Title: Metabolomic clustering of antibiotic mechanisms of action. A tool for novelty assessment

Biography:

Gilles Courtemanche completed his PhD from Pierre & Marie Curie University (Paris, France) in 1991. After more than 20 years in the pharma industry as Medicinal Chemist and Drug Discovery Expert, he is now the Director of the Antimicrobials Program at BIOASTER, a French Technology Research Institute dedicated to Microbiology and Infectious Diseases. He has published more than 12 papers in reputed journals and is an inventor on more than 20 patents.

Abstract

With the growing spread of antibiotic resistance, everyone agrees there is an urgent need to identify new and innovative antibiotics. Innovative means not only novel chemotypes but also new Mechanisms of Action (MoA). Several new and promising targets have been identified, but target-based screening remains a challenge, since the vast majority of compounds active on the isolated target are inactive on the whole bacteria because of a lack membrane penetration. That’s why phenotypic screening is usually preferred, but in this case, the MoA of hits is unknown. Deciphering a MoA is a long and costly process that is mostly dedicated to Development Candidates, after several years of efforts since hit identification, with substantial financial resources spent. Assessing the novelty of MoA at hit identification stage would allow focussing on the most promising series, saving money and time in drug discovery. A medium throughput screening of hit mechanisms of action, using metabolomics will be presented.