Abstract
Neuroendocrine prostate cancer (NEPC) is an aggressive malignancy with no effective targeted therapies. The oncogenic MUC1-C protein is overexpressed in castration-resistant prostate cancer (CRPC) and NEPC, but its specific role is unknown. Here, we demonstrate that upregulation of MUC1-C in androgen-dependent PC cells suppresses androgen receptor (AR) axis signaling and induces the neural BRN2 transcription factor. MUC1-C activates a MYC→BRN2 pathway in association with induction of MYCN, EZH2 and NE differentiation markers (ASCL1, AURKA and SYP) linked to NEPC progression. Moreover, MUC1-C suppresses the p53 pathway, induces the Yamanaka pluripotency factors (OCT4, SOX2, KLF4 and MYC) and drives stemness. Targeting MUC1-C decreases PC self-renewal capacity and tumorigenicity, suggesting a potential therapeutic approach for CRPC and NEPC. In PC tissues, MUC1 expression associates with suppression of AR signaling and increases in BRN2 expression and NEPC score. These results highlight MUC1-C as a master effector of lineage plasticity driving progression to NEPC.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Aurora Kinase A / metabolism
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Basic Helix-Loop-Helix Transcription Factors / metabolism
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Carcinogenesis / genetics
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Carcinoma, Neuroendocrine / genetics
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Carcinoma, Neuroendocrine / metabolism*
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Cell Line, Tumor
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Disease Progression*
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Enhancer of Zeste Homolog 2 Protein / metabolism
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Gene Expression Regulation, Neoplastic
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Homeodomain Proteins / metabolism
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Humans
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Kruppel-Like Factor 4
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Kruppel-Like Transcription Factors / metabolism
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Male
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Mice
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Mice, Nude
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Mucin-1 / genetics
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Mucin-1 / metabolism*
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N-Myc Proto-Oncogene Protein / metabolism
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Neoplastic Stem Cells / metabolism
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Neuronal Plasticity / physiology*
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Octamer Transcription Factor-3 / metabolism
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POU Domain Factors / metabolism
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Prostate / pathology
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Prostatic Neoplasms / genetics
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Prostatic Neoplasms / metabolism*
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Prostatic Neoplasms, Castration-Resistant / genetics
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Prostatic Neoplasms, Castration-Resistant / metabolism
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Proto-Oncogene Proteins c-myc
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SOXB1 Transcription Factors / metabolism
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Signal Transduction
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Synaptophysin / metabolism
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Tumor Suppressor Protein p53 / metabolism
Substances
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ASCL1 protein, human
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Basic Helix-Loop-Helix Transcription Factors
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Homeodomain Proteins
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KLF4 protein, human
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Klf4 protein, mouse
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Kruppel-Like Factor 4
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Kruppel-Like Transcription Factors
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MUC1 protein, human
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MYC protein, human
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MYCN protein, human
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Mucin-1
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N-Myc Proto-Oncogene Protein
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Octamer Transcription Factor-3
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POU Domain Factors
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POU5F1 protein, human
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Proto-Oncogene Proteins c-myc
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SOX2 protein, human
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SOXB1 Transcription Factors
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SYP protein, human
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Synaptophysin
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Tumor Suppressor Protein p53
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transcription factor Brn-2
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EZH2 protein, human
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Enhancer of Zeste Homolog 2 Protein
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Aurora Kinase A