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Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer
Yu, Zilin1,2; Carlucci, Giuseppe1,2; Ananias, Hildo J. K.2; Dierckx, Rudi A. J. O.1; Liu, Shuang3; Helfrich, Wijnand4; Wang, Fan5; de Jong, Igle J.2; Elsinga, Philip H.1
关键词GRPR Bombesin homodimer Radiolabeled Imaging Prostate cancer PC-3 Tc-99m HYNIC SPECT
刊名AMINO ACIDS
2013-02-01
DOI10.1007/s00726-012-1369-9
44期:2页:543-553
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology
研究领域[WOS]Biochemistry & Molecular Biology
关键词[WOS]GASTRIN-RELEASING-PEPTIDE ; ALPHA(V)BETA(3) INTEGRIN ; RGD PEPTIDES ; HETERODIMER ; TUMORS ; PET ; IMMUNOREACTIVITY ; EXPRESSION ; ANALOGS ; DIMERS
英文摘要

Multimerization of peptides can improve the binding characteristics of the tracer by increasing local ligand concentration and decreasing dissociation kinetics. In this study, a new bombesin homodimer was developed based on an epsilon-aminocaproic acid-bombesin(7-14) (Aca-bombesin(7-14)) fragment, which has been studied for targeting the gastrin-releasing peptide receptor (GRPR) in prostate cancer. The bombesin homodimer was conjugated to 6-hydrazinopyridine-3-carboxylic acid (HYNIC) and labeled with Tc-99m for SPECT imaging. The in vitro binding affinity to GRPR, cell uptake, internalization and efflux kinetics of the radiolabeled bombesin dimer were investigated in the GRPR-expressing human prostate cancer cell line PC-3. Biodistribution and the GRPR-targeting potential were evaluated in PC-3 tumor-bearing athymic nude mice. When compared with the bombesin monomer, the binding affinity of the bombesin dimer is about ten times lower. However, the Tc-99m labeled bombesin dimer showed a three times higher cellular uptake at 4 h after incubation, but similar internalization and efflux characters in vitro. Tumor uptake and in vivo pharmacokinetics in PC-3 tumor-bearing mice were comparable. The tumor was visible on the dynamic images in the first hour and could be clearly distinguished from non-targeted tissues on the static images after 4 h. The GRPR-targeting ability of the Tc-99m labeled bombesin dimer was proven in vitro and in vivo. This bombesin homodimer provides a good starting point for further studies on enhancing the tumor targeting activity of bombesin multimers.

语种英语
WOS记录号WOS:000313794600025
引用统计
被引频次:11[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/63806
专题北京大学医药卫生分析中心
作者单位1.Univ Groningen, Univ Med Ctr Groningen, Dept Nucl Med & Mol Imaging, NL-9831 EZ Groningen, Netherlands
2.Univ Groningen, Univ Med Ctr Groningen, Dept Urol, NL-9831 EZ Groningen, Netherlands
3.Purdue Univ, Sch Hlth Sci, W Lafayette, IN 47907 USA
4.Univ Groningen, Univ Med Ctr Groningen, Dept Surg, NL-9831 EZ Groningen, Netherlands
5.Peking Univ, Med Isotopes Res Ctr, Beijing 100871, Peoples R China
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Yu, Zilin,Carlucci, Giuseppe,Ananias, Hildo J. K.,et al. Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer[J]. AMINO ACIDS,2013,44(2):543-553.
APA Yu, Zilin.,Carlucci, Giuseppe.,Ananias, Hildo J. K..,Dierckx, Rudi A. J. O..,Liu, Shuang.,...&Elsinga, Philip H..(2013).Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer.AMINO ACIDS,44(2),543-553.
MLA Yu, Zilin,et al."Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer".AMINO ACIDS 44.2(2013):543-553.
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