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Page 1
Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.
Taoka BM, Wu WL, Hao J, Dolmaski M, Wang H, Levorse D, Orth P, Hyde LA, Smith B, Michener MS, Kennedy ME, Parker EM, Cumming JN. Taoka BM, et al. Among authors: michener ms. Bioorg Med Chem Lett. 2022 Jan 15;56:128463. doi: 10.1016/j.bmcl.2021.128463. Epub 2021 Nov 24. Bioorg Med Chem Lett. 2022. PMID: 34838652
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.
Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW. Mandal M, et al. Among authors: michener ms. J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 26937601
CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition.
Dobrowolska JA, Michener MS, Wu G, Patterson BW, Chott R, Ovod V, Pyatkivskyy Y, Wildsmith KR, Kasten T, Mathers P, Dancho M, Lennox C, Smith BE, Gilberto D, McLoughlin D, Holder DJ, Stamford AW, Yarasheski KE, Kennedy ME, Savage MJ, Bateman RJ. Dobrowolska JA, et al. Among authors: michener ms. J Neurosci. 2014 Jun 11;34(24):8336-46. doi: 10.1523/JNEUROSCI.0540-14.2014. J Neurosci. 2014. PMID: 24920637 Free PMC article.
Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.
Zhu H, Young MB, Nantermet PG, Graham SL, Colussi D, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Shi XP, Tugusheva K, Holahan MA, Michener MS, Cook JJ, Simon A, Hazuda DJ, Vacca JP, Rajapakse HA. Zhu H, et al. Among authors: michener ms. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1779-82. doi: 10.1016/j.bmcl.2010.01.005. Epub 2010 Jan 11. Bioorg Med Chem Lett. 2010. PMID: 20122828
Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys.
Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Hayashi I, Hughes BL, Moxham CM, Bays NW, Smotrov N, Hill AD, Pan BS, Wu Z, Moy LY, Tanga F, Kenific C, Cruz JC, Walker D, Bouthillette M, Nikov GN, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Michener MS, Cook JJ, Munoz B, Shearman MS. Fischer C, et al. Among authors: michener ms. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3488-94. doi: 10.1016/j.bmcl.2015.07.003. Epub 2015 Jul 9. Bioorg Med Chem Lett. 2015. PMID: 26212776
Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing.
Nantermet PG, Rajapakse HA, Stanton MG, Stauffer SR, Barrow JC, Gregro AR, Moore KP, Steinbeiser MA, Swestock J, Selnick HG, Graham SL, McGaughey GB, Colussi D, Lai MT, Sankaranarayanan S, Simon AJ, Munshi S, Cook JJ, Holahan MA, Michener MS, Vacca JP. Nantermet PG, et al. Among authors: michener ms. ChemMedChem. 2009 Jan;4(1):37-40. doi: 10.1002/cmdc.200800308. ChemMedChem. 2009. PMID: 19085994 No abstract available.
Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound.
Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, Wang JX, Wu G, Yarasheski KE, Bateman RJ. Cook JJ, et al. Among authors: michener ms. J Neurosci. 2010 May 12;30(19):6743-50. doi: 10.1523/JNEUROSCI.1381-10.2010. J Neurosci. 2010. PMID: 20463236 Free PMC article.
16 results