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BMP4-driven morphogenetic reprogramming sustains EGFR-TKI resistance via SOX2 suppression and EMT activation
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BMP4-driven morphogenetic reprogramming sustains EGFR-TKI resistance via SOX2 suppression and EMT activation

Alvin Chen, Dong-Jun Xie, Yu-Wei Jhu, Yen-Ju Lin, Dong-Yu Wu, Shi-Long Yan, Yu-Ting Chou 和 Jen-Chung Ko
Biomedicine & pharmacotherapy, 卷.198, 頁.119281
01/05/2026
PMID: 41904893

摘要

Adenocarcinoma of Lung - drug therapy Adenocarcinoma of Lung - genetics Adenocarcinoma of Lung - pathology Animals Apoptosis - drug effects Bone Morphogenetic Protein 4 - genetics Bone Morphogenetic Protein 4 - metabolism Bone Morphogenetic Protein Receptors, Type II - genetics Bone Morphogenetic Protein Receptors, Type II - metabolism Cell Line, Tumor Drug Resistance, Neoplasm - drug effects Epithelial-Mesenchymal Transition - drug effects ErbB Receptors - antagonists & inhibitors ErbB Receptors - genetics ErbB Receptors - metabolism Humans Lung Neoplasms - drug therapy Lung Neoplasms - genetics Lung Neoplasms - metabolism Lung Neoplasms - pathology Protein Kinase Inhibitors - pharmacology SOXB1 Transcription Factors - genetics SOXB1 Transcription Factors - metabolism Signal Transduction
Drug-resistant cells pose a major challenge to targeted therapy in EGFR-mutant lung adenocarcinoma (LUAD), yet the survival pathways they depend on remain unclear. Here, we identify BMP4 signaling as a key driver of resistance and therapeutic persistence. BMP4 is selectively enriched in EGFR-TKI-selected resistant cells, where it suppresses SOX2 and promotes an epithelial-mesenchymal transition (EMT)-like state. Knockdown of BMP4 or its receptor BMPR2 triggered apoptosis, upregulated pro-apoptotic factors (BAD, BMF), and impaired colony formation. Pharmacologic or inducible inhibition of BMP4 sensitized resistant cells, as well as residual tolerant populations in EGFR-TKI-sensitive cells, to osimertinib, while BMP4 enrichment also conferred cisplatin tolerance. Mechanistically, TGF-β1 induced BMP4 expression, and HDAC1/2 inhibition de-repressed BMP4, establishing a cytokine-epigenetic axis that maintains the BMP4 /SOX2 phenotype. Clinical analyses further revealed that BMP4 expression correlates with EMT signatures, chemoresistance pathways, and poor patient survival. These findings define a developmental signaling network in which BMP4 suppresses SOX2 to promote EMT, sustain resistant cell survival, and drive therapeutic resistance. Targeting the BMP4 axis presents a promising strategy for overcoming resistance in EGFR-mutant LUAD.

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https://doi.org/10.1016/j.biopha.2026.119281檢視
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