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The Science

SerpinPC inhibits APC

APC degrades the complex that makes thrombin; SerpinPC inhibits APC, allowing prothrombinase more time to make thrombin.








SerpinPC is an irreversible inhibitor of APC

How SerpinPC inhibits APC. APC recognises the RCL of SerpinPC as a substrate (middle). During the cleavage of the scissile bond, APC is translocated to the opposite pole of SerpinPC and inactivated through conformational disruption. The final covalent complex (right) is rapidly cleared by the liver.





 


Design and characterization of an APC-specific serpin for the treatment of hemophilia
- Commentary in Blood

Design and characterization of an APC-specific serpin for the treatment of hemophilia.

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BLOOD JOURNAL, 5 JANUARY 2017
Correcting the hemophilic imbalance

Polderdijk et al design and evaluate a therapeutic inhibitor of activated protein C.1...

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CURRENT OPINION IN HEMATOLOGY, SEPTEMBER 2017
Targeting activated protein C to treat hemophilia

Hemostasis is a dynamic process involving procoagulant and anticoagulant factors operating simultaneously to detect and repair damage to the vascular endothelium, and to prevent inappropriate clot formation. Perturbations affecting this balance cause bleeding or thrombosis, because of insufficient or excessive formation of the enzyme thrombin....

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