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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: van der stelt m. 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.
Structural basis of selective cannabinoid CB2 receptor activation.
Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T. Li X, et al. Among authors: van der stelt m, van den berg rjbhn, van der horst c. Nat Commun. 2023 Mar 15;14(1):1447. doi: 10.1038/s41467-023-37112-9. Nat Commun. 2023. PMID: 36922494 Free PMC article.
Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6.
Janssen FJ, Deng H, Baggelaar MP, Allarà M, van der Wel T, den Dulk H, Ligresti A, van Esbroeck AC, McGuire R, Di Marzo V, Overkleeft HS, van der Stelt M. Janssen FJ, et al. Among authors: van der stelt m, van der wel t, van esbroeck ac. J Med Chem. 2014 Aug 14;57(15):6610-22. doi: 10.1021/jm500681z. Epub 2014 Jul 23. J Med Chem. 2014. PMID: 24988361
Structure Kinetics Relationships and Molecular Dynamics Show Crucial Role for Heterocycle Leaving Group in Irreversible Diacylglycerol Lipase Inhibitors.
Janssen APA, van Hengst JMA, Béquignon OJM, Deng H, van Westen GJP, van der Stelt M. Janssen APA, et al. Among authors: van der stelt m, van westen gjp, van hengst jma. J Med Chem. 2019 Sep 12;62(17):7910-7922. doi: 10.1021/acs.jmedchem.9b00686. Epub 2019 Aug 30. J Med Chem. 2019. PMID: 31437392 Free PMC article.
Identification of α,β-Hydrolase Domain Containing Protein 6 as a Diacylglycerol Lipase in Neuro-2a Cells.
van Esbroeck ACM, Kantae V, Di X, van der Wel T, den Dulk H, Stevens AF, Singh S, Bakker AT, Florea BI, Stella N, Overkleeft HS, Hankemeier T, van der Stelt M. van Esbroeck ACM, et al. Among authors: van der stelt m, van der wel t. Front Mol Neurosci. 2019 Nov 26;12:286. doi: 10.3389/fnmol.2019.00286. eCollection 2019. Front Mol Neurosci. 2019. PMID: 31849602 Free PMC 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. Among authors: van der stelt m, van der wel t, van boeckel caa, van esbroeck acm, van der gracht amf, van den hurk h. 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.
Structure-Activity Relationship Studies of α-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family.
Zhou J, Mock ED, Al Ayed K, Di X, Kantae V, Burggraaff L, Stevens AF, Martella A, Mohr F, Jiang M, van der Wel T, Wendel TJ, Ofman TP, Tran Y, de Koster N, van Westen GJP, Hankemeier T, van der Stelt M. Zhou J, et al. Among authors: van der stelt m, van der wel t, van westen gjp. J Med Chem. 2020 Sep 10;63(17):9340-9359. doi: 10.1021/acs.jmedchem.0c00522. Epub 2020 Aug 13. J Med Chem. 2020. PMID: 32787138 Free PMC article.
163 results