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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: brunskill apj. 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.
Discovery of SCH 900229, a Potent Presenilin 1 Selective γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease.
Wu WL, Domalski M, Burnett DA, Josien H, Bara T, Rajagopalan M, Xu R, Clader J, Greenlee WJ, Brunskill A, Hyde LA, Del Vecchio RA, Cohen-Williams ME, Song L, Lee J, Terracina G, Zhang Q, Nomeir A, Parker EM, Zhang L. Wu WL, et al. ACS Med Chem Lett. 2012 Apr 9;3(11):892-6. doi: 10.1021/ml300044f. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900404 Free PMC article.
Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease.
Scott JD, Li SW, Brunskill AP, Chen X, Cox K, Cumming JN, Forman M, Gilbert EJ, Hodgson RA, Hyde LA, Jiang Q, Iserloh U, Kazakevich I, Kuvelkar R, Mei H, Meredith J, Misiaszek J, Orth P, Rossiter LM, Slater M, Stone J, Strickland CO, Voigt JH, Wang G, Wang H, Wu Y, Greenlee WJ, Parker EM, Kennedy ME, Stamford AW. Scott JD, et al. J Med Chem. 2016 Dec 8;59(23):10435-10450. doi: 10.1021/acs.jmedchem.6b00307. Epub 2016 Nov 18. J Med Chem. 2016. PMID: 27933948
A multifunctional catalyst that stereoselectively assembles prodrugs.
DiRocco DA, Ji Y, Sherer EC, Klapars A, Reibarkh M, Dropinski J, Mathew R, Maligres P, Hyde AM, Limanto J, Brunskill A, Ruck RT, Campeau LC, Davies IW. DiRocco DA, et al. Science. 2017 Apr 28;356(6336):426-430. doi: 10.1126/science.aam7936. Science. 2017. PMID: 28450641
24 results