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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: wittwer mb. 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.
Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice.
Mock ED, Mustafa M, Gunduz-Cinar O, Cinar R, Petrie GN, Kantae V, Di X, Ogasawara D, Varga ZV, Paloczi J, Miliano C, Donvito G, van Esbroeck ACM, van der Gracht AMF, Kotsogianni I, Park JK, Martella A, van der Wel T, Soethoudt M, Jiang M, Wendel TJ, Janssen APA, Bakker AT, Donovan CM, Castillo LI, Florea BI, Wat J, van den Hurk H, Wittwer M, Grether U, Holmes A, van Boeckel CAA, Hankemeier T, Cravatt BF, Buczynski MW, Hill MN, Pacher P, Lichtman AH, van der Stelt M. Mock ED, et al. Nat Chem Biol. 2020 Jun;16(6):667-675. doi: 10.1038/s41589-020-0528-7. Epub 2020 May 11. Nat Chem Biol. 2020. PMID: 32393901 Free PMC article.
Discovery, synthesis and evaluation of novel reversible monoacylglycerol lipase radioligands bearing a morpholine-3-one scaffold.
He Y, Gobbi LC, Herde AM, Rombach D, Ritter M, Kuhn B, Wittwer MB, Heer D, Hornsperger B, Bell C, O'Hara F, Benz J, Honer M, Keller C, Collin L, Richter H, Schibli R, Grether U, Mu L. He Y, et al. Among authors: wittwer mb. Nucl Med Biol. 2022 May-Jun;108-109:24-32. doi: 10.1016/j.nucmedbio.2022.02.002. Epub 2022 Feb 23. Nucl Med Biol. 2022. PMID: 35248850 Free article.
A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence.
Jiang M, Huizenga MCW, Wirt JL, Paloczi J, Amedi A, van den Berg RJBHN, Benz J, Collin L, Deng H, Di X, Driever WF, Florea BI, Grether U, Janssen APA, Hankemeier T, Heitman LH, Lam TW, Mohr F, Pavlovic A, Ruf I, van den Hurk H, Stevens AF, van der Vliet D, van der Wel T, Wittwer MB, van Boeckel CAA, Pacher P, Hohmann AG, van der Stelt M. Jiang M, et al. Among authors: wittwer mb. Nat Commun. 2023 Dec 5;14(1):8039. doi: 10.1038/s41467-023-43606-3. Nat Commun. 2023. PMID: 38052772 Free PMC article.
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: wittwer mb. 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
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: wittwer mb. Chembiochem. 2024 Nov 28:e202400704. doi: 10.1002/cbic.202400704. Online ahead of print. Chembiochem. 2024. PMID: 39607084
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: wittwer mb. 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
83 results