@article{723a2311bbdb4df0ad5e70f7543a05d4,
title = "A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging",
abstract = "We have developed a novel radiogallium (Ga)-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging. A CXCR4 imaging probe with two CXCR4 antagonists (Ac-TZ14011) on Ga-DOTA core, Ga-DOTA-TZ2, was synthesized, and the affinity and binding to CXCR4 was evaluated in CXCR4 expressing cells in vitro. The affinity of Ga-DOTA-TZ2 for CXCR4 was 20-fold greater than the corresponding monovalent probe, Ga-DOTA-TZ1. 67Ga-DOTA-TZ2 showed the significantly higher accumulation in CXCR4-expressing tumor cells compared with 67Ga-DOTA-TZ1, suggesting the bivalent effect enhances its binding to CXCR4. The incorporation of two CXCR4 antagonists to Ga-DOTA could be effective in detecting CXCR4-expressing tumors.",
keywords = "Bivalent effect, CXCR4, DOTA, Radiogallium",
author = "Kohei Sano and Ryo Masuda and Hayato Hisada and Shinya Oishi and Kenta Shimokawa and Masahiro Ono and Nobutaka Fujii and Hideo Saji and Takahiro Mukai",
note = "Funding Information: We would like to thank FUJIFILM RI Pharma Co., Ltd, Tokyo, Japan , for donating 67 GaCl 3 . This work was supported in part by a Grant-in-Aid for Scientific Research (B) ( 21390347 ), a Grant-in-Aid for Scientific Research on Priority Areas from the Japan Society for the Promotion of Science , and the Project to Develop {\textquoteleft}Innovative Seeds{\textquoteright} of the Japan Science and Technology Agency . R.M. is grateful for Research Fellowships from the JSPS for Young Scientists . ",
year = "2014",
month = mar,
day = "1",
doi = "10.1016/j.bmcl.2014.01.031",
language = "English",
volume = "24",
pages = "1386--1388",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "5",
}