In 1995, I started studying Chemistry at Lille (France). In 1999, I moved to Warwick University (UK) to discover Chemical Biology and carbohydrates synthesis. Back to France in 2000, I received a master degree in Organic Chemistry (Lille). I decided to further explore medicinal chemistry and received a Ph.D. in 2003 under the direction of Pr. André Tartar. Appointed lecturer in 2002, I assumed the position of assistant Professor of Organic Chemistry at the school of Pharmacy in Lille between 2004 and 2013. In 2013, I was appointed Full Professor of Organic Chemistry.
My research program in the Inserm U1177 unit, leading by Pr. B. Deprez, focuses on three main topics:
(a) the development of new scaffolds and new synthesis procedures for the design of chemical libraries,
(b) the development of new strategies to fight infectious diseases (especially tuberculosis),
(c) the design of new tools for chemical biology approaches based on click-chemistry strategies.
During my Ph.D., I started working on the development of the regional chemical library by selecting lead-like and drug-like molecules from commercial libraries thanks to the development of in silico filters. In parallel, I worked on the design of new scaffolds and privileged structures used for the synthesis of focused libraries (Willand et al. Tet. Lett. 2004). Moreover I validated the discovery of new chemical pathways for the synthesis of drug-like molecules (Willand et al. Tet. Lett. 2007) and identified new multi-component synthesis to enrich the chemical library with original structures (Toto et al. Tet. Lett. 2006). Today, this library, which is now composed of almost 70 000 compounds, has already been given hits after screening on many targets (enzymes, receptors, protein protein interactions) and continues to grow thanks to chemical innovations (Jida et al. 2011).
In a second part of my research, I focus on the development of new strategies to fight tuberculosis, lying on the boosting of known antibiotics. This work started 9 years ago in collaboration with microbiologists (A. Baulard, Lille and P. Brodin, Seoul) and crystallographers (V. Villeret, Lille). In this context, we validated a mycobacterial transcriptional repressor EthR as a new target to boost ethionamide, and discovered inhibitors thanks to three complementary approaches: a structure-based design, a high-throughput screening of the regional library based on the development of new assays and a fragment-based strategy. 4 years later, we published in the prestigious review Nature Medicine the proof of principle after testing our lead compound in a mouse model of tuberculosis infection (Willand et al. Nat. Med. 2009). Today, we have so far identified 3 distinct chemical families of boosters after a second round of optimization (Flipo et al. J. Med. Chem. 2011 & 2012). We have now started the preclinical development of candidates in collaboration with the Swiss company Bioversys and GlaxoSmithKline under the funding of the Wellcome Trust.
For these achievements, I received in 2009 the prize for the creation of innovative technologies from Oseo and the french ministry of research and in 2011 the Award in Medicinal Chemistry from the French Society of Therapeutic Chemistry and Servier Laboratories.
Over the past 10 years, I have demonstrated skills to supervise projects in the field of applied organic chemistry, drug design and chemical biology. This work has resulted in the identification of candidates for regulatory preclinical development. My scientific production accounts for: 30 publications in peer-reviewed journals, 2 publications in a book of international conference, 5 patent applications licensed to Bioversys A.G. and 6 oral presentations as guest speaker.
