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Page 1
β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.
Hilpert H, Guba W, Woltering TJ, Wostl W, Pinard E, Mauser H, Mayweg AV, Rogers-Evans M, Humm R, Krummenacher D, Muser T, Schnider C, Jacobsen H, Ozmen L, Bergadano A, Banner DW, Hochstrasser R, Kuglstatter A, David-Pierson P, Fischer H, Polara A, Narquizian R. Hilpert H, et al. Among authors: kuglstatter a. J Med Chem. 2013 May 23;56(10):3980-95. doi: 10.1021/jm400225m. Epub 2013 May 2. J Med Chem. 2013. PMID: 23590342
Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
Martin RE, Aebi JD, Hornsperger B, Krebs HJ, Kuhn B, Kuglstatter A, Alker AM, Märki HP, Müller S, Burger D, Ottaviani G, Riboulet W, Verry P, Tan X, Amrein K, Mayweg AV. Martin RE, et al. Among authors: kuglstatter a. J Med Chem. 2015 Oct 22;58(20):8054-65. doi: 10.1021/acs.jmedchem.5b00851. Epub 2015 Oct 2. J Med Chem. 2015. PMID: 26403853
A Real-World Perspective on Molecular Design.
Kuhn B, Guba W, Hert J, Banner D, Bissantz C, Ceccarelli S, Haap W, Körner M, Kuglstatter A, Lerner C, Mattei P, Neidhart W, Pinard E, Rudolph MG, Schulz-Gasch T, Woltering T, Stahl M. Kuhn B, et al. Among authors: kuglstatter a. J Med Chem. 2016 May 12;59(9):4087-102. doi: 10.1021/acs.jmedchem.5b01875. Epub 2016 Feb 24. J Med Chem. 2016. PMID: 26878596
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. Among authors: kuglstatter a. 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
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. Among authors: kuglstatter a. 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
Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.
Liu Y, Wu J, Zhou M, Chen W, Li D, Wang Z, Hornsperger B, Aebi JD, Märki HP, Kuhn B, Wang L, Kuglstatter A, Benz J, Müller S, Hochstrasser R, Ottaviani G, Xin J, Kirchner S, Mohr S, Verry P, Riboulet W, Shen HC, Mayweg AV, Amrein K, Tan X. Liu Y, et al. Among authors: kuglstatter a. J Med Chem. 2020 Jul 9;63(13):6876-6897. doi: 10.1021/acs.jmedchem.0c00233. Epub 2020 Jun 25. J Med Chem. 2020. PMID: 32530624
Potent and Selective BACE-1 Peptide Inhibitors Lower Brain Aβ Levels Mediated by Brain Shuttle Transport.
Ruderisch N, Schlatter D, Kuglstatter A, Guba W, Huber S, Cusulin C, Benz J, Rufer AC, Hoernschemeyer J, Schweitzer C, Bülau T, Gärtner A, Hoffmann E, Niewoehner J, Patsch C, Baumann K, Loetscher H, Kitas E, Freskgård PO. Ruderisch N, et al. Among authors: kuglstatter a. EBioMedicine. 2017 Oct;24:76-92. doi: 10.1016/j.ebiom.2017.09.004. Epub 2017 Sep 7. EBioMedicine. 2017. PMID: 28923680 Free PMC article.
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
Padilla F, Bhagirath N, Chen S, Chiao E, Goldstein DM, Hermann JC, Hsu J, Kennedy-Smith JJ, Kuglstatter A, Liao C, Liu W, Lowrie LE Jr, Luk KC, Lynch SM, Menke J, Niu L, Owens TD, O-Yang C, Railkar A, Schoenfeld RC, Slade M, Steiner S, Tan YC, Villaseñor AG, Wang C, Wanner J, Xie W, Xu D, Zhang X, Zhou M, Lucas MC. Padilla F, et al. Among authors: kuglstatter a. J Med Chem. 2013 Feb 28;56(4):1677-92. doi: 10.1021/jm301720p. Epub 2013 Feb 12. J Med Chem. 2013. PMID: 23350847
53 results