Design, synthesis and validation of integrin α2β 1-targeted probe for microPET imaging of prostate cancer

Chiun Wei Huang, Zibo Li, Hancheng Cai, Kai Chen, Tony Shahinian, Peter S. Conti

Research output: Contribution to journalArticlepeer-review

22 Scopus citations


Purpose: The ability of PET to aid in the diagnosis and management of recurrent and/or disseminated metastatic prostate cancer may be enhanced by the development of novel prognostic imaging probes. Accumulating experimental evidence indicates that overexpression of integrin α2β 1 may correlate with progression in human prostate cancer. In this study, 64Cu-labeled integrin α2β1- targeted PET probes were designed and evaluated for the imaging of prostate cancer. Methods: DGEA peptides conjugated with a bifunctional chelator (BFC) were developed to image integrin α2β1 expression with PET in a subcutaneous PC-3 xenograft model. The microPET images were reconstructed by a two-dimensional ordered subsets expectation maximum algorithm. The average radioactivity accumulation within a tumor or an organ was quantified from the multiple region of interest volumes. Results: The PET tracer demonstrated prominent tumor uptake in the PC-3 xenograft (integrin α2β1-positive). The receptor specificity was confirmed in a blocking experiment. Moreover, the low tracer uptake in a CWR-22 tumor model (negative control) further confirmed the receptor specificity. Conclusion: The sarcophagine-conjugated DGEA peptide allows noninvasive imaging of tumor-associated α2β1 expression, which may be a useful PET probe for evaluating the metastatic potential of prostate cancer.

Original languageEnglish (US)
Pages (from-to)1313-1322
Number of pages10
JournalEuropean Journal of Nuclear Medicine and Molecular Imaging
Issue number7
StatePublished - Jul 2011


  • DGEA peptide
  • Integrin αβ
  • Metastatic biomarker
  • Prostate tumor imaging
  • microPET imaging

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging


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