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Tc-99m-labeled cyclic RGDfK dimer: Initial evaluation for SPECT imaging of glioma integrin alpha(v)beta(3) expression
Jia, Bing; Shi, Jiyun; Yang, Zhi; Xu, Bing; Liu, Zhaofei; Zhao, Huiyun; Liu, Shuang; Wang, Fan
刊名BIOCONJUGATE CHEMISTRY
2006-07-19
DOI10.1021/bc060055b
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
引用统计
被引频次:59[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/400002259/54725
专题北京大学医药卫生分析中心
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
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GB/T 7714
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.
APA Jia, Bing.,Shi, Jiyun.,Yang, Zhi.,Xu, Bing.,Liu, Zhaofei.,...&Wang, Fan.(2006).Tc-99m-labeled cyclic RGDfK dimer: Initial evaluation for SPECT imaging of glioma integrin alpha(v)beta(3) expression.BIOCONJUGATE CHEMISTRY,17(4),1069-1076.
MLA Jia, Bing,et al."Tc-99m-labeled cyclic RGDfK dimer: Initial evaluation for SPECT imaging of glioma integrin alpha(v)beta(3) expression".BIOCONJUGATE CHEMISTRY 17.4(2006):1069-1076.
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