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23 results

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New aminoimidazoles as β-secretase (BACE-1) inhibitors showing amyloid-β (Aβ) lowering in brain.
Gravenfors Y, Viklund J, Blid J, Ginman T, Karlström S, Kihlström J, Kolmodin K, Lindström J, von Berg S, von Kieseritzky F, Bogar K, Slivo C, Swahn BM, Olsson LL, Johansson P, Eketjäll S, Fälting J, Jeppsson F, Strömberg K, Janson J, Rahm F. Gravenfors Y, et al. Among authors: falting j. J Med Chem. 2012 Nov 8;55(21):9297-311. doi: 10.1021/jm300991n. Epub 2012 Oct 3. J Med Chem. 2012. PMID: 23017051
Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy.
Swahn BM, Holenz J, Kihlström J, Kolmodin K, Lindström J, Plobeck N, Rotticci D, Sehgelmeble F, Sundström M, Berg Sv, Fälting J, Georgievska B, Gustavsson S, Neelissen J, Ek M, Olsson LL, Berg S. Swahn BM, et al. Among authors: falting j. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1854-9. doi: 10.1016/j.bmcl.2012.01.079. Epub 2012 Jan 28. Bioorg Med Chem Lett. 2012. PMID: 22325942
Design and synthesis of β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of β-amyloid peptides.
Swahn BM, Kolmodin K, Karlström S, von Berg S, Söderman P, Holenz J, Berg S, Lindström J, Sundström M, Turek D, Kihlström J, Slivo C, Andersson L, Pyring D, Rotticci D, Ohberg L, Kers A, Bogar K, von Kieseritzky F, Bergh M, Olsson LL, Janson J, Eketjäll S, Georgievska B, Jeppsson F, Fälting J. Swahn BM, et al. Among authors: falting j. J Med Chem. 2012 Nov 8;55(21):9346-61. doi: 10.1021/jm3009025. Epub 2012 Sep 17. J Med Chem. 2012. PMID: 22924815
Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease.
Jeppsson F, Eketjäll S, Janson J, Karlström S, Gustavsson S, Olsson LL, Radesäter AC, Ploeger B, Cebers G, Kolmodin K, Swahn BM, von Berg S, Bueters T, Fälting J. Jeppsson F, et al. Among authors: falting j. J Biol Chem. 2012 Nov 30;287(49):41245-57. doi: 10.1074/jbc.M112.409110. Epub 2012 Oct 9. J Biol Chem. 2012. PMID: 23048024 Free PMC article.
Core refinement toward permeable β-secretase (BACE-1) inhibitors with low hERG activity.
Ginman T, Viklund J, Malmström J, Blid J, Emond R, Forsblom R, Johansson A, Kers A, Lake F, Sehgelmeble F, Sterky KJ, Bergh M, Lindgren A, Johansson P, Jeppsson F, Fälting J, Gravenfors Y, Rahm F. Ginman T, et al. Among authors: falting j. J Med Chem. 2013 Jun 13;56(11):4181-205. doi: 10.1021/jm3011349. Epub 2013 May 20. J Med Chem. 2013. PMID: 23126626
AZ-4217: a high potency BACE inhibitor displaying acute central efficacy in different in vivo models and reduced amyloid deposition in Tg2576 mice.
Eketjäll S, Janson J, Jeppsson F, Svanhagen A, Kolmodin K, Gustavsson S, Radesäter AC, Eliason K, Briem S, Appelkvist P, Niva C, Berg AL, Karlström S, Swahn BM, Fälting J. Eketjäll S, et al. Among authors: falting j. J Neurosci. 2013 Jun 12;33(24):10075-84. doi: 10.1523/JNEUROSCI.1165-13.2013. J Neurosci. 2013. PMID: 23761903 Free PMC article.
Combining an amyloid-beta (Aβ) cleaving enzyme inhibitor with a γ-secretase modulator results in an additive reduction of Aβ production.
Strömberg K, Eketjäll S, Georgievska B, Tunblad K, Eliason K, Olsson F, Radesäter AC, Klintenberg R, Arvidsson PI, von Berg S, Fälting J, Cowburn RF, Dabrowski M. Strömberg K, et al. Among authors: falting j. FEBS J. 2015 Jan;282(1):65-73. doi: 10.1111/febs.13103. Epub 2014 Nov 7. FEBS J. 2015. PMID: 25303711 Free article.
Revisiting the peripheral sink hypothesis: inhibiting BACE1 activity in the periphery does not alter β-amyloid levels in the CNS.
Georgievska B, Gustavsson S, Lundkvist J, Neelissen J, Eketjäll S, Ramberg V, Bueters T, Agerman K, Juréus A, Svensson S, Berg S, Fälting J, Lendahl U. Georgievska B, et al. Among authors: falting j. J Neurochem. 2015 Feb;132(4):477-86. doi: 10.1111/jnc.12937. Epub 2014 Sep 18. J Neurochem. 2015. PMID: 25156639 Free article.
23 results