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Page 1
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: andrez jc. Science. 2015 Dec 18;350(6267):aac5464. doi: 10.1126/science.aac5464. Science. 2015. PMID: 26680203
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: andrez jc. 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: andrez jc. 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
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy.
Focken T, Burford K, Grimwood ME, Zenova A, Andrez JC, Gong W, Wilson M, Taron M, Decker S, Lofstrand V, Chowdhury S, Shuart N, Lin S, Goodchild SJ, Young C, Soriano M, Tari PK, Waldbrook M, Nelkenbrecher K, Kwan R, Lindgren A, de Boer G, Lee S, Sojo L, DeVita RJ, Cohen CJ, Wesolowski SS, Johnson JP Jr, Dehnhardt CM, Empfield JR. Focken T, et al. Among authors: andrez jc. J Med Chem. 2019 Nov 14;62(21):9618-9641. doi: 10.1021/acs.jmedchem.9b01032. Epub 2019 Oct 3. J Med Chem. 2019. PMID: 31525968
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: andrez jc. 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
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: andrez jc. Elife. 2022 Mar 2;11:e72468. doi: 10.7554/eLife.72468. Elife. 2022. PMID: 35234610 Free PMC article.
Mitomycins syntheses: a recent update.
Andrez JC. Andrez JC. Beilstein J Org Chem. 2009 Jul 8;5:33. doi: 10.3762/bjoc.5.33. Beilstein J Org Chem. 2009. PMID: 19777135 Free PMC article.
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: andrez jc. 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
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: andrez jc. Br J Pharmacol. 2024 Oct;181(20):3993-4011. doi: 10.1111/bph.16481. Epub 2024 Jun 24. Br J Pharmacol. 2024. PMID: 38922847
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