Online ISSN: 1884-4111 Print ISSN: 0033-8303
Radioisotopes 65(6): 247-255 (2016)


金属放射性核種で標識した蛋白質プローブを用いたHaloTag技術のインビボ分子イメージングへの応用Application of HaloTag® Technology to in Vivo Molecular Imaging Using Protein Probes Labeled by Metallic Radionuclides

1国立がん研究センター先端医療開発センター機能診断開発分野Division of Functional Imaging, National Cancer Center ◇ 277–8577 千葉県柏市柏の葉6–5–1 ◇ 6–5–1 Kashiwanoha, Kashiwa-shi, Chiba Pref. 277–8577, Japan

2東京工業大学大学院生命理工学研究科生体分子機能学専攻Department of Biomolecular Engineering, 
Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology ◇ 226–8501 神奈川県横浜市緑区長津田町4259–B60 ◇ 4259–B60 Nagatsuda-cho, Midori-ku, Yokohama-shi, Kanagawa Pref. 226–8501, Japan

受付日:2015年12月15日Received: December 15, 2015
受理日:2016年3月9日Accepted: March 9, 2016
発行日:2016年6月15日Published: June 15, 2016


We are developing new protein probes for in vivo radionuclide imaging using HaloTag® interchangeable labeling system. The selective and rapid bond formation between the HaloTag protein and HaloTag ligands can be applied to a more sophisticated labeling method for protein probes as a substitute of avidin–biotin interaction. For this purpose, we propose to use HaloTag-fusion proteins, which comprise targeting domain and HaloTag domain. In this study, we synthesized 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)–HaloTag ligands that could chelate radioactive metals useful for in vivo imaging. DOTA–HaloTag ligands were actually labeled with 111In efficiently, and the labeled ligands were successfully conjugated to a POH protein, which is a protein probe designed for imaging of hypoxia inducible factor-1α activity. The obtained 111In-labeled HaloTag-POH protein probes actually accumulated in implanted tumors in mice, which were visualized by single photon emission computed tomography (SPECT).

Key words: HaloTag; HaloTag ligand; Interchangeable labeling system; metal-chelate; in vivo imaging; multimodality imaging

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