| Literature DB >> 28197313 |
Jalal Soubhye1, Michel Gelbcke1, Pierre Van Antwerpen1, François Dufrasne1, Mokhtaria Yasmina Boufadi2, Jean Nève1, Paul G Furtmüller3, Christian Obinger3, Karim Zouaoui Boudjeltia4, Franck Meyer5.
Abstract
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.Entities:
Keywords: Myeloperoxidase; dynamic combinatorial chemistry; kinetic study; molecular docking; reversible and irreversible inhibitors
Year: 2016 PMID: 28197313 PMCID: PMC5304337 DOI: 10.1021/acsmedchemlett.6b00417
Source DB: PubMed Journal: ACS Med Chem Lett ISSN: 1948-5875 Impact factor: 4.345