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IR@PKUHSC  > 北京大学医药卫生分析中心  > 期刊论文
学科主题: 公共卫生
题名:
Tc-99m-labeled cyclic RGDfK dimer: Initial evaluation for SPECT imaging of glioma integrin alpha(v)beta(3) expression
作者: Jia, Bing; Shi, Jiyun; Yang, Zhi; Xu, Bing; Liu, Zhaofei; Zhao, Huiyun; Liu, Shuang; Wang, Fan
刊名: BIOCONJUGATE CHEMISTRY
发表日期: 2006-07-19
DOI: 10.1021/bc060055b
卷: 17, 期:4, 页:1069-1076
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemical Research Methods ; Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary ; Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]: RECEPTOR-POSITIVE TUMORS ; CANCER ALPHA(V)-INTEGRIN EXPRESSION ; VASCULAR INTEGRIN ALPHA(V)BETA(3) ; POSITRON-EMISSION-TOMOGRAPHY ; VITRONECTIN RECEPTOR ; BREAST-CANCER ; BRAIN-TUMORS ; IN-VIVO ; ALPHA-V-BETA-3 INTEGRIN ; BIOLOGICAL EVALUATION
英文摘要:

This report describes the evaluation of biodistribution properties of three radiotracers, [Tc-99m(SQ168)(EDDA)], [Tc-99m(SQ168)(tricine)(PDA)], and [Tc-99m(SQ168)(tricine)(TPPTS)] (SQ168 = [2-[[[5-[carboonyl]-2-pyridinyl]-hydrazono] methyl]benzenesulfonic acid]-Glu(cyclo{Lys-Arg-Gly-Asp-D-Phe})-cyclo{Lys-Arg-Gly-Asp-D-Phe}; EDDA = ethylenediamine-N,N′-diacetic acid; PDA = 2,5-pyridinedicarboxylic acid; TPPTS = trisodium triphenylphosphine-3,3′, 3"-trisulfonate), and their potential to image the glioma integrin alpha(v)beta(3) expression in BALB/c nude mice bearing the U87MG human glioma xenografts. It was found that all three radiotracers were able to localize in glioma tumors with a relatively high tumor uptake and long tumor retention time by binding to the integrin alpha(v)beta(3) expressed on both tumor cells and endothelial cells of tumor neovasculature. It seems that the coligand has minimal effect on integrin alpha(v)beta(3) targeting capability of the Tc-99m-labeled RGDfK dimer, but it has a significant impact on their biodistribution properties. For example, the complex [Tc-99m(SQ168)(tricine)( TPPTS)] has the lowest liver uptake and the highest metabolic stability in normal BALB/c nude mice. Results from SPECT imaging studies show that the glioma tumors can be clearly visualized with all three radiotracers at 4 h postinjection. Among the three radiotracers evaluated in this study, [Tc-99m(SQ168)(tricine)(TPPTS)] has the best imaging quality and is a promising candidate for more preclinical evaluations in the future.

语种: 英语
WOS记录号: WOS:000239120500028
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54725
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: 1.China Inst Atom Energy, Beijing 102413, Peoples R China
2.Purdue Univ, Sch Hlth Sci, W Lafayette, IN 47907 USA
3.Peking Univ, Med Isotopes Res Ctr, Beijing 100083, Peoples R China
4.Peking Univ, Oncol Sch, Dept Nucl Med, Beijing 100036, Peoples R China

Recommended Citation:
Jia, Bing,Shi, Jiyun,Yang, Zhi,et al. Tc-99m-labeled cyclic RGDfK dimer: Initial evaluation for SPECT imaging of glioma integrin alpha(v)beta(3) expression[J]. BIOCONJUGATE CHEMISTRY,2006,17(4):1069-1076.
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