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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
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 forExpand
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Conditional activation of Pik3caH1047R in a knock-in mouse model promotes mammary tumorigenesis and emergence of mutations
Oncogenic mutations in PIK3CA, which encodes the phosphoinositide-3-kinase (PI3K) catalytic subunit p110α, occur in ∼25% of human breast cancers. In this study, we report the development of aExpand
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Proteasome-based mechanisms of intrinsic and acquired bortezomib resistance in non-small cell lung cancer.
The proteasome inhibitor bortezomib, registered for Multiple Myeloma treatment, is currently explored for activity in solid tumors including non-small cell lung cancer (NSCLC). Here we studied theExpand
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Carfilzomib and ONX 0912 Inhibit Cell Survival and Tumor Growth of Head and Neck Cancer and Their Activities Are Enhanced by Suppression of Mcl-1 or Autophagy
Purpose: Carfilzomib is a selective, irreversible inhibitor of the chymotrypsin-like activity of the proteasome and is undergoing clinical evaluation in myeloma. ONX 0912 (oprozomib) is an orallyExpand
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Overcoming bortezomib resistance in human B cells by anti-CD20/rituximab-mediated complement-dependent cytotoxicity and epoxyketone-based irreversible proteasome inhibitors
BackgroundIn clinical and experimental settings, antibody-based anti-CD20/rituximab and small molecule proteasome inhibitor (PI) bortezomib (BTZ) treatment proved effective modalities for B cellExpand
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The next generation proteasome inhibitors carfilzomib and oprozomib activate prosurvival autophagy via induction of the unfolded protein response and ATF4
The proteasome inhibitor bortezomib has shown remarkable clinical success in the treatment of multiple myeloma. However, the efficacy and mechanism of action of bortezomib in solid tumor malignanciesExpand
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Inactivating PSMB 5 mutations and P-glycoprotein ( MDR 1 / ABCB 1 ) mediate resistance to proteasome inhibitors : ex vivo efficacy of ( immuno ) proteasome inhibitors in mononuclear blood cells from
Submitted 5 Inactivating PSMB5 mutations and P-glyco-protein (MDR1/ ABCB1) mediate resistance to proteasome inhibitors: ex vivo efficacy of (immuno) proteasome inhibitors in mononuclear blood cellsExpand
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Synergistic effects of proteasome inhibitor carfilzomib in combination with tyrosine kinase inhibitors in imatinib-sensitive and -resistant chronic myeloid leukemia models
The tyrosine kinase inhibitor (TKI) imatinib has transformed the treatment and outlook of chronic myeloid leukemia (CML); however, the development of drug resistance and the persistence ofExpand
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Inactivating PSMB 5 Mutations and P-Glycoprotein ( Multidrug Resistance-Associated Protein / ATP-Binding Cassette B 1 ) Mediate Resistance to Proteasome Inhibitors : Ex Vivo Efficacy of ( Immuno )
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 forExpand
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Sensitivity of Pediatric Acute Leukemia Cells to Bortezomib and Epoxyketone-Based Proteasome Inhibitors: Correlations with Proteasome Subunit Expression
Abstract 1513 Good response to glucocorticoids (GC) has favorable prognostic value for the survival of children with acute lymphoblastic leukemia (ALL). Hence, GC-resistant and relapsed ALLExpand
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