64Cu-PSMA-617: A novel PSMA-targeted radio-tracer for PET imaging in gastric adenocarcinoma xenografted mice model

Xue Di Han, Chen Liu, Fei Liu, Qing Hua Xie, Te Li Liu, Xiao Yi Guo, Xiaoxia Xu, Xing Yang, Hua Zhu, Zhi Yang

Research output: Contribution to journalArticle

Abstract

Here, we report that it's feasible for imaging gastric adenocarcinoma mice model with prostate-specific membrane antigen (PSMA) targeting imaging agents, which could potentially provide an alternate and readily translational tool for managing gastric adenocarcinoma. DKFZ-PSMA-617, a PSMA targeting ligand reported recently, was chosen to be radio-labeled with nuclide 64Cu. 64Cu-PSMA-617 was radio-synthesized in high radio-chemical yield and specific activity up to 19.3 GBq/μmol. It showed good stability in vitro. The specificity of 64Cu-PSMA-617 was confirmed by cell uptake experiments in PSMA (+) LNCaP cell and PSMA (-) PC-3 and gastric adenocarcinoma BGC-823 cells. Micro-PET imaging in BGC-823 and PC-3 xenografts nude mice was evaluated (n = 4). And the tumors were visualized and better tumor-tobackground achieved till 24 h. Co-administration of N- [[[(1S)-1-Carboxy-3- methylbutyl]amino]-carbonyl]-L-glutamic acid (ZJ-43) can substantially block the uptake in those tumors. Dissected tumor tissues were analyzed by auto-radiography and immunohistochemistry, and these results confirmed the PSMA expression in neo-vasculature which explained the target molecular imaging of 64Cu-PSMA-617. All those results suggested 64Cu-PSMA-617 may serve as a novel radio-tracer for tumor imaging more than prostate cancer.

Original languageEnglish (US)
Pages (from-to)74159-74169
Number of pages11
JournalOncotarget
Volume8
Issue number43
DOIs
Publication statusPublished - Jan 1 2017

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Keywords

  • 64Cu
  • Gastric cancer
  • Neo-vasculature
  • PET
  • Prostate specific membrane antigen

ASJC Scopus subject areas

  • Oncology

Cite this

Han, X. D., Liu, C., Liu, F., Xie, Q. H., Liu, T. L., Guo, X. Y., ... Yang, Z. (2017). 64Cu-PSMA-617: A novel PSMA-targeted radio-tracer for PET imaging in gastric adenocarcinoma xenografted mice model. Oncotarget, 8(43), 74159-74169. https://doi.org/10.18632/oncotarget.18276