Abstract
EGFR is frequently amplified, mutated, and overexpressed in malignant gliomas. Yet the EGFR-targeted therapies have thus far produced only marginal clinical responses, and the underlying mechanism remains poorly understood. Using an inducible oncogenic EGFR-driven glioma mouse model system, our current study reveals that a small population of glioma cells can evade therapy-initiated apoptosis and potentiate relapse development by adopting a mesenchymal-like phenotypic state that no longer depends on oncogenic EGFR signaling. Transcriptome analyses of proximal and distal treatment responses identified TGFβ/YAP/Slug signaling cascade activation as a major regulatory mechanism that promotes therapy-induced glioma mesenchymal lineage transdifferentiation. Following anti-EGFR treatment, TGFβ secreted from stressed glioma cells acted to promote YAP nuclear translocation that stimulated upregulation of the pro-mesenchymal transcriptional factor SLUG and subsequent glioma lineage transdifferentiation toward a stable therapy-refractory state. Blockade of this adaptive response through suppression of TGFβ-mediated YAP activation significantly delayed anti-EGFR relapse and prolonged animal survival. Together, our findings shed new insight into EGFR-targeted therapy resistance and suggest that combinatorial therapies of targeting both EGFR and mechanisms underlying glioma lineage transdifferentiation could ultimately lead to deeper and more durable responses. SIGNIFICANCE: This study demonstrates that molecular reprogramming and lineage transdifferentiation underlie anti-EGFR therapy resistance and are clinically relevant to the development of new combinatorial targeting strategies against malignant gliomas with aberrant EGFR signaling.
©2021 American Association for Cancer Research.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adaptor Proteins, Signal Transducing / antagonists & inhibitors
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Adaptor Proteins, Signal Transducing / metabolism
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Animals
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Antineoplastic Combined Chemotherapy Protocols / pharmacology*
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Antineoplastic Combined Chemotherapy Protocols / therapeutic use
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Apoptosis / drug effects
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Apoptosis / genetics
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Brain Neoplasms / drug therapy*
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Brain Neoplasms / genetics
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Brain Neoplasms / pathology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cell Proliferation / genetics
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Cell Transdifferentiation / drug effects*
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Cell Transdifferentiation / genetics
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Datasets as Topic
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Disease Models, Animal
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Drug Resistance, Neoplasm / drug effects
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Drug Resistance, Neoplasm / genetics
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ErbB Receptors / antagonists & inhibitors
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ErbB Receptors / genetics
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Erlotinib Hydrochloride / pharmacology
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Erlotinib Hydrochloride / therapeutic use
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Female
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Gene Expression Regulation, Neoplastic / drug effects
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Glioma / drug therapy*
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Glioma / genetics
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Glioma / mortality
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Glioma / pathology
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Homeodomain Proteins / genetics
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Humans
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Male
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Mice
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Mice, Knockout
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Neoplasm Recurrence, Local / epidemiology*
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Neoplasm Recurrence, Local / genetics
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Neoplasm Recurrence, Local / prevention & control
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Prognosis
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Progression-Free Survival
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RNA-Seq
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Signal Transduction / drug effects
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Signal Transduction / genetics
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Transcription Factors / antagonists & inhibitors
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Transcription Factors / metabolism
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Transforming Growth Factor beta1 / antagonists & inhibitors
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Transforming Growth Factor beta1 / metabolism
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Xenograft Model Antitumor Assays
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YAP-Signaling Proteins
Substances
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Adaptor Proteins, Signal Transducing
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Homeodomain Proteins
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TGFB1 protein, human
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Tgfb1 protein, mouse
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Transcription Factors
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Transforming Growth Factor beta1
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YAP-Signaling Proteins
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YAP1 protein, human
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Yap1 protein, mouse
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RAG-1 protein
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Erlotinib Hydrochloride
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EGFR protein, human
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EGFR protein, mouse
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ErbB Receptors