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Chemical Proteomics Reveals Off-Targets of the Anandamide Reuptake Inhibitor WOBE437.
Gagestein B, Stevens AF, Fazio D, Florea BI, van der Wel T, Bakker AT, Fezza F, Dulk HD, Overkleeft HS, Maccarrone M, van der Stelt M. Gagestein B, et al. Among authors: stevens af. ACS Chem Biol. 2022 May 20;17(5):1174-1183. doi: 10.1021/acschembio.2c00122. Epub 2022 Apr 28. ACS Chem Biol. 2022. PMID: 35482948 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: stevens af. 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.
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: stevens af. 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.
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: stevens af. Nat Commun. 2023 Dec 5;14(1):8039. doi: 10.1038/s41467-023-43606-3. Nat Commun. 2023. PMID: 38052772 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: stevens af. 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.
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: stevens af. 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
16 results