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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: chen j, chen l, chen h, chen y. 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.
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: chen j, chen h, chen y. 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
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: chen j, chen y. 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
Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors.
Hu DX, Patel S, Chen H, Wang S, Staben ST, Dimitrova YN, Wallweber HA, Lee JY, Chan GKY, Sneeringer CJ, Prangley MS, Moffat JG, Wu KC, Schutt LK, Salphati L, Pang J, McNamara E, Huang H, Chen Y, Wang Y, Zhao W, Lim J, Murthy A, Siu M. Hu DX, et al. Among authors: chen h, chen y. J Med Chem. 2022 Sep 8;65(17):11500-11512. doi: 10.1021/acs.jmedchem.1c01180. Epub 2021 Nov 15. J Med Chem. 2022. PMID: 34779204
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.
Burch JD, Lau K, Barker JJ, Brookfield F, Chen Y, Chen Y, Eigenbrot C, Ellebrandt C, Ismaili MH, Johnson A, Kordt D, MacKinnon CH, McEwan PA, Ortwine DF, Stein DB, Wang X, Winkler D, Yuen PW, Zhang Y, Zarrin AA, Pei Z. Burch JD, et al. Among authors: chen y. J Med Chem. 2014 Jul 10;57(13):5714-27. doi: 10.1021/jm500550e. Epub 2014 Jun 27. J Med Chem. 2014. PMID: 24918870
Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.
Burch JD, Barrett K, Chen Y, DeVoss J, Eigenbrot C, Goldsmith R, Ismaili MH, Lau K, Lin Z, Ortwine DF, Zarrin AA, McEwan PA, Barker JJ, Ellebrandt C, Kordt D, Stein DB, Wang X, Chen Y, Hu B, Xu X, Yuen PW, Zhang Y, Pei Z. Burch JD, et al. Among authors: chen y. J Med Chem. 2015 May 14;58(9):3806-16. doi: 10.1021/jm501998m. Epub 2015 Apr 16. J Med Chem. 2015. PMID: 25844760
Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases.
Liu K, Li D, Zheng W, Shi M, Chen Y, Tang M, Yang T, Zhao M, Deng D, Zhang C, Liu J, Yuan X, Yang Z, Chen L. Liu K, et al. Among authors: chen l, chen y. J Med Chem. 2021 Jul 8;64(13):8951-8970. doi: 10.1021/acs.jmedchem.1c00004. Epub 2021 Jun 17. J Med Chem. 2021. PMID: 34138567
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