Journal article
Copper-64 Labeled Macrobicyclic Sarcophagine Coupled to a GRP Receptor Antagonist Shows Great Promise for PET Imaging of Prostate Cancer
E Gourni, L Del Pozzo, E Kheirallah, C Smerling, B Waser, JC Reubi, BM Paterson, PS Donnelly, PT Meyer, HR Maecke
Molecular Pharmaceutics | Published : 2015
DOI: 10.1021/mp500671j
Abstract
The gastrin-releasing peptide receptor (GRPr) is an important molecular target for the visualization and therapy of tumors and can be targeted with radiolabeled bombesin derivatives. The present study aims to develop statine-based bombesin receptor antagonists suitable for labeling with 64Cu for imaging by positron emission tomography (PET). The potent GRPr antagonist d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 was conjugated to the sarcophagine (3,6,10,13,16,19-hexaazabicyclo[6.6.6] icosane = Sar) derivative 5-(8-methyl-3,6,10,13,16,19-hexaaza-bicyclo[6.6.6]icosan-1-ylamino)-5-oxopentanoic acid (MeCOSar) via PEG4 (LE1) and PEG2 (LE2) spacers and radiolabeled with 64Cu2+ with >95% yield and sp..
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Funding Acknowledgements
This work was supported by the German Consortium for Translational Cancer Research (DKTK). We thank Yvonne Kiefer and Roswitha Toennesmann for their technical assistance.