Abstract
Knowledge of oncogenic mutations can inspire therapeutic strategies that are synthetically lethal, affecting cancer cells while sparing normal cells. Lenalidomide is an active agent in the activated B cell-like (ABC) subtype of diffuse large B cell lymphoma (DLBCL), but its mechanism of action is unknown. Lenalidomide kills ABC DLBCL cells by augmenting interferon β (IFNβ) production, owing to the oncogenic MYD88 mutations in these lymphomas. In a cereblon-dependent fashion, lenalidomide downregulates IRF4 and SPIB, transcription factors that together prevent IFNβ production by repressing IRF7 and amplify prosurvival NF-κB signaling by transactivating CARD11. Blockade of B cell receptor signaling using the BTK inhibitor ibrutinib also downregulates IRF4 and consequently synergizes with lenalidomide in killing ABC DLBCLs, suggesting attractive therapeutic strategies.
Copyright © 2012 Elsevier Inc. All rights reserved.
Publication types
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Research Support, N.I.H., Intramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Adaptor Proteins, Signal Transducing
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Adenine / analogs & derivatives
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Animals
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Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
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Blotting, Western
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Cell Line, Tumor
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DNA-Binding Proteins / genetics
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DNA-Binding Proteins / metabolism
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Female
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Gene Expression Profiling
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Gene Expression Regulation, Neoplastic / drug effects
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Gene Regulatory Networks / drug effects
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Humans
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Interferon Regulatory Factors / genetics
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Interferon Regulatory Factors / metabolism
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Interferon-beta / genetics
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Interferon-beta / metabolism
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Interferon-beta / pharmacology
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Lenalidomide
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Lymphoma, Large B-Cell, Diffuse / drug therapy*
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Lymphoma, Large B-Cell, Diffuse / genetics
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Lymphoma, Large B-Cell, Diffuse / pathology
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Mice
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Mice, Inbred NOD
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Mice, SCID
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NF-kappa B / genetics
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NF-kappa B / metabolism
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Peptide Hydrolases / genetics
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Peptide Hydrolases / metabolism
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Piperidines
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Pyrazoles / administration & dosage
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Pyrimidines / administration & dosage
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RNA Interference
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Reverse Transcriptase Polymerase Chain Reaction
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Signal Transduction / drug effects
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Thalidomide / administration & dosage
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Thalidomide / analogs & derivatives
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Transcription Factors / genetics
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Transcription Factors / metabolism
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Tumor Burden / drug effects*
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Tumor Burden / genetics
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Ubiquitin-Protein Ligases
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Xenograft Model Antitumor Assays*
Substances
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Adaptor Proteins, Signal Transducing
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CRBN protein, human
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DNA-Binding Proteins
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Interferon Regulatory Factors
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NF-kappa B
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Piperidines
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Pyrazoles
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Pyrimidines
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Transcription Factors
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interferon regulatory factor-4
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SPIB protein, human
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ibrutinib
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Thalidomide
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Interferon-beta
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Ubiquitin-Protein Ligases
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Peptide Hydrolases
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Lenalidomide
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Adenine
Associated data
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GEO/GSE32456
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GEO/GSE33012