properties, the EPCR-APC complex triggers cytoprotective, anti-inflammatory, and anti-apoptotic signaling through the cleavage of Protease-activated receptor 1 (PAR-1) [2]. This dual role makes it a vital component in maintaining vascular integrity and regulating the host immune response during organ transplantation [4]. [1] UniProt (Q9UNN8); [2] PMID: 11069105; [3] PMID: 26458185; [4] PMID: 35045221.

Other names
PROCRCD201Activated protein C receptorAPC receptorProtein C receptor endothelial
02

Mechanism of action

EPCR binds Protein C and facilitates its activation by the thrombin-thrombomodulin complex on the endothelial surface. Once activated, Protein C (APC) dissociates or remains bound to EPCR to initiate cytoprotective signaling via PAR-1, which stabilizes the endothelial barrier and inhibits pro-inflammatory pathways [1, 2].

03

Biological functions

AnticoagulationAnti-inflammatoryCytoprotectionCell signalingVascular homeostasis
04

Disease associations

ThrombosisSepsisXenograft rejectionCoagulopathyInflammation
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Safety considerations

Shedding of the receptor into a soluble form (sEPCR) can neutralize APCPotential for localized bleedingImmunogenicity of the transgene in xenotransplantation [3]
06

Interacting drugs

Protein C

4 more in the full profile.

07

Biomarkers

Soluble EPCR (sEPCR)Activated Protein C (APC) levelsD-dimerThrombin-antithrombin (TAT) complexes

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