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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: de bruin g. 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.
Proteasome inhibitors with photocontrolled activity.
Hansen MJ, Velema WA, de Bruin G, Overkleeft HS, Szymanski W, Feringa BL. Hansen MJ, et al. Among authors: de bruin g. Chembiochem. 2014 Sep 22;15(14):2053-7. doi: 10.1002/cbic.201402237. Epub 2014 Aug 14. Chembiochem. 2014. PMID: 25125335
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: de bruin g. Haematologica. 2015 Oct;100(10):1350-60. doi: 10.3324/haematol.2014.109421. Epub 2015 Jun 11. Haematologica. 2015. PMID: 26069288 Free PMC article.
The novel β2-selective proteasome inhibitor LU-102 decreases phosphorylation of I kappa B and induces highly synergistic cytotoxicity in combination with ibrutinib in multiple myeloma cells.
Kraus J, Kraus M, Liu N, Besse L, Bader J, Geurink PP, de Bruin G, Kisselev AF, Overkleeft H, Driessen C. Kraus J, et al. Among authors: de bruin g. Cancer Chemother Pharmacol. 2015 Aug;76(2):383-96. doi: 10.1007/s00280-015-2801-0. Epub 2015 Jun 23. Cancer Chemother Pharmacol. 2015. PMID: 26099967 Free PMC article.
69 results