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Page 1
Nature of pharmacophore influences active site specificity of proteasome inhibitors.
Screen M, Britton M, Downey SL, Verdoes M, Voges MJ, Blom AE, Geurink PP, Risseeuw MD, Florea BI, van der Linden WA, Pletnev AA, Overkleeft HS, Kisselev AF. Screen M, et al. Among authors: van der linden wa. J Biol Chem. 2010 Dec 17;285(51):40125-34. doi: 10.1074/jbc.M110.160606. Epub 2010 Oct 11. J Biol Chem. 2010. PMID: 20937826 Free PMC article.
The novel β2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells.
Kraus M, Bader J, Geurink PP, Weyburne ES, Mirabella AC, Silzle T, Shabaneh TB, van der Linden WA, de Bruin G, Haile SR, van Rooden E, Appenzeller C, Li N, Kisselev AF, Overkleeft H, Driessen C. Kraus M, et al. Among authors: van rooden e, van der linden wa. Haematologica. 2015 Oct;100(10):1350-60. doi: 10.3324/haematol.2014.109421. Epub 2015 Jun 11. Haematologica. 2015. PMID: 26069288 Free PMC article.
A fluorescent broad-spectrum proteasome inhibitor for labeling proteasomes in vitro and in vivo.
Verdoes M, Florea BI, Menendez-Benito V, Maynard CJ, Witte MD, van der Linden WA, van den Nieuwendijk AM, Hofmann T, Berkers CR, van Leeuwen FW, Groothuis TA, Leeuwenburgh MA, Ovaa H, Neefjes JJ, Filippov DV, van der Marel GA, Dantuma NP, Overkleeft HS. Verdoes M, et al. Among authors: van der marel ga, van der linden wa, van den nieuwendijk am, van leeuwen fw. Chem Biol. 2006 Nov;13(11):1217-26. doi: 10.1016/j.chembiol.2006.09.013. Chem Biol. 2006. PMID: 17114003
A panel of subunit-selective activity-based proteasome probes.
Verdoes M, Willems LI, van der Linden WA, Duivenvoorden BA, van der Marel GA, Florea BI, Kisselev AF, Overkleeft HS. Verdoes M, et al. Among authors: van der marel ga, van der linden wa. Org Biomol Chem. 2010 Jun 21;8(12):2719-27. doi: 10.1039/c001036g. Epub 2010 May 6. Org Biomol Chem. 2010. PMID: 20449511 Free PMC article.
Activity-based profiling reveals reactivity of the murine thymoproteasome-specific subunit beta5t.
Florea BI, Verdoes M, Li N, van der Linden WA, Geurink PP, van den Elst H, Hofmann T, de Ru A, van Veelen PA, Tanaka K, Sasaki K, Murata S, den Dulk H, Brouwer J, Ossendorp FA, Kisselev AF, Overkleeft HS. Florea BI, et al. Among authors: van den elst h, van der linden wa, van veelen pa. Chem Biol. 2010 Aug 27;17(8):795-801. doi: 10.1016/j.chembiol.2010.05.027. Chem Biol. 2010. PMID: 20797608 Free PMC article.
Discovery of a potent and highly β1 specific proteasome inhibitor from a focused library of urea-containing peptide vinyl sulfones and peptide epoxyketones.
van der Linden WA, Willems LI, Shabaneh TB, Li N, Ruben M, Florea BI, van der Marel GA, Kaiser M, Kisselev AF, Overkleeft HS. van der Linden WA, et al. Among authors: van der marel ga. Org Biomol Chem. 2012 Jan 7;10(1):181-94. doi: 10.1039/c1ob06554h. Epub 2011 Nov 22. Org Biomol Chem. 2012. PMID: 22105930 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.
32 results