Specific PET Imaging Probes for Early Detection of Prostate Cancer Metastases.

摘要

Cell permeable peptide is considered as an efficient delivery system to cross the cell membrane barrier. However, the underlying mechanisms are very complicated. Through this project, we found that laminin receptor is one of initial binding site(s) responsible for R11 peptide uptake in prostate cells. Towards the goal of developing R11 for specific prostate cancer detection, we have successfully developed an approach to impart multivalency to a bifunctional chelator for targeted PET imaging probe design. This type of multivalent scaffolds features a chelator that forms a stable and neutral complex with a radiometal and multiple functional groups for multimeric presentation of targeting molecules. The in vitro and in vivo evaluation clearly demonstrated the multivalent probes with the anticipated multivalent effect as compared to its monomeric counterpart. Tested in various tumor models, our R11 based imaging probes showed the anticipated prostate cancer detection specificity.