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Robust Pharmacodynamic Effect of LY3202626, a Central Nervous System Penetrant, Low Dose BACE1 Inhibitor, in Humans and Nonclinical Species.
J Alzheimers Dis Rep. 2022 Jan 11;6(1):1-15. doi: 10.3233/ADR-210037. eCollection 2022.
J Alzheimers Dis Rep. 2022.
PMID: 35243208
Free PMC article.
The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans.
May PC, Willis BA, Lowe SL, Dean RA, Monk SA, Cocke PJ, Audia JE, Boggs LN, Borders AR, Brier RA, Calligaro DO, Day TA, Ereshefsky L, Erickson JA, Gevorkyan H, Gonzales CR, James DE, Jhee SS, Komjathy SF, Li L, Lindstrom TD, Mathes BM, Martényi F, Sheehan SM, Stout SL, Timm DE, Vaught GM, Watson BM, Winneroski LL, Yang Z, Mergott DJ.
May PC, et al. Among authors: borders ar.
J Neurosci. 2015 Jan 21;35(3):1199-210. doi: 10.1523/JNEUROSCI.4129-14.2015.
J Neurosci. 2015.
PMID: 25609634
Free PMC article.
Clinical Trial.
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Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.
McKinzie DL, Winneroski LL, Green SJ, Hembre EJ, Erickson JA, Willis BA, Monk SA, Aluise CD, Baker TK, Lopez JE, Hendle J, Beck JP, Brier RA, Boggs LN, Borders AR, Cocke PJ, Garcia-Losada P, Lowe SL, Mathes BM, May PC, Porter WJ, Stout SL, Timm DE, Watson BM, Yang Z, Mergott DJ.
McKinzie DL, et al. Among authors: borders ar.
J Med Chem. 2021 Jun 24;64(12):8076-8100. doi: 10.1021/acs.jmedchem.1c00489. Epub 2021 Jun 3.
J Med Chem. 2021.
PMID: 34081466
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Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.
Winneroski LL, Schiffler MA, Erickson JA, May PC, Monk SA, Timm DE, Audia JE, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hudziak KJ, Klimkowski VJ, Garcia Losada P, Mathes BM, Stout SL, Watson BM, Mergott DJ.
Winneroski LL, et al. Among authors: borders ar.
Bioorg Med Chem. 2015 Jul 1;23(13):3260-8. doi: 10.1016/j.bmc.2015.04.062. Epub 2015 May 6.
Bioorg Med Chem. 2015.
PMID: 26001341
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Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Winneroski LL, Erickson JA, Green SJ, Lopez JE, Stout SL, Porter WJ, Timm DE, Audia JE, Barberis M, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hembre EJ, Hendle J, Garcia-Losada P, Minguez JM, Mathes BM, May PC, Monk SA, Rankovic Z, Shi Y, Watson BM, Yang Z, Mergott DJ.
Winneroski LL, et al. Among authors: borders ar.
Bioorg Med Chem. 2020 Jan 1;28(1):115194. doi: 10.1016/j.bmc.2019.115194. Epub 2019 Nov 15.
Bioorg Med Chem. 2020.
PMID: 31786008
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