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学科主题: 公共卫生
题名:
F-18, Cu-64, and Ga-68 Labeled RGD-Bombesin Heterodimeric Peptides for PET Imaging of Breast Cancer
作者: Liu, Zhaofei1,2,3; Yan, Yongjun1,2; Liu, Shuanglong1,2; Wang, Fan3; Chen, Xiaoyuan1,2
刊名: BIOCONJUGATE CHEMISTRY
发表日期: 2009-05-01
DOI: 10.1021/bc9000245
卷: 20, 期:5, 页:1016-1025
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]: INTEGRIN ALPHA(V)BETA(3) EXPRESSION ; HUMAN PROSTATE ADENOCARCINOMA ; IN-VIVO EVALUATION ; TUMOR ANGIOGENESIS ; MOUSE MODEL ; CELL-LINES ; RECEPTOR ; MICROPET ; ANALOGS ; GRP
英文摘要:

Radiolabeled RGD (Arg-Gly-Asp) and bombesin (BBN) radiotracers that specifically target integrin alpha(v)beta(3) and gastrin releasing peptide receptor (GRPR) are both promising radiopharmaceuticals for tumor imaging. We recently designed and synthesized a RGD-BBN heterodimeric peptide with both RGD and BBN motifs in one single molecule. The F-18-labeled RGD-BBN heterodimer exhibited dual integrin alpha(v)beta(3) and GRPR targeting in a PC-3 prostate cancer model. In this study we investigated whether radiolabeled RGD-BBN tracers can be used to detect breast cancer by using microPET. Cell binding assay demonstrated that the high GRPR expressing breast cancer cells typically express low to moderate level of integrin a,03, while high integrin alpha(v)beta(3) expressing breast cancer cells have negligible level of GRPR. We labeled RGD-BBN heterodimer with three positron emitting radionuclides F-18, Cu-64, and Ga-68 and investigated the corresponding PET radiotracers in both orthotopic T47D (GRPR(+)/low integrin alpha(v)beta(3)) and MDA-MB-435 (GRPR(-)/integrin alpha(v)beta(+)(3)) breast cancer models. The three radiotracers all possessed in vitro dual integrin a alpha(v)beta(3) and GRPR binding affinity. The advantages of the RGD-BBN radiotracers over the corresponding BBN analogues are obvious for imaging MDA-MB-435 (GRPR(-)/integrin alpha(v)beta(+)(3)) tumor. F-18-FB-PEG(3)-RGD-BBN showed lower tumor uptake than Cu-64-NOTA-RGD-BBN and Ga-68-NOTA-RGD-BBN but was able to visualize breast cancer tumors with high contrast. Synthesis of Cu-64-NOTA-RGD-BBN and Ga-68-NOTA-RGD-BBN is much faster and easier than F-18-FB-PEG(3)-RGD-BBN. Cu-64-NOTA-RGD-BBN showed prolonged tumor uptake but also higher liver retention and kidney uptake than 68Ga-NOTA-RGD-BBN and F-18-FB-PEG(3)-RGD-BBN. Ga-68-NOTA-RGD-BBN possessed high tumor signals but also relatively high background uptake compared with the other two radiotracers. In summary, the prosthetic labeling groups, chelators, and isotopes all have a profound effect on the tumor targeting efficacy and in vivo kinetics of the RGD-BBN tracers for dual integrin and GRPR recognition. Further development of suitably labeled RGD-BBN tracers for PET imaging of cancer is warranted.

语种: 英语
所属项目编号: R01 120188 ; R01 CA119053 ; R21 CA121842 ; R21 CA102123 ; P50 CA1 14747 ; U54 CA1 19367 ; R24 CA93862
项目资助者: National Cancer Institute ; China Scholarship Council (CSC)
WOS记录号: WOS:000266292500023
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/51915
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, Sch Med, Mol Imaging Program Stanford, Dept Radiol, Stanford, CA 94305 USA
2.Stanford Univ, Sch Med, BioX Program, Stanford, CA 94305 USA
3.Peking Univ, Med Isotopes Res Ctr, Beijing 100191, Peoples R China

Recommended Citation:
Liu, Zhaofei,Yan, Yongjun,Liu, Shuanglong,et al. F-18, Cu-64, and Ga-68 Labeled RGD-Bombesin Heterodimeric Peptides for PET Imaging of Breast Cancer[J]. BIOCONJUGATE CHEMISTRY,2009,20(5):1016-1025.
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