Principal Investigator Barbara Imperiali
We apply fragment-based screening and structure-driven approaches for development of synthetic small molecule inhibitors of bacterial virulence. The targets that we focus on are the biosynthetic enzymes that lead to prokaryote-specific bacterial sugars commonly found in virulence-associated glycoconjugates. Our synthetic approaches exploit a wide range of reactions, including heterocycle generation, transition metal-catalyzed coupling, and click-type conjugation in order to efficiently synthesize diverse inhibitors for in vitro and in vivo assays as well as structure analysis of inhibitor-bound enzyme complexes.