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学科主题: 公共卫生
题名:
Potential therapeutic radiotracers: preparation, biodistribution and metabolic characteristics of Lu-177-labeled cyclic RGDfK dimer
作者: 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
发表日期: 2010-06-01
DOI: 10.1007/s00726-009-0382-0
卷: 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
所属项目编号: 30640067 ; 30870728 ; 30930030 ; 30900373 ; 2007AA02Z467 ; 2009ZX09103-733
项目资助者: NSFC ; 863 project ; Ministry of Science and Technology of China
WOS记录号: WOS:000278519200009
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/50468
Appears in Collections:北京大学医药卫生分析中心_期刊论文

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作者单位: Peking Univ, Med Isotopes Res Ctr, Beijing 100191, Peoples R China

Recommended Citation:
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.
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