A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging

作者：Sano Kohei; Masuda Ryo; Hisada Hayato; Oishi Shinya; Shimokawa Kenta; Ono Masahiro; Fujii Nobutaka; Saji Hideo; Mukai Takahiro^*

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(5): 1386-1388.

DOI：10.1016/j.bmcl.2014.01.031

• Radiogallium
• DOTA
• CXCR4
• Bivalent effect

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. Ga-67-DOTA-TZ2 showed the significantly higher accumulation in CXCR4-expressing tumor cells compared with Ga-67-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.

• 出版日期2014-3-1