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(99m)Technetium-HYNIC(tricine/TPPTS)-Aca-Bombesin(7-14) as a Targeted Imaging Agent with MicroSPECT in a PC-3 Prostate Cancer Xenograft Model
Ananias, Hildo J. K.1; Yu, Zilin2; Dierckx, Rudi A.2; van der Wiele, Christophe3; Helfrich, Wijnand4; Wang, Fan5; Tan, Yongjun6; Chen, Xiaoyuan6; de Jong, Igle J.1; Elsinga, Philip H.2
关键词bombesin prostate cancer imaging SPECT microSPECT GRPR GRP
刊名MOLECULAR PHARMACEUTICS
2011-07-01
DOI10.1021/mp200014h
8期:4页:1165-1173
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Medicine, Research & Experimental ; Pharmacology & Pharmacy
研究领域[WOS]Research & Experimental Medicine ; Pharmacology & Pharmacy
关键词[WOS]GASTRIN-RELEASING-PEPTIDE ; RADIOLABELED BOMBESIN ANALOGS ; PELVIC LYMPH-NODES ; RECEPTOR ANTAGONIST ; POSITIVE TUMORS ; BONE METASTASES ; IN-VITRO ; GRP ; RADIOPHARMACEUTICALS ; DIAGNOSIS
英文摘要

The peptide bombesin (BN) and derivates thereof show high binding affinity for the gastrin-releasing peptide receptor (GRPR), which is highly expressed in primary and metastasized prostate cancer. We have synthesized a new BN-based radiopharmaceutical (99m)technetium-HYNIC(tricine/TPPTS)-Aca-BN(7-14) (Tc-99m-HABN) and evaluated its GRPR targeting properties in vitro and in a xenograft tumor model for human prostate cancer in athymic mice. Tc-99m-HABN was synthesized, and its lipophilicity and stability were investigated. The IC50, internalization and efflux properties were determined in vitro using the GRPR expressing human prostate cancer cell line PC-3. Tc-99m-HABN biodistribution and microSPECT imaging were performed in PC-3 tumor-bearing athymic mice. Tc-99m-HABN was prepared with high labeling yield (>90%), hip radiochemical purity (>95%) and a specific activity of similar to 19.8 MBq/nmol. The partition coefficient log D value was -1.60 +/- 0.06. Tc-99m-HABN proved to be stable in human serum for 6 h. The IC50 of HYNIC-Aca-BN(7-14) was 12.81 +/- 0.14 nM. Incubation of PC-3 cells with Tc-99m-HABN demonstrated rapid cellular internalization and a long intracellular retention time. When mice were injected with Tc-99m-HABN, the activity was predominantly cleared via the kidneys. Uptake in the tumor was 2.24 +/- 0.64% ID/g after 30 min, with a steady decrease during the 4 h study period. In vivo experiments with a blocking agent showed GRPR mediated uptake. Tc-99m-HABN microSPECT imaging resulted in clear delineation of the tumor. Tc-99m-HABN is a novel BN-based radiopharmaceutical that proved to be suitable for targeted imaging of prostate cancer with microSPECT using the human prostate cancer cell line PC-3 in a xenograft mouse model.

语种英语
WOS记录号WOS:000293307400019
引用统计
被引频次:20[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/400002259/64161
专题北京大学医药卫生分析中心
作者单位1.Univ Groningen, Univ Med Ctr Groningen, Dept Urol, NL-9713 AV Groningen, Netherlands
2.Univ Groningen, Univ Med Ctr Groningen, Dept Nucl Med & Mol Imaging, NL-9713 AV Groningen, Netherlands
3.Ghent Univ Hosp, Dept Nucl Med, B-9000 Ghent, Belgium
4.Univ Groningen, Univ Med Ctr Groningen, Surg Res Lab, NL-9713 AV Groningen, Netherlands
5.Peking Univ, Med Isotopes Res Ctr, Beijing, Peoples R China
6.Natl Inst Biomed Imaging & Bioengn, Lab Mol Imaging & Nanomed, NIH, Bethesda, MD USA
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Ananias, Hildo J. K.,Yu, Zilin,Dierckx, Rudi A.,et al. (99m)Technetium-HYNIC(tricine/TPPTS)-Aca-Bombesin(7-14) as a Targeted Imaging Agent with MicroSPECT in a PC-3 Prostate Cancer Xenograft Model[J]. MOLECULAR PHARMACEUTICS,2011,8(4):1165-1173.
APA Ananias, Hildo J. K..,Yu, Zilin.,Dierckx, Rudi A..,van der Wiele, Christophe.,Helfrich, Wijnand.,...&Elsinga, Philip H..(2011).(99m)Technetium-HYNIC(tricine/TPPTS)-Aca-Bombesin(7-14) as a Targeted Imaging Agent with MicroSPECT in a PC-3 Prostate Cancer Xenograft Model.MOLECULAR PHARMACEUTICS,8(4),1165-1173.
MLA Ananias, Hildo J. K.,et al."(99m)Technetium-HYNIC(tricine/TPPTS)-Aca-Bombesin(7-14) as a Targeted Imaging Agent with MicroSPECT in a PC-3 Prostate Cancer Xenograft Model".MOLECULAR PHARMACEUTICS 8.4(2011):1165-1173.
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