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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. Haematologica. 2015 Oct;100(10):1350-60. doi: 10.3324/haematol.2014.109421. Epub 2015 Jun 11. Haematologica. 2015. PMID: 26069288 Free PMC article.
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: overkleeft hs. 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.
Use of proteasome inhibitors.
Downey SL, Florea BI, Overkleeft HS, Kisselev AF. Downey SL, et al. Among authors: overkleeft hs. Curr Protoc Immunol. 2015 Apr 1;109:9.10.1-9.10.8. doi: 10.1002/0471142735.im0910s109. Curr Protoc Immunol. 2015. PMID: 25845565
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: overkleeft hs. 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
Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes.
Xin BT, de Bruin G, Huber EM, Besse A, Florea BI, Filippov DV, van der Marel GA, Kisselev AF, van der Stelt M, Driessen C, Groll M, Overkleeft HS. Xin BT, et al. Among authors: overkleeft hs. J Med Chem. 2016 Aug 11;59(15):7177-87. doi: 10.1021/acs.jmedchem.6b00705. Epub 2016 Aug 1. J Med Chem. 2016. PMID: 27438186
502 results