Nicolas Moitessier
McGill University
Canada
Title: Computer-aided design, efficient synthesis and mechanistic studies of serine protease covalent inhibitors
Biography
Biography: Nicolas Moitessier
Abstract
Covalent serine peptidase inhibitors. Prolyl oligopeptidase, DPP-IV and fibroblast activation protein α are serine exo- and endopeptidases from the S9 family which are targets for cancer, Alzheimer’s disease and diabetes type II therapeutics. These 3 enzymes have been inhibited using covalent inhibitors. Our approach combined software development (covalent docking), synthesis, biochemistry and biophysical approaches to develop novel active inhibitors and develop methods for mechanistic studies of covalent inhibition. This integrated approach led to the discovery of a number of novel potent chemical series, novel synthetic methodologies and a better understanding of the covalent inhibition