We are hiring!

Mingshuo Zeng, Jessica M. Grandner, Marian C. Bryan, Vishal Verma, Robin Larouche-Gauthier, Jean-Philippe Leclerc, Liang Zhao, Pouyan Haghshenas, Samuel Aubert-Nicol, Arun Yadav, Melissa Ashley, Jacob Z. Chen, Matthew Durk, Karen E. Samy, Marika Nespi, Elizabeth Levy,
Karl Merrick, John G. Moffat, Jeremy Murray, Angela Oh, Christine Orr, Ehud Segal, Jessica Sims, Christopher Sneeringer, Madeleine Prangley, Steffan Vartanian, Steven Magnuson, and Brendan T. Parr. ACS Med. Chem. Lett. 2023,42, 1704

Marineau, Jason J.; Hamman, Kristin B.; Hu, Shanhu; Alnemy, Sydney; Mihalich, Janessa; Kabro, Anzhelika; Whitmore, Kenneth Matthew; Winter, Dana K.; Roy, Stephanie; Ciblat, Stephane; Ke, Nan; Savinainen, Anneli; Wilsily, Ashraf; Malojcic, Goran; Zahler, Robert; Schmidt, Darby; Bradley, Michael J.; Waters, Nigel J.; Chuaqui, Claudio. Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7. J. Med. Chem. 2022 65, 1458

Terrett, J. A.; Chen, H.; Shore, D. G.; Villemure, E.; Larouche-Gauthier, R.; Déry, M.; Beaumier, F.; Constantineau-Forget, L.; Grand-Maître, C.; Lépissier, L.; Ciblat, S.; Sturino, C.; Chen, Y.; Hu, B.; Lu, A.; Wang, Y.; Cridland, A. P.; Ward, S. I.; Hackos, D. H.; Reese, R. M.; Shields, S. D.; Chen, J.; Balestrini, A.; Riol-Blanco, L.; Lee, W. P.; Liu, J.; Suto, E.; Wu, X.; Zhang, J.; Ly, J. Q.; La, H.; Johnson, K.; Baumgardner, M.; Chou, K.-J.; Rohou, A.; Rougé, L.; Safina, B. S.; Magnuson, S.; Volgraf, M. Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy. J. Med. Chem. 2021 ASAP

Vuillermet, F.; Bourret, J.; Pelletier, G. J. Org. Chem. 2020,86, 388

Beveridge, R. E.; Wallweber, H. A.; Ashkenazi, A.; Beresini, M.; Clark, K. R.; Gibbons, P.; Ghiro, E.; Kaufman, S.; Larivée, A.; Leblanc, M.; Leclerc, J.-P.; Lemire, A.; Ly, C.; Rudolph, J.; Schwarz, J. B.; Srivastava, S.; Wang, W.; Zhao, L.; Braun, M.-G. ACS Med. Chem. Lett. 2020,11 2389

Picard, A.; Ciblat, S.; Ramtohul, Y. K. Synlett 2020, 31, 507

Bronner, S. M.; Merrick, K. A.; Murray, J.; Salphati, L.; Moffat, J. G.; Pang, J.; Sneeringer, C. J.; Dompe, N.; Cyr, P.; Purkey, H.; Boenig, G. de L.; Li, J.; Kolesnikov, A.; Larouche-Gauthier, R.; Lai, K. W.; Shen, X.; Aubert-Nicol, S.; Chen, Y.-C.; Cheong, J.; Crawford, J. J.; Hafner, M.; Haghshenas, P.; Jakalian, A.; Leclerc, J.-P.; Lim, N.-K.; O’Brien, T.; Plise, E. G.; Shalan, H.; Sturino, C.; Wai, J.; Xiao, Y.; Yin, J.; Zhao, L.; Gould, S.; Olivero, A.; Heffron, T. P. Bioorganic & Medicinal Chemistry Letters 2019, 29, 2294

Cooper, A. B.; Ciblat, S.; Shipps, J.; Levine, J.; Kostura, M.; Oza, V.; Constantineau-Forget, L.; Dery, M.; Grand-Maître, C.; Bruneau-Latour, N.; Bellavance, E.; Siddiqui, M. A.; Luther, M. Bioorg. Med. Chem. Lett. 2017, 27, 4471

Ahmada, T.; Dansereau, J.; Héberta, M.; Grand-Maître, C.; Larivée, A.; Siddiqui, A.; Gagnon, A. Tetrahedron Lett. 2016, 57, 4284

Ding, H.; DeRoy, P.; Perreault, C.; Larivee, A.; Siddiqui, A.; Caldwell, C. G.; Harran, S.; Harran, P. G. Angew. Chem. Int. Ed. 2015, 54, 4818

A paper disclosing a retrospective analysis of the influence the binding sites and their location relative to the cell membrane on the optimization of two distinct series of TRPA1 antagonists was just published in the ACS Medicinal Chemistry Letters. This work was conducted in collaboration with Genentech.

Elisia Villemure, Jack A. Terrett, Robin Larouche-Gauthier, Martin Déry, Huifen Chen, Rebecca M. Reese, Shannon D. Shields, Jun Chen, Steven Magnuson, and Matthew Volgraf, ACS Med. Chem. Lett. 2021, ASAP - A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists