ONECUT2 is a driver of neuroendocrine prostate cancer.

TitleONECUT2 is a driver of neuroendocrine prostate cancer.
Publication TypeJournal Article
Year of Publication2019
AuthorsGuo H, Ci X, Ahmed M, Hua JTony, Soares F, Lin D, Puca L, Vosoughi A, Xue H, Li E, Su P, Chen S, Nguyen T, Liang Y, Zhang Y, Xu X, Xu J, Sheahan AV, Ba-Alawi W, Zhang S, Mahamud O, Vellanki RN, Gleave M, Bristow RG, Haibe-Kains B, Poirier JT, Rudin CM, Tsao M-S, Wouters BG, Fazli L, Feng FY, Ellis L, van der Kwast T, Berlin A, Koritzinsky M, Boutros PC, Zoubeidi A, Beltran H, Wang Y, He HHansen
JournalNat Commun
Volume10
Issue1
Pagination278
Date Published2019 01 17
ISSN2041-1723
KeywordsAnimals, Carcinogenesis, Cell Hypoxia, Cell Line, Tumor, Cell Proliferation, Datasets as Topic, Disease Progression, Gene Expression Profiling, Gene Expression Regulation, Neoplastic, Homeodomain Proteins, Humans, Hypoxia-Inducible Factor 1, alpha Subunit, Male, Mice, Mice, Inbred NOD, Mice, SCID, Neuroendocrine Tumors, Nitroimidazoles, Phosphoramide Mustards, Prostate, Prostatic Neoplasms, RNA, Small Interfering, Signal Transduction, Smad3 Protein, Transcription Factors, Up-Regulation, Xenograft Model Antitumor Assays
Abstract

Neuroendocrine prostate cancer (NEPC), a lethal form of the disease, is characterized by loss of androgen receptor (AR) signaling during neuroendocrine transdifferentiation, which results in resistance to AR-targeted therapy. Clinically, genomically and epigenetically, NEPC resembles other types of poorly differentiated neuroendocrine tumors (NETs). Through pan-NET analyses, we identified ONECUT2 as a candidate master transcriptional regulator of poorly differentiated NETs. ONECUT2 ectopic expression in prostate adenocarcinoma synergizes with hypoxia to suppress androgen signaling and induce neuroendocrine plasticity. ONEUCT2 drives tumor aggressiveness in NEPC, partially through regulating hypoxia signaling and tumor hypoxia. Specifically, ONECUT2 activates SMAD3, which regulates hypoxia signaling through modulating HIF1α chromatin-binding, leading NEPC to exhibit higher degrees of hypoxia compared to prostate adenocarcinomas. Treatment with hypoxia-activated prodrug TH-302 potently reduces NEPC tumor growth. Collectively, these results highlight the synergy between ONECUT2 and hypoxia in driving NEPC, and emphasize the potential of hypoxia-directed therapy for NEPC patients.

DOI10.1038/s41467-018-08133-6
Alternate JournalNat Commun
PubMed ID30655535
PubMed Central IDPMC6336817
Grant ListP30 CA008748 / CA / NCI NIH HHS / United States
P50 CA211024 / CA / NCI NIH HHS / United States