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学科主题: 公共卫生
题名:
Small-Animal PET of Tumors with (64Cu)-Labeled RGD-Bombesin Heterodimer
作者: Liu, Zhaofei1,2,3; Li, Zi-Bo1,2; Cao, Qizhen1,2; Liu, Shuanglong1,2; Wang, Fan3; Chen, Xiaoyuan1,2
关键词: RGD-BBN heterodimer ; bombesin ; positron emission tomography (PET) ; gastrin-releasing peptide receptor (GRPR) ; integrin alpha(v)beta(3) ; (64)Cu
刊名: JOURNAL OF NUCLEAR MEDICINE
发表日期: 2009-07-01
DOI: 10.2967/jnumed.108.061739
卷: 50, 期:7, 页:1168-1177
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]: RECEPTOR-POSITIVE TUMORS ; HUMAN PROSTATE ADENOCARCINOMA ; IN-VIVO EVALUATION ; PEPTIDE RECEPTOR ; INTEGRIN ALPHA(V)BETA(3) ; BIOLOGICAL EVALUATION ; MONOCLONAL-ANTIBODY ; CANCER CELLS ; MOUSE MODEL ; ANALOGS
英文摘要:

The overexpression of gastrin-releasing peptide receptor (GRPR) in various tumor types suggests that GRPR is an attractive target for cancer imaging and therapy with radiolabeled bombesin analogs. We recently reported the ability of (18)F-labeled RGD-bombesin heterodimer to be used for dual integrin alpha(v)beta(3)- and GRPR-targeted imaging. To further investigate the synergistic effect of the dual-receptor targeting of peptide heterodimers, we evaluated (64)Cu-labeled RGD-bombesin for PET imaging of tumors. Methods: RGD-bombesin was coupled with 1,4,7,10-tetraazacyclododecane-N, N ′, N ′′, N ′′′-tetraacetic acid (DOTA) and 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), and the conjugates were labeled with (64)Cu. The in vitro and in vivo characteristics of (64)Cu-NOTA-RGD-bombesin were compared with those of (64)Cu-NOTA-RGD, (64)Cu-NOTA-bombesin, and (64)Cu-DOTA-RGD-bombesin. Results: (64)Cu-NOTA-RGD-bombesin and (64)Cu-DOTA-RGD-bombesin had comparable dual integrin alpha(v)beta(3)- and GRPR-binding affinities in vitro, both of which were slightly lower than RGD for integrin binding and bombesin for GRPR binding. (64)Cu-NOTA-RGD-bombesin possessed significantly higher tumor uptake than did (64)Cu-NOTA-RGD, (64)Cu-NOTA-bombesin, the mixture of (64)Cu-NOTA-RGD and (64)Cu-NOTA-bombesin, or (64)Cu-DOTA-RGD-bombesin in PC-3 prostate cancer. (64)Cu-NOTA-RGD-bombesin also showed improved in vivo kinetics such as lower liver and intestinal activity accumulation than did the bombesin tracers. (64)Cu-NOTA-RGD-bombesin also outperformed (64)Cu-NOTA-RGD in a 4T1 murine mammary carcinoma model that expresses integrin on tumor vasculature but no GRPR in tumor tissue, which had no uptake of (64)Cu-NOTA-bombesin. Conclusion: Compared with other tracers, (64)Cu-NOTA-RGD-bombesin showed favorable in vivo kinetics and enhanced tumor uptake, which warrants its further investigation for targeting tumors that express integrin or GRPR or that coexpress integrin and GRPR for imaging and therapeutic applications. The synergistic effect of RGD-bombesin heterodimers observed in this study also encourages further investigations of novel heterodimers recognizing other cell surface receptors for tumor targeting.

语种: 英语
所属项目编号: NCI R01 120188 ; R01 CA119053 ; R21 CA121842 ; R21 CA102123 ; P50 CA114747 ; U54 CA119367 ; R24 CA93862
项目资助者: National Cancer Institute
WOS记录号: WOS:000272547100030
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60133
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, Bio X Program, Stanford, CA 94305 USA
2.Stanford Univ, Sch Med, Dept Radiol, Biophys Program,Mol Imaging Program Stanford, Stanford, CA 94305 USA
3.Peking Univ, Med Isotopes Res Ctr, Beijing 100871, Peoples R China

Recommended Citation:
Liu, Zhaofei,Li, Zi-Bo,Cao, Qizhen,et al. Small-Animal PET of Tumors with (64Cu)-Labeled RGD-Bombesin Heterodimer[J]. JOURNAL OF NUCLEAR MEDICINE,2009,50(7):1168-1177.
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