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Tc-99m-Labeled RGD-BBN Peptide for Small-Animal SPECT/CT of Lung Carcinoma
Liu, Zhaofei1,2; Huang, Jinming1,2; Dong, Chengyan1,2; Cui, Liyang1,2; Jin, Xiaona3; Jia, Bing1,2; Zhu, Zhaohui3; Li, Fang3; Wang, Fan1,2
关键词Rgd-bombesin Integrin Alpha(v)Beta(3) Grpr Lung Carcinoma Single-photon Emission Computed Tomography (Spect)
刊名MOLECULAR PHARMACEUTICS
2012-05-01
DOI10.1021/mp200661t
9期:5页:1409-1417
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Medicine, Research & Experimental ; Pharmacology & Pharmacy
资助者National Natural Science Foundation of China (NSFC) ; Outstanding Youth Fund ; "973" project ; Ministry of Science and Technology of China ; National Natural Science Foundation of China (NSFC) ; Outstanding Youth Fund ; "973" project ; Ministry of Science and Technology of China
研究领域[WOS]Research & Experimental Medicine ; Pharmacology & Pharmacy
关键词[WOS]GASTRIN-RELEASING-PEPTIDE ; BOMBESIN HETERODIMER ; TUMOR-CELLS ; CANCER ; PET ; INFLAMMATION ; F-18-FDG ; FDG ; INTEGRIN ; EXPRESSION
英文摘要

We recently designed and synthesized a Gluc(RGDyK)-bombesin (RGD-BBN) heterodimeric peptide exhibiting a dual integrin alpha(v)beta(3) and gastrin-releasing peptide receptor (GRPR) targeting property. In this study, we investigated whether Tc-99m-labeled RGD-BBN peptide could be used for the non-invasive detection of lung carcinoma by using small-animal single-photon emission computed tomography (SPECT)/CT. RGD-BBN peptide was conjugated with 6-hydrazinonicotinyl (HYNIC) and then radiolabeled with Tc-99m using tricine and TPPTS as the coligands (TPPTS = trisodium triphenylphosphine-3,3′,3 ′′-trisulfonate). The biodistribution, planar gamma imaging, and small-animal SPECT/CT studies of Tc-99m-HYNIC(tricine)(TPPTS)-RGD-BBN (Tc-99m-RGD-BBN) were performed in C57/BL6 mice bearing Lewis lung carcinoma (LLC) or bearing both inflammation and LLC. HYNIC-RGD-BBN possessed a dual integrin alpha(v)beta(3) and GRPR binding capacity. Tc-99m-RGD-BBN was prepared with a high radiochemical purity (>98%), and it exhibited specific tumor imaging with high contrast to the contralateral background. Tc-99m-RGD-BBN was superior to F-18-FDG for distinguishing lung carcinoma from inflammation. The uptake of Tc-99m-RGD-BBN in LLC xenografts was 2.69 +/- 0.66% ID/g at 1 h postinjection (p.i.) and was decreased to 1.99 +/- 0.61% ID/g at 2 h p.i. The inflammation uptake of Tc-99m-RGD-BBN was 1.20 +/- 0.32% ID/g at 1 h and 0.56 +/- 0.17% ID/g at 2 h p.i., respectively. High pancreas uptake (25.76 +/- 5.49%ID/g and 19.56 +/- 6.78% ID/g at 1 and 2 h p.i., respectively) was also found due to the high GRPR expression of this organ. Small-animal SPECT/CT using Tc-99m-RGD-BBN can specifically detect the LLC pulmonary metastases. Our results suggested that SPECT/CT with Tc-99m-RGD-BBN would provide an effective approach for the noninvasive detection of lung cancer.

语种英语
所属项目编号81000625 ; 30930030 ; 30870728 ; 30900373 ; 81028009 ; 81125011 ; 2011CB707703 ; 2009ZX09103-733 ; 2012ZX09102301-018 ; 2011YQ030114
资助者National Natural Science Foundation of China (NSFC) ; Outstanding Youth Fund ; "973" project ; Ministry of Science and Technology of China ; National Natural Science Foundation of China (NSFC) ; Outstanding Youth Fund ; "973" project ; Ministry of Science and Technology of China
WOS记录号WOS:000303961100035
Citation statistics
Cited Times:27[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/400002259/51058
Collection北京大学医药卫生分析中心
作者单位1.Peking Univ, Med Isotopes Res Ctr, Beijing 100191, Peoples R China
2.Peking Univ, Sch Basic Med Sci, Dept Radiat Med, Beijing 100191, Peoples R China
3.Beijing Union Med Coll Hosp, Dept Nucl Med, Beijing 100857, Peoples R China
Recommended Citation
GB/T 7714
Liu, Zhaofei,Huang, Jinming,Dong, Chengyan,et al. Tc-99m-Labeled RGD-BBN Peptide for Small-Animal SPECT/CT of Lung Carcinoma[J]. MOLECULAR PHARMACEUTICS,2012,9(5):1409-1417.
APA Liu, Zhaofei.,Huang, Jinming.,Dong, Chengyan.,Cui, Liyang.,Jin, Xiaona.,...&Wang, Fan.(2012).Tc-99m-Labeled RGD-BBN Peptide for Small-Animal SPECT/CT of Lung Carcinoma.MOLECULAR PHARMACEUTICS,9(5),1409-1417.
MLA Liu, Zhaofei,et al."Tc-99m-Labeled RGD-BBN Peptide for Small-Animal SPECT/CT of Lung Carcinoma".MOLECULAR PHARMACEUTICS 9.5(2012):1409-1417.
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