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Page 1
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.
Incorporation of non-natural amino acids improves cell permeability and potency of specific inhibitors of proteasome trypsin-like sites.
Geurink PP, van der Linden WA, Mirabella AC, Gallastegui N, de Bruin G, Blom AE, Voges MJ, Mock ED, Florea BI, van der Marel GA, Driessen C, van der Stelt M, Groll M, Overkleeft HS, Kisselev AF. Geurink PP, et al. Among authors: van der stelt m, van der marel ga, van der linden wa. J Med Chem. 2013 Feb 14;56(3):1262-75. doi: 10.1021/jm3016987. Epub 2013 Jan 28. J Med Chem. 2013. PMID: 23320547 Free PMC article.
Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-α in brain.
Baggelaar MP, Janssen FJ, van Esbroeck AC, den Dulk H, Allarà M, Hoogendoorn S, McGuire R, Florea BI, Meeuwenoord N, van den Elst H, van der Marel GA, Brouwer J, Di Marzo V, Overkleeft HS, van der Stelt M. Baggelaar MP, et al. Among authors: van der stelt m, van den elst h, van der marel ga, van esbroeck ac. Angew Chem Int Ed Engl. 2013 Nov 11;52(46):12081-5. doi: 10.1002/anie.201306295. Epub 2013 Oct 31. Angew Chem Int Ed Engl. 2013. PMID: 24173880 No abstract available.
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
Development of an acid ceramidase activity-based probe.
Ouairy CM, Ferraz MJ, Boot RG, Baggelaar MP, van der Stelt M, Appelman M, van der Marel GA, Florea BI, Aerts JM, Overkleeft HS. Ouairy CM, et al. Among authors: van der stelt m, van der marel ga. Chem Commun (Camb). 2015 Apr 11;51(28):6161-3. doi: 10.1039/c5cc00356c. Chem Commun (Camb). 2015. PMID: 25748248
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.
The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity.
Mukhopadhyay P, Baggelaar M, Erdelyi K, Cao Z, Cinar R, Fezza F, Ignatowska-Janlowska B, Wilkerson J, van Gils N, Hansen T, Ruben M, Soethoudt M, Heitman L, Kunos G, Maccarrone M, Lichtman A, Pacher P, Van der Stelt M. Mukhopadhyay P, et al. Among authors: van der stelt m, van gils n. Br J Pharmacol. 2016 Feb;173(3):446-58. doi: 10.1111/bph.13338. Epub 2016 Jan 15. Br J Pharmacol. 2016. PMID: 26398481 Free PMC article.
A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities.
de Bruin G, Xin BT, Kraus M, van der Stelt M, van der Marel GA, Kisselev AF, Driessen C, Florea BI, Overkleeft HS. de Bruin G, et al. Among authors: van der stelt m, van der marel ga. Angew Chem Int Ed Engl. 2016 Mar 18;55(13):4199-203. doi: 10.1002/anie.201509092. Epub 2015 Oct 29. Angew Chem Int Ed Engl. 2016. PMID: 26511210
155 results