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学科主题: 公共卫生
题名:
Linker effects on biological properties of In-111-Labeled DTPA conjugates of a cyclic RGDfK dimer
作者: Jia, Bing2,3; Liu, Zhaofei2; Shi, Jiyun2,3; Yu, Zilin2; Yang, Zhi4; Zhao, Huiyun2; He, Zhengjie1; Liu, Shuang1; Wang, Fan2
刊名: BIOCONJUGATE CHEMISTRY
发表日期: 2008
卷: 19, 期:1, 页:201-210
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]: GLIOMA INTEGRIN-ALPHA(V)BETA(3) EXPRESSION ; CANCER ALPHA(V)-INTEGRIN EXPRESSION ; RECEPTOR ANTAGONIST USEFUL ; ALPHA(V)BETA(3) INTEGRIN ; VITRONECTIN RECEPTOR ; TUMOR ANGIOGENESIS ; IMAGING AGENTS ; BREAST-CANCER ; IN-VIVO ; PEPTIDES
英文摘要:

In this report, we present in vitro and in vivo evaluation of three In-111-labeled DTPA conjugates of a cyclic RGDfK dimer: DTPA-Bn-SU016 (SU016 = E[c(RGDfK)](2); DTPA-Bn = 2-(p-isothioureidobenzyl)diethylenetriaminepentaacetic acid), DTPA-Bn-E-SU016 (E = glutamic acid) and DTPA-Bn-Cys-SU016 (Cys = cysteic acid). The integrin (43 binding affinities of SU016, DTPA-Bn-SU016, DTPA-Bn-E-SU016, and DTPA-Bn-Cys-SU016 were determined to be 5.0 +/- 0.7 nM, 7.9 +/- 0.6 nM, 5.8 +/- 0.6 nM, and 6.9 +/- 0.9 nM, respectively, against I-125-c(RGDyK) in binding to integrin alpha(v)beta(3), suggesting that E or Cys residue has little effect on the integrin (43 affinity of E[c(RGDfK)12, It was also found that the In-111-labeling efficiency of DTPA-Bn-SU016 and DTPA-Bn-E-SU016 is 3-5 times better than that of DOTA analogues due to fast chelation kinetics and high-yield In-111-labeling under mild conditions (e.g., room temperature). Biodistribution studies were performed using BALB/c nude mice bearing U87MG human glioma xenografts. In-111-DTPA-Bn-SU016, In-111-DTPA-Bn-Cys-SU016, and In-111-DTPA-Bn-Cys-SU016 all displayed rapid blood clearance. Their tumor uptake was comparable between 0.5 and 4 h postinjection (p.i.) within experimental error. (111)InDTPA-Bn-E-SU016 had a significantly lower (p < 0.01) kidney uptake than In-111-DTPA-Bn-SU016 and In-111-DTPA-Bn-Cys-SUO16. The liver uptake of In-111-DTPA-Bn-SU016 was 1.69 +/- 0.18% ID/g at 24 h p.i., while the liver uptake values of In-111-DTPA-Bn-E-SU016 and In-111-DTPA-Bn-Cys-SU016 were 0.55 +/- 0.11% ID/g and 0.79 +/- 0.15% ID/g at 24 h p.i., respectively. Among the three In-111 radiotracers evaluated in this study, In-111-DTPA-Bn-E-SU016 has the lowest liver and kidney uptake and the best tumor/liver and tumor/kidney ratios. Results from metabolism studies indicated that there is little metabolism (<10%) for three In-111 radiotracers at 1 h p.i. Imaging data showed that tumors can be clearly visualized at 4 h p.i. with good contrast in the tumor-bearing mice administered with In-111-DTPA-Bn-E-SU016. It is concluded that using a glutamic acid linker can significantly improve excretion kinetics of the In-labeled E[c(RGDfK)12 from liver and kidneys.

语种: 英语
WOS记录号: WOS:000252520300027
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54519
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 100083, Peoples R China
3.China Inst Atom Energy, Dept Isotope, Beijing 102413, Peoples R China
4.Peking Univ, Oncol Sch, Dept Nucl Med, Beijing 100036, Peoples R China

Recommended Citation:
Jia, Bing,Liu, Zhaofei,Shi, Jiyun,et al. Linker effects on biological properties of In-111-Labeled DTPA conjugates of a cyclic RGDfK dimer[J]. BIOCONJUGATE CHEMISTRY,2008,19(1):201-210.
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