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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 wel t. 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.
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
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.
Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons.
Baggelaar MP, Chameau PJ, Kantae V, Hummel J, Hsu KL, Janssen F, van der Wel T, Soethoudt M, Deng H, den Dulk H, Allarà M, Florea BI, Di Marzo V, Wadman WJ, Kruse CG, Overkleeft HS, Hankemeier T, Werkman TR, Cravatt BF, van der Stelt M. Baggelaar MP, et al. Among authors: van der stelt m, van der wel t. J Am Chem Soc. 2015 Jul 15;137(27):8851-7. doi: 10.1021/jacs.5b04883. Epub 2015 Jul 1. J Am Chem Soc. 2015. PMID: 26083464 Free PMC article.
Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-α and ABHD6 inhibitors.
Deng H, van der Wel T, van den Berg RJBHN, van den Nieuwendijk AMCH, Janssen FJ, Baggelaar MP, Overkleeft HS, van der Stelt M. Deng H, et al. Among authors: van der stelt m, van der wel t, van den berg rjbhn, van den nieuwendijk amch. Medchemcomm. 2017 Mar 10;8(5):982-988. doi: 10.1039/c7md00029d. eCollection 2017 May 1. Medchemcomm. 2017. PMID: 30108813 Free PMC article.
Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition.
Ogasawara D, Deng H, Viader A, Baggelaar MP, Breman A, den Dulk H, van den Nieuwendijk AM, Soethoudt M, van der Wel T, Zhou J, Overkleeft HS, Sanchez-Alavez M, Mori S, Nguyen W, Conti B, Liu X, Chen Y, Liu QS, Cravatt BF, van der Stelt M. Ogasawara D, et al. Among authors: van der stelt m, van der wel t, van den nieuwendijk am. Proc Natl Acad Sci U S A. 2016 Jan 5;113(1):26-33. doi: 10.1073/pnas.1522364112. Epub 2015 Dec 14. Proc Natl Acad Sci U S A. 2016. PMID: 26668358 Free PMC article.
Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474.
van Esbroeck ACM, Janssen APA, Cognetta AB 3rd, Ogasawara D, Shpak G, van der Kroeg M, Kantae V, Baggelaar MP, de Vrij FMS, Deng H, Allarà M, Fezza F, Lin Z, van der Wel T, Soethoudt M, Mock ED, den Dulk H, Baak IL, Florea BI, Hendriks G, De Petrocellis L, Overkleeft HS, Hankemeier T, De Zeeuw CI, Di Marzo V, Maccarrone M, Cravatt BF, Kushner SA, van der Stelt M. van Esbroeck ACM, et al. Among authors: van der kroeg m, van der stelt m, van der wel t. Science. 2017 Jun 9;356(6342):1084-1087. doi: 10.1126/science.aaf7497. Science. 2017. PMID: 28596366 Free PMC article.
25 results