Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders

Guillaume De Nanteuil*, Philippe Gloanec, Suzette Beguin, Peter L. A. Giesen, H. Coenraad Hemker, Philippe Mennecier, Alain Rupin, Tony J. Verbeuren

*Corresponding author for this work

    Research output: Contribution to journalComment/Letter to the editorAcademicpeer-review

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    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.
    Original languageEnglish
    Pages (from-to)5047-5050
    Number of pages4
    JournalJournal of Medicinal Chemistry
    Issue number17
    Publication statusPublished - 25 Jul 2006

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