The novel β2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells.

Abstract

Proteasome inhibitor resistance is a challenge for myeloma therapy. Bortezomib targets the β5 and β1 activity, but not the β2 activity of the proteasome. Bortezomib-resistant myeloma cells down-regulate the activation status of the unfolded protein response, and up-regulate β2 proteasome activity. To improve proteasome inhibition in bortezomib-resistant… (More)
DOI: 10.3324/haematol.2014.109421

Topics

7 Figures and Tables

Cite this paper

@article{Kraus2015TheN, title={The novel β2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells.}, author={Marianne Kraus and Juergen Bader and Paul P. Geurink and Emily S Weyburne and Anne C. Mirabella and Tobias Silzle and Tamer B Shabaneh and Wouter A. van der Linden and Gerjan de Bruin and Sarah Roberta Haile and Eva J van Rooden and Christina Appenzeller and Nan Li and Alexei F. Kisselev and Herman S Overkleeft and Christoph Driessen}, journal={Haematologica}, year={2015}, volume={100 10}, pages={1350-60} }