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101 results

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Page 1
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: erickson ja. 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
P3 cap modified Phe*-Ala series BACE inhibitors.
Chen SH, Lamar J, Guo D, Kohn T, Yang HC, McGee J, Timm D, Erickson J, Yip Y, May P, McCarthy J. Chen SH, et al. Bioorg Med Chem Lett. 2004 Jan 5;14(1):245-50. doi: 10.1016/j.bmcl.2003.09.085. Bioorg Med Chem Lett. 2004. PMID: 14684336
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: erickson ja. 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.
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: erickson ja. 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
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: erickson ja. 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
Design and synthesis of statine-containing BACE inhibitors.
Hu J, Cwi CL, Smiley DL, Timm D, Erickson JA, McGee JE, Yang HC, Mendel D, May PC, Shapiro M, McCarthy JR. Hu J, et al. Among authors: erickson ja. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4335-9. doi: 10.1016/j.bmcl.2003.09.037. Bioorg Med Chem Lett. 2003. PMID: 14643321
Biochemical and kinetic characterization of BACE1: investigation into the putative species-specificity for beta- and beta'-cleavage sites by human and murine BACE1.
Yang HC, Chai X, Mosior M, Kohn W, Boggs LN, Erickson JA, McClure DB, Yeh WK, Zhang L, Gonzalez-DeWhitt P, Mayer JP, Martin JA, Hu J, Chen SH, Bueno AB, Little SP, McCarthy JR, May PC. Yang HC, et al. Among authors: erickson ja. J Neurochem. 2004 Dec;91(6):1249-59. doi: 10.1111/j.1471-4159.2004.02764.x. J Neurochem. 2004. PMID: 15584902 Free article.
Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.
Chappell MD, Li R, Smith SC, Dressman BA, Tromiczak EG, Tripp AE, Blanco MJ, Vetman T, Quimby SJ, Matt J, Britton TC, Fivush AM, Schkeryantz JM, Mayhugh D, Erickson JA, Bures MG, Jaramillo C, Carpintero M, Diego JE, Barberis M, Garcia-Cerrada S, Soriano JF, Antonysamy S, Atwell S, MacEwan I, Condon B, Sougias C, Wang J, Zhang A, Conners K, Groshong C, Wasserman SR, Koss JW, Witkin JM, Li X, Overshiner C, Wafford KA, Seidel W, Wang XS, Heinz BA, Swanson S, Catlow JT, Bedwell DW, Monn JA, Mitch CH, Ornstein PL. Chappell MD, et al. Among authors: erickson ja. J Med Chem. 2016 Dec 22;59(24):10974-10993. doi: 10.1021/acs.jmedchem.6b01119. Epub 2016 Dec 6. J Med Chem. 2016. PMID: 28002967
101 results