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Dual Integrin and Gastrin-Releasing Peptide Receptor Targeted Tumor Imaging Using F-18-labeled PEGylated RGD-Bombesin Heterodimer F-18-FB-PEG(3)-Glu-RGD-BBN
Liu, Zhaofei1,2,3; Yan, Yongjun1,2; Chin, Frederic T.1,2; Wang, Fan3; Chen, Xiaoyuan1,2
刊名JOURNAL OF MEDICINAL CHEMISTRY
2009-01-22
DOI10.1021/jm801285t
52期:2页:425-432
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]HUMAN PROSTATE ADENOCARCINOMA ; POSITRON-EMISSION-TOMOGRAPHY ; ALPHA(V)BETA(3) EXPRESSION ; HUMAN BREAST ; ALPHA-V-BETA-3 INTEGRIN ; CANCER ; MICROPET ; PET ; ANGIOGENESIS ; CARCINOMA
英文摘要

Radiolabeled RGD and bombesin peptides have been extensively investigated for tumor integrin alpha(v)beta(3) and GRPR imaging, respectively. Due to the fact that many tumors are both integrin and GRPR positive, we designed and synthesized a heterodimeric peptide Glu-RGD-BBN, which is expected to be advantageous over the monomeric peptides for dual-receptor targeting. A PEG(3) spacer was attached to the glutamate a-amino group of Glu-RGD-BBN to enhance the F-18 labeling yield and to improve the in vivo kinetics. PEG(3)-Glu-RGD-BBN possesses the comparable GRPR and integrin alpha(v)beta(3) receptor-binding affinities as the corresponding monomers, respectively. The dual-receptor targeting properties of F-18-FB-PEG(3)-Glu-RGD-BBN were observed in PC-3 tumor model. F-18-FB-PEG(3)-Glu-RGD-BBN with high tumor contrast and favorable pharmacokinetics is a promising PET tracer for dual integrin and GRPR positive tumor imaging. This heterodimer strategy may also be an applicable method to develop other molecules with improved in vitro and in vivo characterizations for tumor diagnosis and therapy.

语种英语
WOS记录号WOS:000262522100022
引用统计
被引频次:72[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/61561
专题北京大学医药卫生分析中心
北京大学基础医学院
作者单位1.Stanford Univ, Sch Med, MIPS, 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 100083, Peoples R China
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GB/T 7714
Liu, Zhaofei,Yan, Yongjun,Chin, Frederic T.,et al. Dual Integrin and Gastrin-Releasing Peptide Receptor Targeted Tumor Imaging Using F-18-labeled PEGylated RGD-Bombesin Heterodimer F-18-FB-PEG(3)-Glu-RGD-BBN[J]. JOURNAL OF MEDICINAL CHEMISTRY,2009,52(2):425-432.
APA Liu, Zhaofei,Yan, Yongjun,Chin, Frederic T.,Wang, Fan,&Chen, Xiaoyuan.(2009).Dual Integrin and Gastrin-Releasing Peptide Receptor Targeted Tumor Imaging Using F-18-labeled PEGylated RGD-Bombesin Heterodimer F-18-FB-PEG(3)-Glu-RGD-BBN.JOURNAL OF MEDICINAL CHEMISTRY,52(2),425-432.
MLA Liu, Zhaofei,et al."Dual Integrin and Gastrin-Releasing Peptide Receptor Targeted Tumor Imaging Using F-18-labeled PEGylated RGD-Bombesin Heterodimer F-18-FB-PEG(3)-Glu-RGD-BBN".JOURNAL OF MEDICINAL CHEMISTRY 52.2(2009):425-432.
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