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Page 1
Association of respiratory failure with inhibition of NaV1.6 in the phrenic nerve.
Klein RM, Layton ME, Regan H, Regan CP, Li Y, Filzen T, Cato M, Clements MK, Wang J, Sanoja R, Greshock TJ, Roecker AJ, Pero JE, Kim R, Burgey C, John CT, Wang YH, Bhandari N, Struyk A, Kraus RL, Henze DA, Houghton AK. Klein RM, et al. Among authors: layton me. Channels (Austin). 2022 Dec;16(1):230-243. doi: 10.1080/19336950.2022.2122309. Channels (Austin). 2022. PMID: 36239534 Free PMC article.
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.
Pero JE, Rossi MA, Kelly MJ 3rd, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, Jacobson MA. Pero JE, et al. Among authors: layton me. ACS Med Chem Lett. 2016 Jan 10;7(3):312-7. doi: 10.1021/acsmedchemlett.5b00459. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985321 Free PMC article.
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice.
Roecker AJ, Egbertson M, Jones KLG, Gomez R, Kraus RL, Li Y, Koser AJ, Urban MO, Klein R, Clements M, Panigel J, Daley C, Wang J, Finger EN, Majercak J, Santarelli V, Gregan I, Cato M, Filzen T, Jovanovska A, Wang YH, Wang D, Joyce LA, Sherer EC, Peng X, Wang X, Sun H, Coleman PJ, Houghton AK, Layton ME. Roecker AJ, et al. Among authors: layton me. Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093. doi: 10.1016/j.bmcl.2017.03.085. Epub 2017 Mar 30. Bioorg Med Chem Lett. 2017. PMID: 28389149
Benzoxazolinone aryl sulfonamides as potent, selective Nav1.7 inhibitors with in vivo efficacy in a preclinical pain model.
Pero JE, Rossi MA, Lehman HDGF, Kelly MJ 3rd, Mulhearn JJ, Wolkenberg SE, Cato MJ, Clements MK, Daley CJ, Filzen T, Finger EN, Gregan Y, Henze DA, Jovanovska A, Klein R, Kraus RL, Li Y, Liang A, Majercak JM, Panigel J, Urban MO, Wang J, Wang YH, Houghton AK, Layton ME. Pero JE, et al. Among authors: layton me. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2683-2688. doi: 10.1016/j.bmcl.2017.04.040. Epub 2017 Apr 22. Bioorg Med Chem Lett. 2017. PMID: 28465103
Nav1.7 target modulation and efficacy can be measured in nonhuman primate assays.
Kraus RL, Zhao F, Pall PS, Zhou D, Vardigan JD, Danziger A, Li Y, Daley C, Ballard JE, Clements MK, Klein RM, Holahan MA, Greshock TJ, Kim RM, Layton ME, Burgey CS, Serra J, Henze DA, Houghton AK. Kraus RL, et al. Among authors: layton me. Sci Transl Med. 2021 May 19;13(594):eaay1050. doi: 10.1126/scitranslmed.aay1050. Sci Transl Med. 2021. PMID: 34011626
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.
Roecker AJ, Layton ME, Pero JE, Kelly MJ 3rd, Greshock TJ, Kraus RL, Li Y, Klein R, Clements M, Daley C, Jovanovska A, Ballard JE, Wang D, Zhao F, Brunskill APJ, Peng X, Wang X, Sun H, Houghton AK, Burgey CS. Roecker AJ, et al. Among authors: layton me. ACS Med Chem Lett. 2021 Jun 1;12(6):1038-1049. doi: 10.1021/acsmedchemlett.1c00218. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141090 Free PMC article.
Invention of MK-7845, a SARS-CoV-2 3CL Protease Inhibitor Employing a Novel Difluorinated Glutamine Mimic.
Shurtleff VW, Layton ME, Parish CA, Perkins JJ, Schreier JD, Wang Y, Adam GC, Alvarez N, Bahmanjah S, Bahnck-Teets CM, Boyce CW, Burlein C, Cabalu TD, Campbell BT, Carroll SS, Chang W, de Lera Ruiz M, Dolgov E, Fay JF, Fox NG, Goh SL, Hartingh TJ, Hurzy DM, Kelly MJ 3rd, Klein DJ, Klingler FM, Krishnamurthy H, Kudalkar S, Mayhood TW, McKenna PM, Murray EM, Nahas D, Nawrat CC, Park S, Qian D, Roecker AJ, Sharma V, Shipe WD, Su J, Taggart RV, Truong Q, Wu Y, Zhou X, Zhuang N, Perlin DS, Olsen DB, Howe JA, McCauley JA. Shurtleff VW, et al. Among authors: layton me. J Med Chem. 2024 Mar 14;67(5):3935-3958. doi: 10.1021/acs.jmedchem.3c02248. Epub 2024 Feb 16. J Med Chem. 2024. PMID: 38365209
Discovery of 3-substituted aminocyclopentanes as potent and orally bioavailable NR2B subtype-selective NMDA antagonists.
Layton ME, Kelly MJ 3rd, Rodzinak KJ, Sanderson PE, Young SD, Bednar RA, Dilella AG, McDonald TP, Wang H, Mosser SD, Fay JF, Cunningham ME, Reiss DR, Fandozzi C, Trainor N, Liang A, Lis EV, Seabrook GR, Urban MO, Yergey J, Koblan KS. Layton ME, et al. ACS Chem Neurosci. 2011 Jul 20;2(7):352-62. doi: 10.1021/cn200013d. Epub 2011 Apr 15. ACS Chem Neurosci. 2011. PMID: 22816022 Free PMC article.
54 results