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Page 1
Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360.
Rueeger H, Lueoend R, Machauer R, Veenstra SJ, Holzer P, Hurth K, Voegtle M, Frederiksen M, Rondeau JM, Tintelnot-Blomley M, Jacobson LH, Staufenbiel M, Laue G, Neumann U. Rueeger H, et al. Among authors: staufenbiel m. J Med Chem. 2021 Apr 22;64(8):4677-4696. doi: 10.1021/acs.jmedchem.0c02143. Epub 2021 Apr 12. J Med Chem. 2021. PMID: 33844524
Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition.
Abramowski D, Wiederhold KH, Furrer U, Jaton AL, Neuenschwander A, Runser MJ, Danner S, Reichwald J, Ammaturo D, Staab D, Stoeckli M, Rueeger H, Neumann U, Staufenbiel M. Abramowski D, et al. Among authors: staufenbiel m. J Pharmacol Exp Ther. 2008 Nov;327(2):411-24. doi: 10.1124/jpet.108.140327. Epub 2008 Aug 7. J Pharmacol Exp Ther. 2008. PMID: 18687920
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: staufenbiel m. 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
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: staufenbiel m. 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 of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides.
Rueeger H, Lueoend R, Rogel O, Rondeau JM, Möbitz H, Machauer R, Jacobson L, Staufenbiel M, Desrayaud S, Neumann U. Rueeger H, et al. Among authors: staufenbiel m. J Med Chem. 2012 Apr 12;55(7):3364-86. doi: 10.1021/jm300069y. Epub 2012 Mar 21. J Med Chem. 2012. PMID: 22380629
Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides.
Rueeger H, Lueoend R, Machauer R, Veenstra SJ, Jacobson LH, Staufenbiel M, Desrayaud S, Rondeau JM, Möbitz H, Neumann U. Rueeger H, et al. Among authors: staufenbiel m. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5300-6. doi: 10.1016/j.bmcl.2013.07.071. Epub 2013 Aug 9. Bioorg Med Chem Lett. 2013. PMID: 23981898
A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice.
Neumann U, Rueeger H, Machauer R, Veenstra SJ, Lueoend RM, Tintelnot-Blomley M, Laue G, Beltz K, Vogg B, Schmid P, Frieauff W, Shimshek DR, Staufenbiel M, Jacobson LH. Neumann U, et al. Among authors: staufenbiel m. Mol Neurodegener. 2015 Sep 3;10:44. doi: 10.1186/s13024-015-0033-8. Mol Neurodegener. 2015. PMID: 26336937 Free PMC article.
Longitudinal noninvasive magnetic resonance imaging of brain microhemorrhages in BACE inhibitor-treated APP transgenic mice.
Beckmann N, Doelemeyer A, Zurbruegg S, Bigot K, Theil D, Frieauff W, Kolly C, Moulin P, Neddermann D, Kreutzer R, Perrot L, Brzak I, Jacobson LH, Staufenbiel M, Neumann U, Shimshek DR. Beckmann N, et al. Among authors: staufenbiel m. Neurobiol Aging. 2016 Sep;45:50-60. doi: 10.1016/j.neurobiolaging.2016.05.009. Epub 2016 May 17. Neurobiol Aging. 2016. PMID: 27459925 Free article.
215 results