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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: van der stelt m. Nat Commun. 2023 Dec 5;14(1):8039. doi: 10.1038/s41467-023-43606-3. Nat Commun. 2023. PMID: 38052772 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.
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.
Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.
Soethoudt M, Grether U, Fingerle J, Grim TW, Fezza F, de Petrocellis L, Ullmer C, Rothenhäusler B, Perret C, van Gils N, Finlay D, MacDonald C, Chicca A, Gens MD, Stuart J, de Vries H, Mastrangelo N, Xia L, Alachouzos G, Baggelaar MP, Martella A, Mock ED, Deng H, Heitman LH, Connor M, Di Marzo V, Gertsch J, Lichtman AH, Maccarrone M, Pacher P, Glass M, van der Stelt M. Soethoudt M, et al. Among authors: van der stelt m, van gils n. Nat Commun. 2017 Jan 3;8:13958. doi: 10.1038/ncomms13958. Nat Commun. 2017. PMID: 28045021 Free PMC article.
Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis.
van der Wel T, Hilhorst R, den Dulk H, van den Hooven T, Prins NM, Wijnakker JAPM, Florea BI, Lenselink EB, van Westen GJP, Ruijtenbeek R, Overkleeft HS, Kaptein A, Barf T, van der Stelt M. van der Wel T, et al. Among authors: van der stelt m, van westen gjp, van den hooven t. Nat Commun. 2020 Jun 25;11(1):3216. doi: 10.1038/s41467-020-17027-5. Nat Commun. 2020. PMID: 32587248 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: 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.
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
155 results