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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: kisselev af. 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.
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: kisselev af. 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.
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: kisselev af. 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.
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: kisselev af. J Med Chem. 2014 Jul 24;57(14):6197-209. doi: 10.1021/jm500716s. Epub 2014 Jul 15. J Med Chem. 2014. PMID: 25006746
Use of proteasome inhibitors.
Downey SL, Florea BI, Overkleeft HS, Kisselev AF. Downey SL, et al. Among authors: kisselev af. Curr Protoc Immunol. 2015 Apr 1;109:9.10.1-9.10.8. doi: 10.1002/0471142735.im0910s109. Curr Protoc Immunol. 2015. PMID: 25845565
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: kisselev af. Haematologica. 2015 Oct;100(10):1350-60. doi: 10.3324/haematol.2014.109421. Epub 2015 Jun 11. Haematologica. 2015. PMID: 26069288 Free PMC article.
61 results