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Small-Animal PET of Tumors with (64Cu)-Labeled RGD-Bombesin Heterodimer
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
2009-07-01
DOI10.2967/jnumed.108.061739
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
资助者National Cancer Institute ; National Cancer Institute
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
资助者National Cancer Institute ; National Cancer Institute
WOS记录号WOS:000272547100030
Citation statistics
Cited Times:85[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/400002259/60133
Collection北京大学医药卫生分析中心
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
GB/T 7714
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.
APA Liu, Zhaofei,Li, Zi-Bo,Cao, Qizhen,Liu, Shuanglong,Wang, Fan,&Chen, Xiaoyuan.(2009).Small-Animal PET of Tumors with (64Cu)-Labeled RGD-Bombesin Heterodimer.JOURNAL OF NUCLEAR MEDICINE,50(7),1168-1177.
MLA Liu, Zhaofei,et al."Small-Animal PET of Tumors with (64Cu)-Labeled RGD-Bombesin Heterodimer".JOURNAL OF NUCLEAR MEDICINE 50.7(2009):1168-1177.
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