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European Journal of Nuclear Medicine and Molecular Imaging

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01.07.2011 | Original Article

Design, synthesis and validation of integrin α₂β₁-targeted probe for microPET imaging of prostate cancer

verfasst von: Chiun-Wei Huang, Zibo Li, Hancheng Cai, Kai Chen, Tony Shahinian, Peter S Conti

Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging | Ausgabe 7/2011

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Abstract

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 α₂β₁ 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.

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Titel: Design, synthesis and validation of integrin α2β1-targeted probe for microPET imaging of prostate cancer
verfasst von: Chiun-Wei Huang
Zibo Li
Hancheng Cai
Kai Chen
Tony Shahinian
Peter S Conti
Publikationsdatum: 01.07.2011
Verlag: Springer-Verlag
Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging / Ausgabe 7/2011
Print ISSN: 1619-7070
Elektronische ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-011-1752-x

Springer Medizin

Abstract

Purpose

Methods

Results

Conclusion

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