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Potential therapeutic radiotracers: preparation, biodistribution and metabolic characteristics of Lu-177-labeled cyclic RGDfK dimer
Shi, Jiyun; Liu, Zhaofei; Jia, Bing; Yu, Zilin; Zhao, Huiyun; Wang, Fan
关键词Integrin Alpha(v)Beta(3) Rgd Dtpa-bz Lu-177 Tumor Therapy
刊名AMINO ACIDS
2010-06-01
DOI10.1007/s00726-009-0382-0
39期:1页:111-120
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]POSITRON-EMISSION-TOMOGRAPHY ; BIFUNCTIONAL CHELATING AGENT ; IMPROVING TUMOR UPTAKE ; INTEGRIN ALPHA(V)BETA(3) ; BOMBESIN HETERODIMER ; RADIONUCLIDE THERAPY ; SOMATOSTATIN ANALOG ; PEG(4) LINKERS ; ANGIOGENESIS ; Y-90
英文摘要

In this study, we reported the preparation and evaluation of Lu-177-DOTA-RGD2, Lu-177-DOTA-Bz-RGD2 and Lu-177-DTPA-Bz-RGD2 (RGD2 = E[c(RGDfK)](2)) as a potential therapeutic radiotracers for the treatment of integrin alpha(v)beta(3)-positive tumors. The BALB/c nude mice bearing the U87MG human glioma xenografts were used to evaluate the biodistribution characteristics and excretion kinetics of Lu-177-DOTA-RGD2, Lu-177-DOTA-Bz-RGD2 and Lu-177-DTPA-Bz-RGD2. It was found that there were no major differences in their lipophilicity and biodistribution characteristics, particularly at latter time points. A major advantage of using DTPA-Bz as the bifunctional chelator (BFC) was its high radiolabeling efficiency (fast and high yield radiolabeling) at room temperature. Using DOTA and DOTA-Bz as BFCs, the radiolabeling kinetics was slow, and heating at 100A degrees C and higher DOTA-conjugate concentration were needed for successful Lu-177-labeling. Therefore, DTPA-Bz is an optimal BFC for routine preparation of Lu-177-labeled cyclic RGDfK peptides, and Lu-177-DTPA-Bz-RGD2 is worthy of further investigation for targeted radiotherapy of integrin alpha(v)beta(3)-positive tumors.

语种英语
WOS记录号WOS:000278519200009
引用统计
被引频次:12[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/400002259/50468
专题北京大学医药卫生分析中心
北京大学基础医学院
作者单位Peking Univ, Med Isotopes Res Ctr, Beijing 100191, Peoples R China
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GB/T 7714
Shi, Jiyun,Liu, Zhaofei,Jia, Bing,et al. Potential therapeutic radiotracers: preparation, biodistribution and metabolic characteristics of Lu-177-labeled cyclic RGDfK dimer[J]. AMINO ACIDS,2010,39(1):111-120.
APA Shi, Jiyun,Liu, Zhaofei,Jia, Bing,Yu, Zilin,Zhao, Huiyun,&Wang, Fan.(2010).Potential therapeutic radiotracers: preparation, biodistribution and metabolic characteristics of Lu-177-labeled cyclic RGDfK dimer.AMINO ACIDS,39(1),111-120.
MLA Shi, Jiyun,et al."Potential therapeutic radiotracers: preparation, biodistribution and metabolic characteristics of Lu-177-labeled cyclic RGDfK dimer".AMINO ACIDS 39.1(2010):111-120.
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