Article
Inactivating PSMB5 mutations and P-glycoprotein (multidrug resistance-associated protein/ATP-binding cassette B1) mediate resistance to proteasome inhibitors: ex vivo efficacy of (immuno)proteasome inhibitors in mononuclear blood cells from patients with rheumatoid arthritis.
The Journal of pharmacology and experimental therapeutics - 1 Apr 2012
Verbrugge Sue Ellen, Assaraf Yehuda G, Dijkmans Ben A C, Scheffer George L, Al Marjon, den Uyl Debby, Oerlemans Ruud, Chan Elena T, Kirk Christopher J, Peters Godefridus J, van der Heijden Joost W, de Gruijl Tanja D, Scheper Rik J, Jansen Gerrit
Abstract excerpt
Bortezomib (BTZ), a registered proteasome inhibitor (PI) for multiple myeloma, has also been proposed as a potential antirheumatic agent. Its reported side effects, however, make it unappealing for long-term administration, and resistance may also develop. To overcome this, second-generation PIs became available. Here, we investigated whether a novel class of peptide epoxyketone-based PIs, including carfilzomib,...
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