New antiviral agents to fight emerging coronaviruses

The project aims to design new molecules capable of inhibiting an essential component of coronavirus functioning in order to identify a treatment for COVID-19 but also therapeutic weapons indispensable to potential future coronavirus-related epidemics. In this context, the 3CL protease (3CL-Pro, MPro), a highly conserved protease within this family of viruses and essential to the viral cycle of coronaviruses, appears to be a promising therapeutic target. The multiparametric optimization of several families of compounds inhibiting this protease, identified in the laboratory through a high-throughput screening of a chemical library of 90,000 compounds, is in progress.

Team

Collaborators

Grants

Publications

2021

  • Cantrelle, F.-X., Boll, E., Brier, L., Moschidi, D., Belouzard, S., Landry, V., Leroux, F., Dewitte, F., Landrieu, I., Dubuisson, J., Deprez, B., Charton, J., & Hanoulle, X. NMR spectroscopy of the main protease of SARS-CoV-2 and fragment-based screening identify three protein hotspots and an antiviral fragment. Angewandte Chemie International Edition,2021, in press. 10.1002/anie.202109965. HAL

Communications

2021

  • Charton, J. Screening for the identification of new inhibitors of the 3CL protease of SARS-CoV-2,6th Scientific Meeting of the Institut Pasteur de Lille Marcq-en-Baroeul, France,14th Sept. 2021
  • Brier, L. Discovery of new inhibitors of the SARS-CoV-2 3CL protease by High Throughput Screening,28th SCT Young Research Fellows Meeting,Paris, France,11th-12th Feb. 2021 flashtalk.

2020

  • Brier, L., Landry, V., Dumont, J., Warenghem, S., Herledan, A., Hanoulle, X., Belouzard, S., Dubuisson, J., Florence, L., Benoit, D., & Julie, C. Discovery of new inhibitors of the SARS-CoV-2 3CL protease by High Throughput Screening,5th Drug Discovery Day - Conception Synthèse Evaluation et Sélection du principe actif,Lille, France,16th Dec. 2020.

Posters

2021

  • Brier, L., Landry, V., Dumont, J., Hassan, H., Warenghem, S., Herledan, A., Hanoulle, X., Belouzard, S., Dubuisson, J., Leroux, F., Deprez, B., & Charton, J. High throughput screening for the identification of new inhibitors of the 3cl protease of sars-cov-2,56th International Conference on Medicinal Chemistry, Interfacing Chemical Biology and Drug Discovery, Virtual Event, 7th-9th July,2021.
  • Brier, L., Landry, V., Bourgeois, F., Ikherbane, S., Dumont, J., Warenghem, S., Herledan, A., Hanoulle, X., Belouzard, S., Dubuisson, J., Florence, L., Benoit, D., & Julie, C. Discovery of new inhibitors of the SARS-CoV-2 3CL protease by High Throughput Screening 28th SCT Young Research Fellows Meeting, Paris, France, 11th-12th Feb.,2021.

 

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