期刊
CONTRAST MEDIA & MOLECULAR IMAGING
卷 -, 期 -, 页码 -出版社
WILEY-HINDAWI
DOI: 10.1155/2017/6873684
关键词
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资金
- Wallenberg infrastructure for PET-MRI (WIPPET) at SciLifeLab Pilot Facility
- Swedish nationally available imaging platform at Uppsala University, Sweden - Knut and Alice Wallenberg Foundation (muSPECT/CT)
- Swedish Cancer Society [CAN2014/474, CAN2015/350]
- Swedish Research Council [2015-02509, 2015-02353]
- Vinnova [2015-02353, 2015-02509] Funding Source: Vinnova
- Swedish Research Council [2015-02509, 2015-02353] Funding Source: Swedish Research Council
High gastrin releasing peptide receptor (GRPR) expression is associated with numerous cancers including prostate and breast cancer. The aim of the current study was to develop a Co-55-labeled PET agent based on GRPR antagonist RM26 for visualization of GRPR-expressing tumors. Labeling with Co-57 and Co-55, stability, binding specificity, and in vitro and in vivo characteristics of Co-57-NOTA-PEG(2)-RM26 were studied. NOTA-PEG(2)-RM26 was successfully radiolabeled with Co-57 and Co-55 with high yields and demonstrated high stability. The radiopeptide showed retained binding specificity to GRPR in vitro and in vivo. Co-57-NOTA-PEG(2)-RM26 biodistribution in mice was characterized by rapid clearance of radioactivity from blood and normal non-GRPR-expressing organs and low hepatic uptake. The clearance was predominantly renal with a low degree of radioactivity reabsorption. Tumor-to-blood ratios were approximately 200 (3 h pi) and 1000 (24 h pi). The favorable biodistribution of cobalt-labeled NOTA-PEG(2)-RM26 translated into high contrast preclinical PET/CT (using Co-55) and SPECT/CT (using Co-57) images of PC-3 xenografts. The initial biological results suggest that Co-55-NOTA-PEG(2)-RM26 is a promising tracer for PET visualization of GRPR-expressing tumors.
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