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Noninvasive imaging of tumor integrin expression using F-18-labeled RGD dimer peptide with PEG(4) linkers
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
2009-08-01
DOI10.1007/s00259-009-1112-2
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
WOS记录号WOS:000267895700010
引用统计
被引频次:83[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/400002259/55455
专题北京大学医药卫生分析中心
北京大学基础医学院
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
推荐引用方式
GB/T 7714
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.
APA Liu, Zhaofei,Liu, Shuanglong,Wang, Fan,Liu, Shuang,&Chen, Xiaoyuan.(2009).Noninvasive imaging of tumor integrin expression using F-18-labeled RGD dimer peptide with PEG(4) linkers.EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,36(8),1296-1307.
MLA Liu, Zhaofei,et al."Noninvasive imaging of tumor integrin expression using F-18-labeled RGD dimer peptide with PEG(4) linkers".EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING 36.8(2009):1296-1307.
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