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A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment.
Balestrini A, Joseph V, Dourado M, Reese RM, Shields SD, Rougé L, Bravo DD, Chernov-Rogan T, Austin CD, Chen H, Wang L, Villemure E, Shore DGM, Verma VA, Hu B, Chen Y, Leong L, Bjornson C, Hötzel K, Gogineni A, Lee WP, Suto E, Wu X, Liu J, Zhang J, Gandham V, Wang J, Payandeh J, Ciferri C, Estevez A, Arthur CP, Kortmann J, Wong RL, Heredia JE, Doerr J, Jung M, Vander Heiden JA, Roose-Girma M, Tam L, Barck KH, Carano RAD, Ding HT, Brillantes B, Tam C, Yang X, Gao SS, Ly JQ, Liu L, Chen L, Liederer BM, Lin JH, Magnuson S, Chen J, Hackos DH, Elstrott J, Rohou A, Safina BS, Volgraf M, Bauer RN, Riol-Blanco L. Balestrini A, et al. Among authors: reese rm. J Exp Med. 2021 Apr 5;218(4):e20201637. doi: 10.1084/jem.20201637. J Exp Med. 2021. PMID: 33620419 Free PMC article. Clinical Trial.
Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.
Chen H, Volgraf M, Do S, Kolesnikov A, Shore DG, Verma VA, Villemure E, Wang L, Chen Y, Hu B, Lu AJ, Wu G, Xu X, Yuen PW, Zhang Y, Erickson SD, Dahl M, Brotherton-Pleiss C, Tay S, Ly JQ, Murray LJ, Chen J, Amm D, Lange W, Hackos DH, Reese RM, Shields SD, Lyssikatos JP, Safina BS, Estrada AA. Chen H, et al. Among authors: reese rm. J Med Chem. 2018 Apr 26;61(8):3641-3659. doi: 10.1021/acs.jmedchem.8b00117. Epub 2018 Apr 12. J Med Chem. 2018. PMID: 29590749
A Non-covalent Ligand Reveals Biased Agonism of the TRPA1 Ion Channel.
Liu C, Reese R, Vu S, Rougé L, Shields SD, Kakiuchi-Kiyota S, Chen H, Johnson K, Shi YP, Chernov-Rogan T, Greiner DMZ, Kohli PB, Hackos D, Brillantes B, Tam C, Li T, Wang J, Safina B, Magnuson S, Volgraf M, Payandeh J, Zheng J, Rohou A, Chen J. Liu C, et al. Neuron. 2021 Jan 20;109(2):273-284.e4. doi: 10.1016/j.neuron.2020.10.014. Epub 2020 Nov 4. Neuron. 2021. PMID: 33152265 Free PMC article.
Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310.
Safina BS, McKerrall SJ, Sun S, Chen CA, Chowdhury S, Jia Q, Li J, Zenova AY, Andrez JC, Bankar G, Bergeron P, Chang JH, Chang E, Chen J, Dean R, Decker SM, DiPasquale A, Focken T, Hemeon I, Khakh K, Kim A, Kwan R, Lindgren A, Lin S, Maher J, Mezeyova J, Misner D, Nelkenbrecher K, Pang J, Reese R, Shields SD, Sojo L, Sheng T, Verschoof H, Waldbrook M, Wilson MS, Xie Z, Young C, Zabka TS, Hackos DH, Ortwine DF, White AD, Johnson JP Jr, Robinette CL, Dehnhardt CM, Cohen CJ, Sutherlin DP. Safina BS, et al. J Med Chem. 2021 Mar 25;64(6):2953-2966. doi: 10.1021/acs.jmedchem.1c00049. Epub 2021 Mar 8. J Med Chem. 2021. PMID: 33682420
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.
Terrett JA, Chen H, Shore DG, 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 AP, Ward SI, Hackos DH, Reese RM, Shields SD, Chen J, Balestrini A, Riol-Blanco L, Lee WP, Liu J, Suto E, Wu X, Zhang J, Ly JQ, La H, Johnson K, Baumgardner M, Chou KJ, Rohou A, Rougé L, Safina BS, Magnuson S, Volgraf M. Terrett JA, et al. Among authors: reese rm. J Med Chem. 2021 Apr 8;64(7):3843-3869. doi: 10.1021/acs.jmedchem.0c02023. Epub 2021 Mar 22. J Med Chem. 2021. PMID: 33749283
Nav1.7 is essential for nociceptor action potentials in the mouse in a manner independent of endogenous opioids.
Deng L, Dourado M, Reese RM, Huang K, Shields SD, Stark KL, Maksymetz J, Lin H, Kaminker JS, Jung M, Foreman O, Tao J, Ngu H, Joseph V, Roose-Girma M, Tam L, Lardell S, Orrhult LS, Karila P, Allard J, Hackos DH. Deng L, et al. Among authors: reese rm. Neuron. 2023 Sep 6;111(17):2642-2659.e13. doi: 10.1016/j.neuron.2023.05.024. Epub 2023 Jun 22. Neuron. 2023. PMID: 37352856 Free article.
39 results