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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: johansson p. J Med Chem. 2012 Nov 8;55(21):9297-311. doi: 10.1021/jm300991n. Epub 2012 Oct 3. J Med Chem. 2012. PMID: 23017051
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: johansson p, johansson a. J Med Chem. 2013 Jun 13;56(11):4181-205. doi: 10.1021/jm3011349. Epub 2013 May 20. J Med Chem. 2013. PMID: 23126626
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. 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
Importance of Binding Site Hydration and Flexibility Revealed When Optimizing a Macrocyclic Inhibitor of the Keap1-Nrf2 Protein-Protein Interaction.
Begnini F, Geschwindner S, Johansson P, Wissler L, Lewis RJ, Danelius E, Luttens A, Matricon P, Carlsson J, Lenders S, König B, Friedel A, Sjö P, Schiesser S, Kihlberg J. Begnini F, et al. Among authors: johansson p. J Med Chem. 2022 Feb 24;65(4):3473-3517. doi: 10.1021/acs.jmedchem.1c01975. Epub 2022 Feb 2. J Med Chem. 2022. PMID: 35108001 Free PMC article.
Mining Natural Products for Macrocycles to Drug Difficult Targets.
Begnini F, Poongavanam V, Over B, Castaldo M, Geschwindner S, Johansson P, Tyagi M, Tyrchan C, Wissler L, Sjö P, Schiesser S, Kihlberg J. Begnini F, et al. Among authors: johansson p. J Med Chem. 2021 Jan 28;64(2):1054-1072. doi: 10.1021/acs.jmedchem.0c01569. Epub 2020 Dec 18. J Med Chem. 2021. PMID: 33337880 Free PMC article.
1,574 results