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Page 1
Discovery of novel cyclopentane carboxylic acids as potent and selective inhibitors of NaV1.7.
Sun S, Chowdhury S, Hemeon I, Hasan A, Wilson MS, Bergeron P, Jia Q, Zenova AY, Grimwood ME, Gong W, Decker SM, Bichler P, Andrez JC, Focken T, Ngyuen T, Zhu J, White AD, Bankar G, Howard S, Chang E, Khakh K, Lin S, Dean R, Johnson JP Jr, Chang JH, Hackos DH, McKerrall SJ, Sellers B, Ortwine DF, Cohen CJ, Safina BS, Sutherlin DP, Dehnhardt CM. Sun S, et al. Among authors: dean r. Bioorg Med Chem Lett. 2025 Feb 1;116:130033. doi: 10.1016/j.bmcl.2024.130033. Epub 2024 Nov 22. Bioorg Med Chem Lett. 2025. PMID: 39580005
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. Among authors: dean r. 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
Identification of aryl sulfonamides as novel and potent inhibitors of NaV1.5.
Sun S, Jia Q, Zenova AY, Lin S, Hussainkhel A, Mezeyova J, Chang E, Goodchild SJ, Xie Z, Lindgren A, de Boer G, Kwan R, Khakh K, Sojo L, Bichler P, Johnson JP Jr, Empfield JR, Cohen CJ, Dehnhardt CM, Dean R. Sun S, et al. Among authors: dean r. Bioorg Med Chem Lett. 2021 Aug 1;45:128133. doi: 10.1016/j.bmcl.2021.128133. Epub 2021 May 24. Bioorg Med Chem Lett. 2021. PMID: 34044121
NBI-921352, a first-in-class, NaV1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats.
Johnson JP, Focken T, Khakh K, Tari PK, Dube C, Goodchild SJ, Andrez JC, Bankar G, Bogucki D, Burford K, Chang E, Chowdhury S, Dean R, de Boer G, Decker S, Dehnhardt C, Feng M, Gong W, Grimwood M, Hasan A, Hussainkhel A, Jia Q, Lee S, Li J, Lin S, Lindgren A, Lofstrand V, Mezeyova J, Namdari R, Nelkenbrecher K, Shuart NG, Sojo L, Sun S, Taron M, Waldbrook M, Weeratunge D, Wesolowski S, Williams A, Wilson M, Xie Z, Yoo R, Young C, Zenova A, Zhang W, Cutts AJ, Sherrington RP, Pimstone SN, Winquist R, Cohen CJ, Empfield JR. Johnson JP, et al. Among authors: dean r. Elife. 2022 Mar 2;11:e72468. doi: 10.7554/eLife.72468. Elife. 2022. PMID: 35234610 Free PMC article.
The contribution of NaV1.6 to the efficacy of voltage-gated sodium channel inhibitors in wild type and NaV1.6 gain-of-function (GOF) mouse seizure control.
Johnson JP Jr, Focken T, Karimi Tari P, Dube C, Goodchild SJ, Andrez JC, Bankar G, Burford K, Chang E, Chowdhury S, Christabel J, Dean R, de Boer G, Dehnhardt C, Gong W, Grimwood M, Hussainkhel A, Jia Q, Khakh K, Lee S, Li J, Lin S, Lindgren A, Lofstrand V, Mezeyova J, Nelkenbrecher K, Shuart NG, Sojo L, Sun S, Waldbrook M, Wesolowski S, Wilson M, Xie Z, Zenova A, Zhang W, Scott FL, Cutts AJ, Sherrington RP, Winquist R, Cohen CJ, Empfield JR. Johnson JP Jr, et al. Among authors: dean r. Br J Pharmacol. 2024 Oct;181(20):3993-4011. doi: 10.1111/bph.16481. Epub 2024 Jun 24. Br J Pharmacol. 2024. PMID: 38922847
Molecular Pharmacology of Selective NaV1.6 and Dual NaV1.6/NaV1.2 Channel Inhibitors that Suppress Excitatory Neuronal Activity Ex Vivo.
Goodchild SJ, Shuart NG, Williams AD, Ye W, Parrish RR, Soriano M, Thouta S, Mezeyova J, Waldbrook M, Dean R, Focken T, Ghovanloo MR, Ruben PC, Scott F, Cohen CJ, Empfield J, Johnson JP. Goodchild SJ, et al. Among authors: dean r. ACS Chem Neurosci. 2024 Mar 20;15(6):1169-1184. doi: 10.1021/acschemneuro.3c00757. Epub 2024 Feb 15. ACS Chem Neurosci. 2024. PMID: 38359277 Free PMC article.
Expanding the genotype-phenotype spectrum in SCN8A-related disorders.
Hebbar M, Al-Taweel N, Gill I, Boelman C, Dean RA, Goodchild SJ, Mezeyova J, Shuart NG, Johnson JP Jr, Lee J, Michoulas A, Huh LL, Armstrong L, Connolly MB, Demos MK. Hebbar M, et al. BMC Neurol. 2024 Jan 17;24(1):31. doi: 10.1186/s12883-023-03478-y. BMC Neurol. 2024. PMID: 38233770 Free PMC article.
Expanding the genotype-phenotype spectrum in SCN8A-related disorders.
Hebbar M, Al-Taweel N, Gill I, Boelman C, Dean RA, Goodchild SJ, Mezeyova J, Shuart NG, Johnson JP, Lee J, Michoulas A, Huh LL, Armstrong L, Connolly MB, Demos MK. Hebbar M, et al. Res Sq [Preprint]. 2023 Aug 8:rs.3.rs-3221902. doi: 10.21203/rs.3.rs-3221902/v1. Res Sq. 2023. Update in: BMC Neurol. 2024 Jan 17;24(1):31. doi: 10.1186/s12883-023-03478-y PMID: 37609289 Free PMC article. Updated. Preprint.
1,715 results