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

Publication on tetrahydrofuran‑based TRPA1 antagonists, their ligand‑based discovery, rodent asthma model activity, and cryo‑EM mechanism‑of‑action

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Authors: Jack A. Terrett, Huifen Chen, Daniel G. Shore, Elisia Villemure, Robin Larouche-Gauthier, Martin Déry, Francis Beaumier, Léa Constantineau-Forget, Chantal Grand-Maître, Luce Lépissier, Stéphane Ciblat, Claudio Sturino, Yong Chen, Baihua Hu, Aijun Lu, Yunli Wang, Andrew P. Cridland, Stuart I Ward, David H. Hackos, Rebecca M. Reese, Shannon D. Shields, Jun Chen, Alessia Balestrini, Lorena Riol-Blanco, Wyne P. Lee, John Liu, Eric Suto, Xiumin Wu, Juan Zhang, Justin Q. Ly, Hank La, Kevin Johnson, Matt Baumgardner, Kang-Jye Chou, Alexis Rohou, Lionel Rougé, Brian S. Safina, Steven Magnuson, Matthew Volgraf

J Med Chem. 2021 Apr 8;64(7):3843-3869

DOI: 10.1021/acs.jmedchem.0c02023

Access the publication at:https://pubmed.ncbi.nlm.nih.gov/33749283/