The role of IRIC’s Drug Discovery Unit is to design and synthesize new small molecules having biological activity and potential therapeutic efficacy. Its specific objective is to optimize the biological activity of so-called hit or lead compounds, identified by high-throughput screening or targeted chemical synthesis, based on thorough investigation of their structure-activity relationships.
The laboratory is available to scientists interested in developing novel and specific molecular tools which are used to facilitate the understanding of novel, therapeutically relevant biological targets, as well as offering support in the discovery of small molecules with therapeutic potential. In the framework of collaborative agreements with pharmaceutical companies, it also offers industrial partners an integrated research strategy encompassing several stages of the drug discovery process, from optimization of hit or lead compounds to identification of clinical candidates.
The Drug Discovery Unit’s activities are led by a team of seasoned chemists and biologists who have extensive drug-discovery experience in an industrial setting, demonstrated by a portfolio of significant achievements across several major therapeutic areas. The expertise of these scientists with background in the pharmaceutical industry is an important asset in adding value to projects aimed at discovering new drugs for the treatment of cancer and other unmet medical needs.
- Synthesis of molecules upon request, development of avenues of synthesis, discovery of active compounds, hit-to-lead optimization, pre-clinical development
- Synthesis of chemical probes
- Computational chemistry,
- Dynamic molecular simulations, virtual screening of molecules, structure-based design
- Library-fragment generation
- Parallel, peptide and macrocyclic synthesis
- Development and implementation of in vitro bioassays for SAR studies
- Mechanism of action of active compounds
- Pharmacological characterization (biased signaling, allosteric modulators, binding site)
- Development of in vivo bioassays to measure the efficacy of the compounds
State-of-the-art instrumentation enables IRIC’s Drug Discovery Unit team to use the latest synthesis, purification and molecule analysis techniques, as well as the characterization of the biological activity related to those molecules.
Quadrupole and Time-of-Flight Mass Spectrometers
- Quadrupole and Time-of-Flight Mass Spectrometers (LC/MS TOF, LC/MS Simple Quad)
Analytical and preparative High-Performance Liquid Chromatography systems
- Reverse-phase and chiral columns
Automated Combi-flash chromatography instruments (ISCO, Biotage)
- Reverse- and normal phase columns
Auto-sampler microwave reactors for high-temperature chemical reactions
- Auto-sampler microwave reactors for high-temperature chemical reactions
Photochemistry equipment, photochemical reactors
- Photochemistry equipment, photochemical reactors
Nuclear magnetic resonance
- Nuclear magnetic resonance (NMR) spectrometers 400 and 600 MHz Varian
Fluorescence and luminescence reading devices (BRET)
- Plate reader Neo2 (Biotek)
- Plate reader Spark10M (Tecan)
Echo550 Acoustic Liquid Handler
- Echo550 Acoustic Liquid Handler (Labcyte)
Robotic system integrating bulk liquid dispenser, a plate reader and an Echo550 Acoustic Liquid Handler
- Robotic system integrating bulk liquid dispenser (Multidrop Combi), a plate reader (Neo2 and Saprk10M) and an Echo550 Acoustic Liquid Handler
Furthermore, the Medicinal and Biological Chemistry Laboratory uses a collection of over 15,000 commercial reagents traceable in real time with the Inventory app. The collection is constantly growing.
All members of the team have access to a full line of e-journals and sophisticated scientific literature research software online, data analysis software, as well as to the laboratory e-notebook.