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Ga-68-labeled NOTA-RGD-BBN peptide for dual integrin and GRPR-targeted tumor imaging
Liu, Zhaofei1,2,3; Niu, Gang1,2; Wang, Fan3; Chen, Xiaoyuan1,2
关键词Integrin alpha(v)beta(3) Gastrin releasing peptide receptor (GRPR) RGD peptide Bombesin Peptide heterodimer Positron emission tomography (PET) Gallium-68 (Ga-68)
刊名EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
2009-09-01
DOI10.1007/s00259-009-1123-z
36期:9页:1483-1494
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Radiology, Nuclear Medicine & Medical Imaging
资助者National Cancer Institute ; China Scholarship Council (CSC) ; National Cancer Institute ; China Scholarship Council (CSC)
研究领域[WOS]Radiology, Nuclear Medicine & Medical Imaging
关键词[WOS]POSITRON-EMISSION-TOMOGRAPHY ; BREAST-CANCER ; ALPHA(V)BETA(3) EXPRESSION ; PROSTATE-CANCER ; RECEPTOR EXPRESSION ; MDA-MB-435 CELLS ; MICROPET ; PET ; BOMBESIN ; HETERODIMER
英文摘要

Radiolabeled Arg-Gly-Asp (RGD) and bombesin (BBN) peptide analogs have been extensively investigated for the imaging of tumor integrin alpha(v)beta(3) and gastrin-releasing peptide receptor (GRPR) expression, respectively. Recently, we designed and synthesized a RGD-BBN heterodimeric peptide from c(RGDyK) and BBN(7-14) through a glutamate linker. The goal of this study was to investigate the dual receptor-targeting property and tumor diagnostic value of RGD-BBN heterodimeric peptide labeled with generator-eluted Ga-68 (t(1/2) 68 min, beta(+) 89% and EC 11%), Ga-68-NOTA-RGD-BBN.

RGD-BBN heterodimer was conjugated with 1,4,7-triazacyclononanetriacetic acid (NOTA) and labeled with Ga-68. The dual receptor binding affinity was investigated by a radioligand competition binding assay. The in vitro and in vivo dual receptor targeting of Ga-68-NOTA-RGD-BBN was evaluated and compared with that of Ga-68-NOTA-RGD and Ga-68-NOTA-BBN.

NOTA-RGD-BBN had integrin alpha(v)beta(3) and GRPR binding affinities comparable to those of the monomeric RGD and BBN, respectively. The dual receptor targeting property of Ga-68-NOTA-RGD-BBN was validated by blocking studies in a PC-3 tumor model. Ga-68-NOTA-RGD-BBN showed higher tumor uptake than Ga-68-NOTA-RGD and Ga-68-NOTA-BBN. Ga-68-NOTA-RGD-BBN can also image tumors with either integrin or GRPR expression.

Ga-68-NOTA-RGD-BBN exhibited dual receptor targeting properties both in vitro and in vivo. The favorable characterizations of Ga-68-NOTA-RGD-BBN such as convenient synthesis, high specific activity, and high tumor uptake, warrant its further investigation for clinical cancer imaging.

语种英语
所属项目编号NCI R01 CA119053 ; R21 CA121842 ; P50 CA114747 ; U54 CA119367
资助者National Cancer Institute ; China Scholarship Council (CSC) ; National Cancer Institute ; China Scholarship Council (CSC)
WOS记录号WOS:000268872200016
Citation statistics
Cited Times:82[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/64490
Collection北京大学医药卫生分析中心
作者单位1.Stanford Univ, Bio X Program, Sch Med, Stanford, CA 94305 USA
2.Stanford Univ, Dept Radiol, Sch Med, MIPS, Stanford, CA 94305 USA
3.Peking Univ, Med Isotopes Res Ctr, Beijing 100191, Peoples R China
Recommended Citation
GB/T 7714
Liu, Zhaofei,Niu, Gang,Wang, Fan,et al. Ga-68-labeled NOTA-RGD-BBN peptide for dual integrin and GRPR-targeted tumor imaging[J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,2009,36(9):1483-1494.
APA Liu, Zhaofei,Niu, Gang,Wang, Fan,&Chen, Xiaoyuan.(2009).Ga-68-labeled NOTA-RGD-BBN peptide for dual integrin and GRPR-targeted tumor imaging.EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,36(9),1483-1494.
MLA Liu, Zhaofei,et al."Ga-68-labeled NOTA-RGD-BBN peptide for dual integrin and GRPR-targeted tumor imaging".EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING 36.9(2009):1483-1494.
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