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Page 1
A Fluorescence Polarization Activity-Based Protein Profiling Assay in the Discovery of Potent, Selective Inhibitors for Human Nonlysosomal Glucosylceramidase.
Lahav D, Liu B, van den Berg RJBHN, van den Nieuwendijk AMCH, Wennekes T, Ghisaidoobe AT, Breen I, Ferraz MJ, Kuo CL, Wu L, Geurink PP, Ovaa H, van der Marel GA, van der Stelt M, Boot RG, Davies GJ, Aerts JMFG, Overkleeft HS. Lahav D, et al. Among authors: van der stelt m, van den berg rjbhn, van der marel ga, van den nieuwendijk amch. J Am Chem Soc. 2017 Oct 11;139(40):14192-14197. doi: 10.1021/jacs.7b07352. Epub 2017 Sep 29. J Am Chem Soc. 2017. PMID: 28937220 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
Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes.
de Bruin G, Huber EM, Xin BT, van Rooden EJ, Al-Ayed K, Kim KB, Kisselev AF, Driessen C, van der Stelt M, van der Marel GA, Groll M, Overkleeft HS. de Bruin G, et al. Among authors: van rooden ej, van der stelt m, van der marel ga. J Med Chem. 2014 Jul 24;57(14):6197-209. doi: 10.1021/jm500716s. Epub 2014 Jul 15. J Med Chem. 2014. PMID: 25006746
N-tetradecylcarbamyl lipopeptides as novel agonists for Toll-like receptor 2.
Willems MM, Zom GG, Khan S, Meeuwenoord N, Melief CJ, van der Stelt M, Overkleeft HS, Codée JD, van der Marel GA, Ossendorp F, Filippov DV. Willems MM, et al. Among authors: van der stelt m, van der marel ga. J Med Chem. 2014 Aug 14;57(15):6873-8. doi: 10.1021/jm500722p. Epub 2014 Jul 23. J Med Chem. 2014. PMID: 25019313
Identification and development of biphenyl substituted iminosugars as improved dual glucosylceramide synthase/neutral glucosylceramidase inhibitors.
Ghisaidoobe AT, van den Berg RJ, Butt SS, Strijland A, Donker-Koopman WE, Scheij S, van den Nieuwendijk AM, Koomen GJ, van Loevezijn A, Leemhuis M, Wennekes T, van der Stelt M, van der Marel GA, van Boeckel CA, Aerts JM, Overkleeft HS. Ghisaidoobe AT, et al. Among authors: van der stelt m, van loevezijn a, van der marel ga, van boeckel ca, van den nieuwendijk am, van den berg rj. J Med Chem. 2014 Nov 13;57(21):9096-104. doi: 10.1021/jm501181z. Epub 2014 Oct 17. J Med Chem. 2014. PMID: 25250725
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
163 results