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学科主题: 公共卫生
题名:
2-Mercaptoacetylglycylglycyl (MAG(2)) as a Bifunctional Chelator for Tc-99m-Labeling of Cyclic RGD Dimers: Effect of Technetium Chelate on Tumor Uptake and Pharmacokinetics
作者: Shi, Jiyun1; Kim, Young-Seung1; Chakraborty, Sudipta1; Jia, Bing2; Wang, Fan2; Liu, Shuang1
刊名: BIOCONJUGATE CHEMISTRY
发表日期: 2009-08-01
DOI: 10.1021/bc9001739
卷: 20, 期:8, 页:1559-1568
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]: INTEGRIN ALPHA(V)BETA(3) EXPRESSION ; GLIOMA INTEGRIN-ALPHA(V)BETA(3) EXPRESSION ; CANCER ALPHA(V)-INTEGRIN EXPRESSION ; POSITRON-EMISSION-TOMOGRAPHY ; IN-VIVO EVALUATION ; BREAST-CANCER ; DRUG DEVELOPMENT ; BIODISTRIBUTION CHARACTERISTICS ; INITIAL EVALUATION ; F-18-LABELED RGD
英文摘要:

This report describes the synthesis of MAG(2)-PEG(4)-E[c(RGDfK)](2) (MAG(2)-P-RGD(2): MAG(2) = S-benzoylmercaptoacetylglycylglycyl; PEG(4) = 15-amino-4.7,10,13-tetraoxapentadecanoic acid) and MAG(2)-PEG(4)-E[PEG(4)-c(RGDfK)](2) (MAG(2)-3P-RGD(2)), and the evaluation of (TcO)-Tc-99m(MAG(2)-P-RGD(2)) and (TcO)-Tc-99m(MAG(2)-3P-RGD(2)) as new radiotracers for tumor imaging in the athymic nude mice bearing U87MG human glioma xenografts. We found that MAG(2) is such all efficient bifunctional chelating agent that (TcO)-Tc-99m(MAG(2)-P-RGD(2)) and (TcO)-Tc-99m(MAG(2)-3P-RGD(2)) could be prepared in high yield (>90%) with high specific activity (similar to 5 Ci/mu mol) using a kit formulation. (TcO)-Tc-99m(MAG(2)-P-RGD(2)) and (TcO)-Tc-99m(MAG(2)-3P-RGD(2)) have very high solution stability in the kit matrix. Biodistribution data in athymic nude mice bearing U87MG human glioma xenografts indicated that replacing the highly charged [(TcO)-Tc-99m(MAG(2) = 6-hydrazinonicotinyl and TPPTS = trisodium triphenylphosphine-3,3′,3 ′′-trisulfonate) with smaller (TcO)-Tc-99m(MAG(2)) resulted in a significant increase in the radiotracer uptake in the tumor and normal organs most likely due to the higher lipophilicity of (TcO)-Tc-99m(MAG(2)-3P-RGD(2)) (log P = -3.15 +/- 0.10) than that for [Tc-99m(HYNIC-3P-RGD(2))(tricine)(TPPTS)] (Tc-99m-3P-RGD(2): log P = -3.96 +/- 0.05). Even though (TcO)-Tc-99m(MAG(2)-3P-RGD(2)) has better tumor uptake (15.36 +/- 2.17%ID/g at 60 min postinjection (p.i.)) than Tc-99m-3P-RGD(2) (9.15 +/- 2.13%ID/g at 60 min p.i.), its tumor-to-background (T/B) ratios (tumor/blood = 13.52 +/- 4.57; tumor/liver = 4.25 +/- 0.88; tumor/lung = 3.17 +/- 0.60; and tumor/muscle = 8.34 +/- 2.34) are not as good as those of Tc-99m-3P-RGD(2) (tumor/blood = 36.0 +/- 11.5; tumor/liver = 5.14 +/- 1.46; tumor/lung = 4.36 +/- 0.54; and tumor/muscle = 13.70 +/- 2.21) at 60 min p.i. On the basis of these results, we believe that Tc-99m-3P-RGD(2) remains a better radiotracer because of its higher T/B ratios.

语种: 英语
所属项目编号: R01 CA115883 A2 ; R21 HL083961-01 ; DE-FG02-08ER64684 ; NSF-30780728
项目资助者: Purdue University and research ; National Cancer Institute (NCI) ; National Heart, Lung, and Blood Institute (NHLBI) ; Department of Energy ; National Science Foundation of China
WOS记录号: WOS:000269042100017
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67943
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.Purdue Univ, Sch Hlth Sci, W Lafayette, IN 47907 USA
2.Peking Univ, Med Isotopes Res Ctr, Beijing 100191, Peoples R China

Recommended Citation:
Shi, Jiyun,Kim, Young-Seung,Chakraborty, Sudipta,et al. 2-Mercaptoacetylglycylglycyl (MAG(2)) as a Bifunctional Chelator for Tc-99m-Labeling of Cyclic RGD Dimers: Effect of Technetium Chelate on Tumor Uptake and Pharmacokinetics[J]. BIOCONJUGATE CHEMISTRY,2009,20(8):1559-1568.
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