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Page 1
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT 2nd, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, San Miguel T, Sickmier EA, Vargas HM, Wahl RC, Wen PH, Whittington DA, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Dineen TA, et al. Among authors: sickmier ea. J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468684
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).
Cheng Y, Judd TC, Bartberger MD, Brown J, Chen K, Fremeau RT Jr, Hickman D, Hitchcock SA, Jordan B, Li V, Lopez P, Louie SW, Luo Y, Michelsen K, Nixey T, Powers TS, Rattan C, Sickmier EA, St Jean DJ Jr, Wahl RC, Wen PH, Wood S. Cheng Y, et al. Among authors: sickmier ea. J Med Chem. 2011 Aug 25;54(16):5836-57. doi: 10.1021/jm200544q. Epub 2011 Jul 29. J Med Chem. 2011. PMID: 21707077
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid.
Weiss MM, Williamson T, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dineen TA, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, Rattan C, San Miguel T, Sickmier EA, Wahl RC, Wen PH, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Weiss MM, et al. Among authors: sickmier ea. J Med Chem. 2012 Nov 8;55(21):9009-24. doi: 10.1021/jm300119p. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468639
A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase.
Kaller MR, Harried SS, Albrecht B, Amarante P, Babu-Khan S, Bartberger MD, Brown J, Brown R, Chen K, Cheng Y, Citron M, Croghan MD, Graceffa R, Hickman D, Judd T, Kriemen C, La D, Li V, Lopez P, Luo Y, Masse C, Monenschein H, Nguyen T, Pennington LD, Miguel TS, Sickmier EA, Wahl RC, Weiss MM, Wen PH, Williamson T, Wood S, Xue M, Yang B, Zhang J, Patel V, Zhong W, Hitchcock S. Kaller MR, et al. Among authors: sickmier ea. ACS Med Chem Lett. 2012 Mar 29;3(11):886-91. doi: 10.1021/ml3000148. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900403 Free PMC article.
Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3.
Murray JK, Qian YX, Liu B, Elliott R, Aral J, Park C, Zhang X, Stenkilsson M, Salyers K, Rose M, Li H, Yu S, Andrews KL, Colombero A, Werner J, Gaida K, Sickmier EA, Miu P, Itano A, McGivern J, Gegg CV, Sullivan JK, Miranda LP. Murray JK, et al. Among authors: sickmier ea. J Med Chem. 2015 Sep 10;58(17):6784-802. doi: 10.1021/acs.jmedchem.5b00495. Epub 2015 Aug 31. J Med Chem. 2015. PMID: 26288216
Facile Modulation of Antibody Fucosylation with Small Molecule Fucostatin Inhibitors and Cocrystal Structure with GDP-Mannose 4,6-Dehydratase.
Allen JG, Mujacic M, Frohn MJ, Pickrell AJ, Kodama P, Bagal D, San Miguel T, Sickmier EA, Osgood S, Swietlow A, Li V, Jordan JB, Kim KW, Rousseau AC, Kim YJ, Caille S, Achmatowicz M, Thiel O, Fotsch CH, Reddy P, McCarter JD. Allen JG, et al. Among authors: sickmier ea. ACS Chem Biol. 2016 Oct 21;11(10):2734-2743. doi: 10.1021/acschembio.6b00460. Epub 2016 Aug 11. ACS Chem Biol. 2016. PMID: 27434622
Structural Basis for Apelin Control of the Human Apelin Receptor.
Ma Y, Yue Y, Ma Y, Zhang Q, Zhou Q, Song Y, Shen Y, Li X, Ma X, Li C, Hanson MA, Han GW, Sickmier EA, Swaminath G, Zhao S, Stevens RC, Hu LA, Zhong W, Zhang M, Xu F. Ma Y, et al. Among authors: sickmier ea. Structure. 2017 Jun 6;25(6):858-866.e4. doi: 10.1016/j.str.2017.04.008. Epub 2017 May 18. Structure. 2017. PMID: 28528775 Free article.
20 results