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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: magnuson s. 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.
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. Among authors: magnuson s. 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. Among authors: magnuson s. 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.
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: magnuson s. 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 selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.
Crawford TD, Ndubaku CO, Chen H, Boggs JW, Bravo BJ, Delatorre K, Giannetti AM, Gould SE, Harris SF, Magnuson SR, McNamara E, Murray LJ, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Stanley M, Vitorino P, Wang L, West K, Wu P, Ye W. Crawford TD, et al. Among authors: magnuson sr. J Med Chem. 2014 Apr 24;57(8):3484-93. doi: 10.1021/jm500155b. Epub 2014 Apr 9. J Med Chem. 2014. PMID: 24673130
Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors.
Wang L, Stanley M, Boggs JW, Crawford TD, Bravo BJ, Giannetti AM, Harris SF, Magnuson SR, Nonomiya J, Schmidt S, Wu P, Ye W, Gould SE, Murray LJ, Ndubaku CO, Chen H. Wang L, et al. Among authors: magnuson sr. Bioorg Med Chem Lett. 2014 Sep 15;24(18):4546-4552. doi: 10.1016/j.bmcl.2014.07.071. Epub 2014 Aug 2. Bioorg Med Chem Lett. 2014. PMID: 25139565
Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.
Burdick DJ, Wang S, Heise C, Pan B, Drummond J, Yin J, Goeser L, Magnuson S, Blaney J, Moffat J, Wang W, Chen H. Burdick DJ, et al. Among authors: magnuson s. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4728-4732. doi: 10.1016/j.bmcl.2015.08.048. Epub 2015 Aug 22. Bioorg Med Chem Lett. 2015. PMID: 26338362
Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer.
Jin L, Garcia J, Chan E, de la Cruz C, Segal E, Merchant M, Kharbanda S, Raisner R, Haverty PM, Modrusan Z, Ly J, Choo E, Kaufman S, Beresini MH, Romero FA, Magnuson S, Gascoigne KE. Jin L, et al. Among authors: magnuson s. Cancer Res. 2017 Oct 15;77(20):5564-5575. doi: 10.1158/0008-5472.CAN-17-0314. Epub 2017 Aug 17. Cancer Res. 2017. PMID: 28819026
87 results