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  • Title: Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders.
    Author: De Nanteuil G, Gloanec P, Béguin S, Giesen PL, Hemker HC, Mennecier P, Rupin A, Verbeuren TJ.
    Journal: J Med Chem; 2006 Aug 24; 49(17):5047-50. PubMed ID: 16913694.
    Abstract:
    The synthesis and evaluation of inhibitors of activated protein C (aPC) are reported. This serine protease is partly responsible for the degradation of factor VIIIa, involved in the regulation of bleeding in hemophilia A. Benzamidine-containing derivatives were found to be potent aPC inhibitors, some of them showing selectivity against the procoagulant protease thrombin. Moreover, compound 1 significantly restored the generation of thrombin in hemophiliac plasma.
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