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Design, synthesis and validation of integrin α2β1-targeted probe for microPET imaging of prostate cancer
Ist Teil von
European journal of nuclear medicine and molecular imaging, 2011-07, Vol.38 (7), p.1313-1322
Ort / Verlag
Berlin/Heidelberg: Springer-Verlag
Erscheinungsjahr
2011
Link zum Volltext
Quelle
MEDLINE
Beschreibungen/Notizen
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 α
2
β
1
may correlate with progression in human prostate cancer. In this study,
64
Cu-labeled integrin α
2
β
1
-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 α
2
β
1
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 α
2
β
1
-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 α
2
β
1
expression, which may be a useful PET probe for evaluating the metastatic potential of prostate cancer.