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Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Ripa L, Edman K, Dearman M, Edenro G, Hendrickx R, Ullah V, Chang HF, Lepistö M, Chapman D, Geschwindner S, Wissler L, Svanberg P, Lawitz K, Malmberg J, Nikitidis A, Olsson RI, Bird J, Llinas A, Hegelund-Myrbäck T, Berger M, Thorne P, Harrison R, Köhler C, Drmota T. Ripa L, et al. Among authors: geschwindner s. J Med Chem. 2018 Mar 8;61(5):1785-1799. doi: 10.1021/acs.jmedchem.7b01690. Epub 2018 Feb 16. J Med Chem. 2018. PMID: 29424542
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: geschwindner s. J Med Chem. 2007 Nov 29;50(24):5912-25. doi: 10.1021/jm070829p. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985862
Ligand Binding Mechanism in Steroid Receptors: From Conserved Plasticity to Differential Evolutionary Constraints.
Edman K, Hosseini A, Bjursell MK, Aagaard A, Wissler L, Gunnarsson A, Kaminski T, Köhler C, Bäckström S, Jensen TJ, Cavallin A, Karlsson U, Nilsson E, Lecina D, Takahashi R, Grebner C, Geschwindner S, Lepistö M, Hogner AC, Guallar V. Edman K, et al. Among authors: geschwindner s. Structure. 2015 Dec 1;23(12):2280-2290. doi: 10.1016/j.str.2015.09.012. Epub 2015 Oct 22. Structure. 2015. PMID: 26602186 Free article.
Preclinical pharmacology of AZD9977: A novel mineralocorticoid receptor modulator separating organ protection from effects on electrolyte excretion.
Bamberg K, Johansson U, Edman K, William-Olsson L, Myhre S, Gunnarsson A, Geschwindner S, Aagaard A, Björnson Granqvist A, Jaisser F, Huang Y, Granberg KL, Jansson-Löfmark R, Hartleib-Geschwindner J. Bamberg K, et al. Among authors: geschwindner s. PLoS One. 2018 Feb 23;13(2):e0193380. doi: 10.1371/journal.pone.0193380. eCollection 2018. PLoS One. 2018. PMID: 29474466 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: geschwindner s. 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.
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: geschwindner s. 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.
47 results