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Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.
Lerchner A, Machauer R, Betschart C, Veenstra S, Rueeger H, McCarthy C, Tintelnot-Blomley M, Jaton AL, Rabe S, Desrayaud S, Enz A, Staufenbiel M, Paganetti P, Rondeau JM, Neumann U. Lerchner A, et al. Among authors: paganetti p. Bioorg Med Chem Lett. 2010 Jan 15;20(2):603-7. doi: 10.1016/j.bmcl.2009.11.092. Epub 2009 Nov 22. Bioorg Med Chem Lett. 2010. PMID: 19963375
Discovery and structure activity relationship of small molecule inhibitors of toxic β-amyloid-42 fibril formation.
Kroth H, Ansaloni A, Varisco Y, Jan A, Sreenivasachary N, Rezaei-Ghaleh N, Giriens V, Lohmann S, López-Deber MP, Adolfsson O, Pihlgren M, Paganetti P, Froestl W, Nagel-Steger L, Willbold D, Schrader T, Zweckstetter M, Pfeifer A, Lashuel HA, Muhs A. Kroth H, et al. Among authors: paganetti p. J Biol Chem. 2012 Oct 5;287(41):34786-800. doi: 10.1074/jbc.M112.357665. Epub 2012 Aug 13. J Biol Chem. 2012. PMID: 22891248 Free PMC article.
Increased efflux of amyloid-β peptides through the blood-brain barrier by muscarinic acetylcholine receptor inhibition reduces pathological phenotypes in mouse models of brain amyloidosis.
Paganetti P, Antoniello K, Devraj K, Toni N, Kieran D, Madani R, Pihlgren M, Adolfsson O, Froestl W, Schrattenholz A, Liebner S, Havas D, Windisch M, Cirrito JR, Pfeifer A, Muhs A. Paganetti P, et al. J Alzheimers Dis. 2014;38(4):767-86. doi: 10.3233/JAD-131091. J Alzheimers Dis. 2014. PMID: 24072071
BACE-1 is expressed in the blood-brain barrier endothelium and is upregulated in a murine model of Alzheimer's disease.
Devraj K, Poznanovic S, Spahn C, Schwall G, Harter PN, Mittelbronn M, Antoniello K, Paganetti P, Muhs A, Heilemann M, Hawkins RA, Schrattenholz A, Liebner S. Devraj K, et al. Among authors: paganetti p. J Cereb Blood Flow Metab. 2016 Jul;36(7):1281-94. doi: 10.1177/0271678X15606463. Epub 2015 Oct 13. J Cereb Blood Flow Metab. 2016. PMID: 26661166 Free PMC article.
Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.
Hanessian S, Yun H, Hou Y, Yang G, Bayrakdarian M, Therrien E, Moitessier N, Roggo S, Veenstra S, Tintelnot-Blomley M, Rondeau JM, Ostermeier C, Strauss A, Ramage P, Paganetti P, Neumann U, Betschart C. Hanessian S, et al. Among authors: paganetti p. J Med Chem. 2005 Aug 11;48(16):5175-90. doi: 10.1021/jm050142+. J Med Chem. 2005. PMID: 16078837
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.
Machauer R, Laumen K, Veenstra S, Rondeau JM, Tintelnot-Blomley M, Betschart C, Jaton AL, Desrayaud S, Staufenbiel M, Rabe S, Paganetti P, Neumann U. Machauer R, et al. Among authors: paganetti p. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1366-70. doi: 10.1016/j.bmcl.2009.01.055. Epub 2009 Jan 22. Bioorg Med Chem Lett. 2009. PMID: 19195887
93 results