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Page 1
Development of a Highly Selective NanoBRET Probe to Assess MAGL Inhibition in Live Cells.
Gazzi T, Brennecke B, Olikauskas V, Hochstrasser R, Wang H, Keen Chao S, Atz K, Mostinski Y, Topp A, Heer D, Kaufmann I, Ritter M, Gobbi L, Hornsperger B, Wagner B, Richter H, O'Hara F, Wittwer MB, Jul Hansen D, Collin L, Kuhn B, Benz J, Grether U, Nazaré M. Gazzi T, et al. Among authors: heer d. Chembiochem. 2024 Nov 28:e202400704. doi: 10.1002/cbic.202400704. Online ahead of print. Chembiochem. 2024. PMID: 39607084
Discovery of Orally Available and Brain Penetrant AEP Inhibitors.
Krummenacher D, He W, Kuhn B, Schnider C, Beurier A, Brom V, Sivasothy T, Marty C, Tosstorff A, Hewings DS, Mesch S, Pinard E, Brändlin M, Hochstrasser R, Westwood P, Rothe J, Kronenberger A, Morandi F, Gutbier S, Schuler A, Heer D, Gloria LE, Joedicke L, Rudolph MG, Müller L, Grüninger F, Baumann K, Kaniyappan S, Manevski N, Bartels B. Krummenacher D, et al. Among authors: heer d. J Med Chem. 2023 Dec 28;66(24):17026-17043. doi: 10.1021/acs.jmedchem.3c01804. Epub 2023 Dec 13. J Med Chem. 2023. PMID: 38090813
Identification of (R)-[18F]YH134 for Monoacylglycerol Lipase Neuroimaging and Exploration of Its Use for Central Nervous System and Peripheral Drug Development.
He Y, Krämer SD, Grether U, Wittwer MB, Collin L, Kuhn B, Topp A, Heer D, O'Hara F, Honer M, Pavlovic A, Richter H, Ritter M, Rombach D, Keller C, Gobbi L, Mu L. He Y, et al. Among authors: heer d. J Nucl Med. 2024 Feb 1;65(2):300-305. doi: 10.2967/jnumed.123.266426. J Nucl Med. 2024. PMID: 38164615
Development of Potent and Selective Monoacylglycerol Lipase Inhibitors. SARs, Structural Analysis, and Biological Characterization.
Butini S, Grether U, Jung KM, Ligresti A, Allarà M, Postmus AGJ, Maramai S, Brogi S, Papa A, Carullo G, Sykes D, Veprintsev D, Federico S, Grillo A, Di Guglielmo B, Ramunno A, Stevens AF, Heer D, Lamponi S, Gemma S, Benz J, Di Marzo V, van der Stelt M, Piomelli D, Campiani G. Butini S, et al. Among authors: heer d. J Med Chem. 2024 Feb 8;67(3):1758-1782. doi: 10.1021/acs.jmedchem.3c01278. Epub 2024 Jan 19. J Med Chem. 2024. PMID: 38241614
Structure-Guided Discovery of cis-Hexahydro-pyrido-oxazinones as Reversible, Drug-like Monoacylglycerol Lipase Inhibitors.
Kuhn B, Ritter M, Hornsperger B, Bell C, Kocer B, Rombach D, Lutz MDR, Gobbi L, Kuratli M, Bartelmus C, Bürkler M, Koller R, Tosatti P, Ruf I, Guerard M, Pavlovic A, Stephanus J, O'Hara F, Wetzl D, Saal W, Stihle M, Roth D, Hug M, Huber S, Heer D, Kroll C, Topp A, Schneider M, Gertsch J, Glasmacher S, van der Stelt M, Martella A, Wittwer MB, Collin L, Benz J, Richter H, Grether U. Kuhn B, et al. Among authors: heer d. J Med Chem. 2024 Oct 24;67(20):18448-18464. doi: 10.1021/acs.jmedchem.4c01769. Epub 2024 Oct 3. J Med Chem. 2024. PMID: 39360636
Exploration of (R)-[11C]YH168 as a PET tracer for imaging monoacylglycerol lipase in the brain: from mice to non-human primates.
He Y, Zheng M, Gu J, Reichert L, Trimborn J, Zhang H, Keller C, Crosby M, Collin L, Heer D, Pavlovic A, Topp A, Wittwer MB, Grether U, Gobbi L, Schibli R, Huang Y, Mu L. He Y, et al. Among authors: heer d. Eur J Nucl Med Mol Imaging. 2024 Dec 14. doi: 10.1007/s00259-024-07013-0. Online ahead of print. Eur J Nucl Med Mol Imaging. 2024. PMID: 39673602
Targeting neuronal lysosomal dysfunction caused by β-glucocerebrosidase deficiency with an enzyme-based brain shuttle construct.
Gehrlein A, Udayar V, Anastasi N, Morella ML, Ruf I, Brugger D, von der Mark S, Thoma R, Rufer A, Heer D, Pfahler N, Jochner A, Niewoehner J, Wolf L, Fueth M, Ebeling M, Villaseñor R, Zhu Y, Deen MC, Shan X, Ehsaei Z, Taylor V, Sidransky E, Vocadlo DJ, Freskgård PO, Jagasia R. Gehrlein A, et al. Among authors: heer d. Nat Commun. 2023 Apr 12;14(1):2057. doi: 10.1038/s41467-023-37632-4. Nat Commun. 2023. PMID: 37045813 Free PMC article.
Multi-parameter optimization: Development of a morpholin-3-one derivative with an improved kinetic profile for imaging monoacylglycerol lipase in the brain.
He Y, Grether U, Taddio MF, Meier C, Keller C, Edelmann MR, Honer M, Huber S, Wittwer MB, Heer D, Richter H, Collin L, Hug MN, Hilbert M, Postmus AGJ, Stevens AF, van der Stelt M, Krämer SD, Schibli R, Mu L, Gobbi LC. He Y, et al. Among authors: heer d. Eur J Med Chem. 2022 Dec 5;243:114750. doi: 10.1016/j.ejmech.2022.114750. Epub 2022 Sep 9. Eur J Med Chem. 2022. PMID: 36137365 Free article.
44 results