Abstract
Nasopharyngeal cancer (NPC), endemic in Southeast Asia, lacks effective diagnostic and therapeutic strategies. Even in high-income countries the 5-year survival rate for stage IV NPC is less than 40%. Here we report high somatostatin receptor 2 (SSTR2) expression in multiple clinical cohorts comprising 402 primary, locally recurrent and metastatic NPCs. We show that SSTR2 expression is induced by the Epstein-Barr virus (EBV) latent membrane protein 1 (LMP1) via the NF-κB pathway. Using cell-based and preclinical rodent models, we demonstrate the therapeutic potential of SSTR2 targeting using a cytotoxic drug conjugate, PEN-221, which is found to be superior to FDA-approved SSTR2-binding cytostatic agents. Furthermore, we reveal significant correlation of SSTR expression with increased rates of survival and report in vivo uptake of the SSTR2-binding 68Ga-DOTA-peptide radioconjugate in PET-CT scanning in a clinical trial of NPC patients (NCT03670342). These findings reveal a key role in EBV-associated NPC for SSTR2 in infection, imaging, targeted therapy and survival.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Epstein-Barr Virus Infections* / drug therapy
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Epstein-Barr Virus Infections* / genetics
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Epstein-Barr Virus Infections* / mortality
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Epstein-Barr Virus Infections* / virology
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Female
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Gene Expression Regulation, Neoplastic*
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Herpesvirus 4, Human / drug effects
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Herpesvirus 4, Human / growth & development
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Herpesvirus 4, Human / pathogenicity
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Host-Pathogen Interactions / genetics
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Humans
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Lymphatic Metastasis
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Male
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Mice
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Mice, Nude
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Molecular Targeted Therapy
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NF-kappa B / genetics
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NF-kappa B / metabolism
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Nasopharyngeal Carcinoma* / drug therapy
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Nasopharyngeal Carcinoma* / genetics
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Nasopharyngeal Carcinoma* / mortality
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Nasopharyngeal Carcinoma* / virology
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Nasopharyngeal Neoplasms* / drug therapy
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Nasopharyngeal Neoplasms* / genetics
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Nasopharyngeal Neoplasms* / mortality
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Nasopharyngeal Neoplasms* / virology
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Neoplasm Recurrence, Local* / drug therapy
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Neoplasm Recurrence, Local* / genetics
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Neoplasm Recurrence, Local* / mortality
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Neoplasm Recurrence, Local* / virology
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Octreotide / pharmacology
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Positron Emission Tomography Computed Tomography
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Receptors, Somatostatin* / antagonists & inhibitors
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Receptors, Somatostatin* / genetics
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Receptors, Somatostatin* / metabolism
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Signal Transduction
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Survival Analysis
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Viral Matrix Proteins* / antagonists & inhibitors
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Viral Matrix Proteins* / genetics
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Viral Matrix Proteins* / metabolism
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Xenograft Model Antitumor Assays
Substances
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Antineoplastic Agents
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EBV-associated membrane antigen, Epstein-Barr virus
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NF-kappa B
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Octreotide
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Receptors, Somatostatin
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SSTR2 protein, human
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Viral Matrix Proteins
Associated data
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ClinicalTrials.gov/NCT03670342