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Mapping the conformational space accessible to BACE2 using surface mutants and cocrystals with Fab fragments, Fynomers and Xaperones.
Banner DW, Gsell B, Benz J, Bertschinger J, Burger D, Brack S, Cuppuleri S, Debulpaep M, Gast A, Grabulovski D, Hennig M, Hilpert H, Huber W, Kuglstatter A, Kusznir E, Laeremans T, Matile H, Miscenic C, Rufer AC, Schlatter D, Steyaert J, Stihle M, Thoma R, Weber M, Ruf A. Banner DW, et al. Acta Crystallogr D Biol Crystallogr. 2013 Jun;69(Pt 6):1124-37. doi: 10.1107/S0907444913006574. Epub 2013 May 15. Acta Crystallogr D Biol Crystallogr. 2013. PMID: 23695257
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.
Zbinden KG, Anselm L, Banner DW, Benz J, Blasco F, Décoret G, Himber J, Kuhn B, Panday N, Ricklin F, Risch P, Schlatter D, Stahl M, Thomi S, Unger R, Haap W. Zbinden KG, et al. Among authors: banner dw. Eur J Med Chem. 2009 Jul;44(7):2787-95. doi: 10.1016/j.ejmech.2008.12.025. Epub 2009 Jan 3. Eur J Med Chem. 2009. PMID: 19200624
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.
Anselm L, Banner DW, Benz J, Zbinden KG, Himber J, Hilpert H, Huber W, Kuhn B, Mary JL, Otteneder MB, Panday N, Ricklin F, Stahl M, Thomi S, Haap W. Anselm L, et al. Among authors: banner dw. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5313-9. doi: 10.1016/j.bmcl.2010.06.126. Epub 2010 Jul 1. Bioorg Med Chem Lett. 2010. PMID: 20650636
BACE1 inhibitors: a head group scan on a series of amides.
Woltering TJ, Wostl W, Hilpert H, Rogers-Evans M, Pinard E, Mayweg A, Göbel M, Banner DW, Benz J, Travagli M, Pollastrini M, Marconi G, Gabellieri E, Guba W, Mauser H, Andreini M, Jacobsen H, Power E, Narquizian R. Woltering TJ, et al. Among authors: banner dw. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4239-43. doi: 10.1016/j.bmcl.2013.05.003. Epub 2013 May 18. Bioorg Med Chem Lett. 2013. PMID: 23735744
Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.
Giroud M, Dietzel U, Anselm L, Banner D, Kuglstatter A, Benz J, Blanc JB, Gaufreteau D, Liu H, Lin X, Stich A, Kuhn B, Schuler F, Kaiser M, Brun R, Schirmeister T, Kisker C, Diederich F, Haap W. Giroud M, et al. J Med Chem. 2018 Apr 26;61(8):3350-3369. doi: 10.1021/acs.jmedchem.7b01869. Epub 2018 Apr 13. J Med Chem. 2018. PMID: 29590750
67 results