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学科主题: 公共卫生
题名:
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
作者: Liu, Zhaofei1,2,3; Yan, Yongjun1,2; Chin, Frederic T.1,2; Wang, Fan3; Chen, Xiaoyuan1,2
刊名: JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2009-01-22
DOI: 10.1021/jm801285t
卷: 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
所属项目编号: R01 120188 ; R01 CA119053 ; R21 CA121842 ; R21 CA102123 ; P50CA1 14747 ; U54CA1 19367 ; R24 CA93862 ; W81XWH-07-1-0374 ; W81XWH-04-1-0697 ; W81XWH-06-1-0665 ; W81XWH-06-1-0042
项目资助者: National Cancer Institute (NCI) ; Department of Defense (DOD) ; China Scholarship Council (CSC)
WOS记录号: WOS:000262522100022
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/61561
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, 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

Recommended Citation:
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.
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