General Presentation

Our lab is dedicated to drug design, discovery and selection. Our project teams gather chemists and biologists cooperating with scientists who work on novel target discovery and validation. Our mission is to design and prepare ligands modulating the effects of these proteins in vitro first and in animal model ultimately. These compounds serve first as pharmacological probe to validate therapeutic approaches and then as drug prototypes. Our know-how is a combination of academic and industrial experience. It spans from medicinal chemistry, parallel synthesis and library management to high throughput screening bioanalysis and early DMPK. We foster close ties with industrial teams and academic researchers, especially with structural biologists (team lead by Vincent Villeret CNRS UMR8161, WJ Tang University of Chicago) and molecular modellers (Bruno Villoutreix, INSERM U648).
We are open to any collaboration where medchem, screening and DMPK can unlatch new drug research and accelerate the translation of new therapeutic concept into drug discovery.

Technologies and equipments

The INSERM U1177 unit is located both at the Faculty of Pharmacy of Lille and at the Pasteur Institute of Lille, in two labs interconnected by a private computer network. It has assembled a library of about 90,000 compounds, distributed into 180,000 vials divided in 3 sections. Sample logistic has been developed that relies on an Access-type data base, built-up in collaboration with Accelrys, Inc.,: this software provides a fast, intuitive set of tools for the storage, retrieval and presentation of chemical data - directly within a familiar and flexible environment. The INSERM U761 unit has access to a comprehensive platform of equipment comprising an automatic screening-robot system, several plate handling options for robotics providing 96, and 384 well liquid dispensing, microplate reader systems using different fluorescent modes, and a LC-MSMS based ADME (absorption, distribution, metabolism and excretion) profiling, to explore and detect organic compounds in complex biological samples.

Scientific Project

Our aim is to uncover and validate novel drug targets and to initiate drug discovery programs. The rich network of research laboratories and scientific or clinical expertise available at the Pasteur Institute of Lille and at Lille 2 University offers several possibilities to search for novel pharmacological targets and identify some of their molecular modulators using our technologies, such as high-throughput molecular screening, analyses of phenotypic changes in cells or model organisms, co-crystallization or combinatorial synthesis catalyzed by the target itself. Further explorations of the biological activities of these modulators can be performed using in vitro and in vivo models. Combining highly effective screening and profiling technologies with parallel synthesis and novel combinatorial chemistry and drug design techniques, the activities of these first molecular modulators can be optimized to obtain lead compounds and then, ideally, drug candidates. The proximity on the Campus of a recombinant protein production facility and of the X-Ray crystallography research unit headed by Vincent Villeret facilitates the work of medicinal chemists and accelerates the optimisation of active compounds though a process of structure-based discovery: a smooth transition from target validation to the first steps of drug discovery would then be possible.

 

The INSERM U1177 unit «Drugs and Molecules for Living Systems» was created on January 2006, as a part of the Federative Research Institutes IFR 142 « molecular and cellular medicine » of the Pasteur Institute Lille and co-founding unit of the c-Dithem, Inserm Consortium for Discovery and Innovation in Therapy and Medicine. Together with the Institut de Chimie Pharmaceutique Albert Lespagnol, it is at the origin of the Interdisciplinary Research Pole for the Drug Discovery, registered and funded by the Contrat de Projets, which federates more than 30 scientists specialized in medicinal chemistry, pharmaceutical chemistry, radiochemistry, analytical chemistry or pharmacology at the CNRS, l'INSERM, Lille1 or Lille2 universities (www.drugdiscoverylille.org)

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