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Page 1
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: safina bs. 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.
Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist.
Ahuja S, Mukund S, Deng L, Khakh K, Chang E, Ho H, Shriver S, Young C, Lin S, Johnson JP Jr, Wu P, Li J, Coons M, Tam C, Brillantes B, Sampang H, Mortara K, Bowman KK, Clark KR, Estevez A, Xie Z, Verschoof H, Grimwood M, Dehnhardt C, Andrez JC, Focken T, Sutherlin DP, Safina BS, Starovasnik MA, Ortwine DF, Franke Y, Cohen CJ, Hackos DH, Koth CM, Payandeh J. Ahuja S, et al. Among authors: safina bs. Science. 2015 Dec 18;350(6267):aac5464. doi: 10.1126/science.aac5464. Science. 2015. PMID: 26680203
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: safina bs. 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
Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain.
Bankar G, Goodchild SJ, Howard S, Nelkenbrecher K, Waldbrook M, Dourado M, Shuart NG, Lin S, Young C, Xie Z, Khakh K, Chang E, Sojo LE, Lindgren A, Chowdhury S, Decker S, Grimwood M, Andrez JC, Dehnhardt CM, Pang J, Chang JH, Safina BS, Sutherlin DP, Johnson JP Jr, Hackos DH, Robinette CL, Cohen CJ. Bankar G, et al. Among authors: safina bs. Cell Rep. 2018 Sep 18;24(12):3133-3145. doi: 10.1016/j.celrep.2018.08.063. Cell Rep. 2018. PMID: 30231997 Free article.
Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain.
McKerrall SJ, Nguyen T, Lai KW, Bergeron P, Deng L, DiPasquale A, Chang JH, Chen J, Chernov-Rogan T, Hackos DH, Maher J, Ortwine DF, Pang J, Payandeh J, Proctor WR, Shields SD, Vogt J, Ji P, Liu W, Ballini E, Schumann L, Tarozzo G, Bankar G, Chowdhury S, Hasan A, Johnson JP Jr, Khakh K, Lin S, Cohen CJ, Dehnhardt CM, Safina BS, Sutherlin DP. McKerrall SJ, et al. Among authors: safina bs. J Med Chem. 2019 Apr 25;62(8):4091-4109. doi: 10.1021/acs.jmedchem.9b00141. Epub 2019 Apr 16. J Med Chem. 2019. PMID: 30943032
TRPA1 modulation by piperidine carboxamides suggests an evolutionarily conserved binding site and gating mechanism.
Chernov-Rogan T, Gianti E, Liu C, Villemure E, Cridland AP, Hu X, Ballini E, Lange W, Deisemann H, Li T, Ward SI, Hackos DH, Magnuson S, Safina B, Klein ML, Volgraf M, Carnevale V, Chen J. Chernov-Rogan T, et al. Proc Natl Acad Sci U S A. 2019 Dec 17;116(51):26008-26019. doi: 10.1073/pnas.1913929116. Epub 2019 Dec 3. Proc Natl Acad Sci U S A. 2019. PMID: 31796582 Free PMC article.
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: safina bs. 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 TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-in-Class Therapy for Respiratory Disease.
Terrett JA, Ly JQ, Katavolos P, Hasselgren C, Laing S, Zhong F, Villemure E, Déry M, Larouche-Gauthier R, Chen H, Shore DG, Lee WP, Suto E, Johnson K, Brooks M, Stablein A, Beaumier F, Constantineau-Forget L, Grand-Maître C, Lépissier L, Ciblat S, Sturino C, Chen Y, Hu B, Elstrott J, Gandham V, Joseph V, Booler H, Cain G, Chou C, Fullerton A, Lepherd M, Stainton S, Torres E, Urban K, Yu L, Zhong Y, Bao L, Chou KJ, Lin J, Zhang W, La H, Liu L, Mulder T, Chen J, Chernov-Rogan T, Johnson AR, Hackos DH, Leahey R, Shields SD, Balestrini A, Riol-Blanco L, Safina BS, Volgraf M, Magnuson S, Kakiuchi-Kiyota S. Terrett JA, et al. Among authors: safina bs. J Med Chem. 2024 Mar 14;67(5):3287-3306. doi: 10.1021/acs.jmedchem.3c02121. Epub 2024 Mar 3. J Med Chem. 2024. PMID: 38431835
33 results