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Dicer1-miR-328-Bace1 signalling controls brown adipose tissue differentiation and function.
Oliverio M, Schmidt E, Mauer J, Baitzel C, Hansmeier N, Khani S, Konieczka S, Pradas-Juni M, Brodesser S, Van TM, Bartsch D, Brönneke HS, Heine M, Hilpert H, Tarcitano E, Garinis GA, Frommolt P, Heeren J, Mori MA, Brüning JC, Kornfeld JW. Oliverio M, et al. Among authors: hilpert h. Nat Cell Biol. 2016 Mar;18(3):328-36. doi: 10.1038/ncb3316. Epub 2016 Feb 22. Nat Cell Biol. 2016. PMID: 26900752
Bace2 is a β cell-enriched protease that regulates pancreatic β cell function and mass.
Esterházy D, Stützer I, Wang H, Rechsteiner MP, Beauchamp J, Döbeli H, Hilpert H, Matile H, Prummer M, Schmidt A, Lieske N, Boehm B, Marselli L, Bosco D, Kerr-Conte J, Aebersold R, Spinas GA, Moch H, Migliorini C, Stoffel M. Esterházy D, et al. Among authors: hilpert h. Cell Metab. 2011 Sep 7;14(3):365-77. doi: 10.1016/j.cmet.2011.06.018. Cell Metab. 2011. PMID: 21907142 Free article.
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: hilpert h. 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
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: hilpert h. 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
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. 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 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: hilpert h. 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
32 results