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Page 1
TRPA1 as a drug target--promise and challenges.
Chen J, Hackos DH. Chen J, et al. Among authors: hackos dh. Naunyn Schmiedebergs Arch Pharmacol. 2015 Apr;388(4):451-63. doi: 10.1007/s00210-015-1088-3. Epub 2015 Feb 3. Naunyn Schmiedebergs Arch Pharmacol. 2015. PMID: 25640188 Free PMC article. Review.
α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.
Verma VA, Shore DGM, Chen H, Chen J, Do S, Hackos DH, Kolesnikov A, Lyssikatos JP, Tay S, Wang L, Estrada AA. Verma VA, et al. Among authors: hackos dh. Bioorg Med Chem Lett. 2016 Jan 15;26(2):495-498. doi: 10.1016/j.bmcl.2015.11.088. Epub 2015 Nov 25. Bioorg Med Chem Lett. 2016. PMID: 26706172
Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors.
Chernov-Rogan T, Li T, Lu G, Verschoof H, Khakh K, Jones SW, Beresini MH, Liu C, Ortwine DF, McKerrall SJ, Hackos DH, Sutherlin D, Cohen CJ, Chen J. Chernov-Rogan T, et al. Among authors: hackos dh. Proc Natl Acad Sci U S A. 2018 Jan 23;115(4):E792-E801. doi: 10.1073/pnas.1713701115. Epub 2018 Jan 8. Proc Natl Acad Sci U S A. 2018. PMID: 29311306 Free PMC article.
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: hackos dh. 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
Structural Basis of Nav1.7 Inhibition by a Gating-Modifier Spider Toxin.
Xu H, Li T, Rohou A, Arthur CP, Tzakoniati F, Wong E, Estevez A, Kugel C, Franke Y, Chen J, Ciferri C, Hackos DH, Koth CM, Payandeh J. Xu H, et al. Among authors: hackos dh. Cell. 2019 Feb 7;176(4):702-715.e14. doi: 10.1016/j.cell.2018.12.018. Epub 2019 Jan 17. Cell. 2019. PMID: 30661758 Free article.
Structural Basis of Nav1.7 Inhibition by a Gating-Modifier Spider Toxin.
Xu H, Li T, Rohou A, Arthur CP, Tzakoniati F, Wong E, Estevez A, Kugel C, Franke Y, Chen J, Ciferri C, Hackos DH, Koth CM, Payandeh J. Xu H, et al. Among authors: hackos dh. Cell. 2019 Feb 21;176(5):1238-1239. doi: 10.1016/j.cell.2019.01.047. Cell. 2019. PMID: 30794776 Free article. No abstract available.
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: hackos dh. 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. Among authors: hackos dh. 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.
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