Abstract. gastrin-releasing peptide receptor (grPr) is overexpressed by a variety of human tumors and in particular, identified to be upregulated in prostate cancers. the current study aimed to develop clinically translatable BBn analogue-based radioligands for positron emission tomography (Pet) of grPr-positive tumors. We developed radiolabeled BBn analogues and modified radiolabeled galacto-BBN analogues and then investigated their tumor-targeting efficacy in vivo. the chelator 1,4,7-triazacyclononane, 1-glutaric acid-4,7 acetic acid (noDaga) was used to radiolabel the peptides with 64 cu. the peptides were evaluated by measuring cell-based receptor-binding affinities. Biodistribution experiments and small animal imaging using Pet were performed in nude mice bearing subcutaneous Pc3 human prostate cancer xenografts. the conjugates were radiolabeled with yields >99%. the stability assay showed that
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