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Page 1
The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease.
Neumann U, Ufer M, Jacobson LH, Rouzade-Dominguez ML, Huledal G, Kolly C, Lüönd RM, Machauer R, Veenstra SJ, Hurth K, Rueeger H, Tintelnot-Blomley M, Staufenbiel M, Shimshek DR, Perrot L, Frieauff W, Dubost V, Schiller H, Vogg B, Beltz K, Avrameas A, Kretz S, Pezous N, Rondeau JM, Beckmann N, Hartmann A, Vormfelde S, David OJ, Galli B, Ramos R, Graf A, Lopez Lopez C. Neumann U, et al. Among authors: jacobson lh. EMBO Mol Med. 2018 Nov;10(11):e9316. doi: 10.15252/emmm.201809316. EMBO Mol Med. 2018. PMID: 30224383 Free PMC article. Clinical Trial.
Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.
Veenstra SJ, Rueeger H, Voegtle M, Lueoend R, Holzer P, Hurth K, Tintelnot-Blomley M, Frederiksen M, Rondeau JM, Jacobson L, Staufenbiel M, Neumann U, Machauer R. Veenstra SJ, et al. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2195-2200. doi: 10.1016/j.bmcl.2018.05.003. Epub 2018 May 3. Bioorg Med Chem Lett. 2018. PMID: 29764741
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: jacobson lh. Mol Neurodegener. 2015 Sep 3;10:44. doi: 10.1186/s13024-015-0033-8. Mol Neurodegener. 2015. PMID: 26336937 Free PMC article.
Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.
Machauer R, Lueoend R, Hurth K, Veenstra SJ, Rueeger H, Voegtle M, Tintelnot-Blomley M, Rondeau JM, Jacobson LH, Laue G, Beltz K, Neumann U. Machauer R, et al. Among authors: jacobson lh. J Med Chem. 2021 Oct 28;64(20):15262-15279. doi: 10.1021/acs.jmedchem.1c01300. Epub 2021 Oct 14. J Med Chem. 2021. PMID: 34648711
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: jacobson lh. 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
Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice.
Shimshek DR, Jacobson LH, Kolly C, Zamurovic N, Balavenkatraman KK, Morawiec L, Kreutzer R, Schelle J, Jucker M, Bertschi B, Theil D, Heier A, Bigot K, Beltz K, Machauer R, Brzak I, Perrot L, Neumann U. Shimshek DR, et al. Among authors: jacobson lh. Sci Rep. 2016 Feb 25;6:21917. doi: 10.1038/srep21917. Sci Rep. 2016. PMID: 26912421 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: jacobson lh. 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.
The second-generation active Aβ immunotherapy CAD106 reduces amyloid accumulation in APP transgenic mice while minimizing potential side effects.
Wiessner C, Wiederhold KH, Tissot AC, Frey P, Danner S, Jacobson LH, Jennings GT, Lüönd R, Ortmann R, Reichwald J, Zurini M, Mir A, Bachmann MF, Staufenbiel M. Wiessner C, et al. Among authors: jacobson lh. J Neurosci. 2011 Jun 22;31(25):9323-31. doi: 10.1523/JNEUROSCI.0293-11.2011. J Neurosci. 2011. PMID: 21697382 Free PMC article.
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: jacobson lh. 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
74 results