Jalal Soubhye, Michel Gelbcke, Pierre Van Antwerpen, François Dufrasne, Mokhtaria Yasmina Boufadi, Jean Nève, Paul G Furtmüller, Christian Obinger, Karim Zouaoui Boudjeltia, Franck Meyer
The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally, in vivo evaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation.
February 9, 2017: ACS Medicinal Chemistry Letters