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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.
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.
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: hackos dh. Science. 2015 Dec 18;350(6267):aac5464. doi: 10.1126/science.aac5464. Science. 2015. PMID: 26680203
A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain.
Wang TM, Brown BM, Deng L, Sellers BD, Lupardus PJ, Wallweber HJA, Gustafson A, Wong E, Volgraf M, Schwarz JB, Hackos DH, Hanson JE. Wang TM, et al. Among authors: hackos dh. Neuropharmacology. 2017 Jul 15;121:204-218. doi: 10.1016/j.neuropharm.2017.04.041. Epub 2017 Apr 27. Neuropharmacology. 2017. PMID: 28457974 Free article.
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.
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: hackos dh. Cell Rep. 2018 Sep 18;24(12):3133-3145. doi: 10.1016/j.celrep.2018.08.063. Cell Rep. 2018. PMID: 30231997 Free article.
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