Task-Force Covid-19

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.

Save the date : 10th Screening School, Bioscreen 2020

The 10th Summer School of Screening, Bioscreen 2020

will take place in les Hauts-de-France Region

from the 29th September to the 2nd of October 2020



10ème Ecole Thématique de Criblage, Bioscreen 2020

« Criblage, optimisation et caractérisation de petites molécules pour explorer et soigner le vivant »

L’édition lilloise (ETC2020, Bioscreen 2020) aura lieu

dans le centre de conférence du ValJoly, Eppe-Sauvage, du 29 septembre au 2 octobre 2020.

Cette école thématique récurrente sur le criblage moléculaire souhaite regrouper des participants multidisciplinaires, académiques et industriels, afin de stimuler des échanges dans ce domaine. Cette manifestation sera l’occasion de former de nouveaux acteurs, mais également de présenter de nouvelles approches scientifiques et méthodologiques aux participants déjà expérimentés.

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

New Positions available!

24-month PostDoc position in BIOLOGICAL SCREENING SCIENCES .
Deadline Sept, 7, 2020

24-month PostDoc position in MEDICINAL CHEMISTRY
Deadline Sept 7,2020

Follow link

Latest Publications

(truncated titles)

Faïon, L., et al, M. Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors. European Journal of Medicinal Chemistry, 2020, 200: 112440. link

Lesire, L., et al, High-Throughput Image-Based Aggresome Quantification, SLAS DISCOVERY, 2020: in press link

Villemagne, B., et al Fragment-Based Optimized EthR Inhibitors, ACS Infect Dis,2020, 6(3): 366-378 link

Singh, N., et al, Virtual screening web servers, Brief Bioinform,2020: in press link

Lu, Y., et al, Gly197Arg mutation in protein C causes recurrent thrombosis, Journal of Thrombosis and Haemostasis,2020, 18(5): 1141-1153 link

Herledan, A., et al  CETSA-aRPPA for Target engagement, SLAS Disc.,2020, 25(2): 207–214 link

Gyulkhandanyan, A., et al Analysis of protein missense alterations, Mol Genet Genomic Med,2020, e1166 link

Bosc, D., et al Kinetic Target-Guided Synthesis, J. Med. Chem., 2020, 3817−3833 link



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