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Page 1
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.
Focken T, Chowdhury S, Zenova A, Grimwood ME, Chabot C, Sheng T, Hemeon I, Decker SM, Wilson M, Bichler P, Jia Q, Sun S, Young C, Lin S, Goodchild SJ, Shuart NG, Chang E, Xie Z, Li B, Khakh K, Bankar G, Waldbrook M, Kwan R, Nelkenbrecher K, Karimi Tari P, Chahal N, Sojo L, Robinette CL, White AD, Chen CA, Zhang Y, Pang J, Chang JH, Hackos DH, Johnson JP Jr, Cohen CJ, Ortwine DF, Sutherlin DP, Dehnhardt CM, Safina BS. Focken T, et al. Among authors: hackos dh. J Med Chem. 2018 Jun 14;61(11):4810-4831. doi: 10.1021/acs.jmedchem.7b01826. Epub 2018 May 23. J Med Chem. 2018. PMID: 29737846
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
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
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.
Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity.
Sun S, Jia Q, Zenova AY, Wilson MS, Chowdhury S, Focken T, Li J, Decker S, Grimwood ME, Andrez JC, Hemeon I, Sheng T, Chen CA, White A, Hackos DH, Deng L, Bankar G, Khakh K, Chang E, Kwan R, Lin S, Nelkenbrecher K, Sellers BD, DiPasquale AG, Chang J, Pang J, Sojo L, Lindgren A, Waldbrook M, Xie Z, Young C, Johnson JP, Robinette CL, Cohen CJ, Safina BS, Sutherlin DP, Ortwine DF, Dehnhardt CM. Sun S, et al. Among authors: hackos dh. J Med Chem. 2019 Jan 24;62(2):908-927. doi: 10.1021/acs.jmedchem.8b01621. Epub 2018 Dec 21. J Med Chem. 2019. PMID: 30499663
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
52 results