U1177 fights antimicrobial resistance (AMR)
The french research Unit 1177 Inserm/IPL/Univ. lille and its AIDD group is committed to fight against antimicrobial resistance !! #AntibioticAwarenessWeek #ResistanceSymbol #AntibioticResistance
Big thanks to our funding agencies and partners @ANR @JPIAMR @isiteULNE @pearl_phd_lille @CIILofficiel @hautsdefrance @Bioversys
Picture from @JoaquimDassonville
A team of researchers from U1177 (in collaboration with U1167 and CIIL) has started a project to discover and optimize inhibitors of the 3CLpro protease of SARS-CoV-2, a non-structural coronavirus protein essential in its replication cycle.
High throughput enzymatic screening of a 100,000-compound library of U1177 based on fluorescent substrate cleavage is in progress. Hit-to-lead optimization will then be performed using the medicinal chemistry tools. The project aims at discovering new broad-spectrum antivirals (preclinical candidates) to deliver therapeutic treatment for the current outbreak or as a preparedness measure in case of future viral outbreaks.
Therapeutic Innovation : Discovery Across Boundaries
U1177 (formerly U761), directed by Pr. Benoit Deprez, is dedicated to drug design, discovery and selection.
The Lab's mission is to design and study compounds that modulates selected molecular targets in a desired way to treat infectious and metabolic diseases.
Our projects engage researchers across physical, chemical and biological sciences to trade ideas and knowledge and sincerely endeavor to validate new therapeutic concepts with drug prototypes and bring drugs candidates to the clinic.
- Developing cutting edge methods for quantitative pharmacology (High Content Screening, Pharmacokinetics)
- Designing the next generation of anti-TB antibiotics : ethionamide boosters.
- Deciphering the role(s) of Insulin Degrading Enzyme in diabetes with several families of modulators.
- Modulating the molecular interplay between intestine, liver and muscles with TGR5 ligands to treat diabetes.
- Developing small chemical modulators of antigenic presentation.
We are open to any type of collaboration with biologists or chemist from academia and industry where medicinal chemistry, in vitro pharmacology and pharmacokinetics enable or accelerate the translation of new therapeutic concept into drug discovery.
Our researchers are committed to the highest standards of scientific quality and integrity in everything they do. We use up-to date electronic lab books to sustainably capitalize knowledge and facilitate collaborations between multiple research sites.
Most of our researchers are also faculty members who teach in PharmD and MSc courses in pharmacy, drug discovery, medicinal chemistry, organic chemistry, and R&D strategies.
A journey with the team
Founding member of the network Chembioscreen
Camberlein, V., et al. Multi-Component Reaction for the Preparation of 1,5-Disubstituted 1,2,3-Triazoles. Tetrahedron Letters, 2021. link
Castellanos-Jankiewicz, A., et al. Hypothalamic bile acid-TGR5 signaling protects from obesity. Cell Metabolism,2021. link
Hoguet, V., et al. Beyond the Rule of 5: Impact of PEGylation. Journal of Medicinal Chemistry,2021. link
Medve, L., et al Modulators of hERAP2. Eur. J. Med. Chem.,2020. link
Guieu, B., et al, Desirable drug–drug interactions or when a matter of concern becomes a renewed therapeutic strategy. Drug Discovery Today,2020. link
Faïon, L., et al, M. Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors. European Journal of Medicinal Chemistry, 2020. link
Lesire, L., et al, High-Throughput Image-Based Aggresome Quantification. SLAS DISCOVERY, 2020. link