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26 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: kolmodin k. 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: kolmodin k. 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: kolmodin k. 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: kolmodin k. 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.
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: kolmodin k. J Neurosci. 2013 Jun 12;33(24):10075-84. doi: 10.1523/JNEUROSCI.1165-13.2013. J Neurosci. 2013. PMID: 23761903 Free PMC article.
Toward β-Secretase-1 Inhibitors with Improved Isoform Selectivity.
Johansson P, Kaspersson K, Gurrell IK, Bäck E, Eketjäll S, Scott CW, Cebers G, Thorne P, McKenzie MJ, Beaton H, Davey P, Kolmodin K, Holenz J, Duggan ME, Budd Haeberlein S, Bürli RW. Johansson P, et al. Among authors: kolmodin k. J Med Chem. 2018 Apr 26;61(8):3491-3502. doi: 10.1021/acs.jmedchem.7b01716. Epub 2018 Apr 10. J Med Chem. 2018. PMID: 29617572
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
Edwards PD, Albert JS, Sylvester M, Aharony D, Andisik D, Callaghan O, Campbell JB, Carr RA, Chessari G, Congreve M, Frederickson M, Folmer RH, Geschwindner S, Koether G, Kolmodin K, Krumrine J, Mauger RC, Murray CW, Olsson LL, Patel S, Spear N, Tian G. Edwards PD, et al. Among authors: kolmodin k. J Med Chem. 2007 Nov 29;50(24):5912-25. doi: 10.1021/jm070829p. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985862
Evidence for dimeric BACE-mediated APP processing.
Jin S, Agerman K, Kolmodin K, Gustafsson E, Dahlqvist C, Jureus A, Liu G, Fälting J, Berg S, Lundkvist J, Lendahl U. Jin S, et al. Among authors: kolmodin k. Biochem Biophys Res Commun. 2010 Feb 26;393(1):21-7. doi: 10.1016/j.bbrc.2010.01.064. Epub 2010 Jan 25. Biochem Biophys Res Commun. 2010. PMID: 20097169
Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.
Besidski Y, Brown W, Bylund J, Dabrowski M, Dautrey S, Harter M, Horoszok L, Hu Y, Johnson D, Johnstone S, Jones P, Leclerc S, Kolmodin K, Kers I, Labarre M, Labrecque D, Laird J, Lundström T, Martino J, Maudet M, Munro A, Nylöf M, Penwell A, Rotticci D, Slaitas A, Sundgren-Andersson A, Svensson M, Terp G, Villanueva H, Walpole C, Zemribo R, Griffin AM. Besidski Y, et al. Among authors: kolmodin k. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6205-11. doi: 10.1016/j.bmcl.2012.08.018. Epub 2012 Aug 14. Bioorg Med Chem Lett. 2012. PMID: 22939234
26 results