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学科主题: 公共卫生
题名:
Noninvasive imaging of tumor integrin expression using F-18-labeled RGD dimer peptide with PEG(4) linkers
作者: Liu, Zhaofei2,3; Liu, Shuanglong2; Wang, Fan3; Liu, Shuang4; Chen, Xiaoyuan1,2
关键词: Integrin alpha(v)beta(3) ; F-18 ; MicroPET ; RGD dimer ; PEGylation
刊名: EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
发表日期: 2009-08-01
DOI: 10.1007/s00259-009-1112-2
卷: 36, 期:8, 页:1296-1307
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Radiology, Nuclear Medicine & Medical Imaging
研究领域[WOS]: Radiology, Nuclear Medicine & Medical Imaging
关键词[WOS]: POSITRON-EMISSION-TOMOGRAPHY ; ENDOTHELIAL GROWTH-FACTOR ; BREAST-CANCER ; ALPHA(V)BETA(3) EXPRESSION ; MDA-MB-435 CELLS ; ANGIOGENESIS ; MICROPET ; PET ; ALPHA-V-BETA-3 ; MELANOMA
英文摘要:

Various radiolabeled Arg-Gly-Asp (RGD) peptides have been previously investigated for tumor integrin alpha(v)beta(3) imaging. To further develop RGD radiotracers with enhanced tumor-targeting efficacy and improved in vivo pharmacokinetics, we designed a new RGD homodimeric peptide with two PEG(4) spacers (PEG(4) = 15-amino-4,7,10,13-tetraoxapentadecanoic acid) between the two monomeric RGD motifs and one PEG(4) linker on the glutamate alpha-amino group (F-18-labeled PEG(4)-E[PEG(4)-c(RGDfK)](2), P-PRGD2), as a promising agent for noninvasive imaging of integrin expression in mouse models.

P-PRGD2 was labeled with F-18 via 4-nitrophenyl 2-F-18-fluoropropionate (F-18-FP) prosthetic group. In vitro and in vivo characteristics of the new dimeric RGD peptide tracer F-18-FP-P-PRGD2 were investigated and compared with those of F-18-FP-P-RGD2 (F-18-labeled RGD dimer without two PEG(4) spacers between the two RGD motifs). The ability of F-18-FP-P-PRGD2 to image tumor vascular integrin expression was evaluated in a 4T1 murine breast tumor model.

With the insertion of two PEG(4) spacers between the two RGD motifs, F-18-FP-P-PRGD2 showed enhanced integrin alpha(v)beta(3)-binding affinity, increased tumor uptake and tumor-to-nontumor background ratios compared with F-18-FP-P-RGD2 in U87MG tumors. MicroPET imaging with F-18-FP-P-PRGD2 revealed high tumor contrast and low background in tumor-bearing nude mice. Biodistribution studies confirmed the in vivo integrin alpha(v)beta(3)-binding specificity of F-18-FP-P-RGD2. F-18-FP-P-PRGD2 can specifically image integrin alpha(v)beta(3) on the activated endothelial cells of tumor neovasculature.

F-18-FP-P-PRGD2 can provide important information on integrin expression on the tumor vasculature. The high integrin binding affinity and specificity, excellent pharmacokinetic properties and metabolic stability make the new RGD dimeric tracer F-18-FP-P-PRGD2 a promising agent for PET imaging of tumor angiogenesis and for monitoring the efficacy of antiangiogenic treatment.

语种: 英语
所属项目编号: R01 120188 ; R01 CA119053 ; R21 CA121842 ; R21 CA102123 ; P50 CA114747 ; U54 CA119367 ; R24 CA93862 ; R01 CA115883 ; DE-FG02-08ER64684
项目资助者: National Cancer Institute ; Department of Energy ; Stanford University
WOS记录号: WOS:000267895700010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/55455
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.Stanford Univ, Mol Imaging Program Stanford, Dept Radiol & Bio X Program, Sch Med, Stanford, CA 94305 USA
2.Stanford Univ, Mol Imaging Program Stanford, Dept Radiol Biophys & Bio X Program, Sch Med, Stanford, CA 94305 USA
3.Peking Univ, Med Isotopes Res Ctr, Beijing 100091, Peoples R China
4.Purdue Univ, Sch Hlth Sci, W Lafayette, IN 47907 USA

Recommended Citation:
Liu, Zhaofei,Liu, Shuanglong,Wang, Fan,et al. Noninvasive imaging of tumor integrin expression using F-18-labeled RGD dimer peptide with PEG(4) linkers[J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,2009,36(8):1296-1307.
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