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.