Structure of active coagulation factor XIII published - milestone on the way to safe anticoagulation

Date: Oct-16-2013Zedira, in cooperation with the group of Prof. Gerhard Klebe in Marburg, reported the first crystal structure of coagulation factor XIII in the active conformation. The article is now published in Angewandte Chemie International Edition and provides a proprietary high-resolution structure of FXIIIa in complex with the inhibitor ZED1301 serving as lead structure. The data are of enormous value for structure based drug design.

Direct acting Factor XIIIa-blockers may provide a novel and safe option for preventing thrombotic events. Such inhibitors would not impair the thrombin level or primary clot formation by platelet activation, but would effectively reduce the mechanical stability and half-life of clots, thereby accelerating fibrinolysis. This approach has the potential of overcoming the apparent strong link between anticoagulation and life threatening bleeding tendencies that limit the use of anticoagulants today.
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