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

Kohei Sano, Ryo Masuda, Hayato Hisada, Shinya Oishi, Kenta Shimokawa, Masahiro Ono, Nobutaka Fujii, Hideo Saji, Takahiro Mukai

Research output: Contribution to journalArticle

3 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1386-1388
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number5
DOIs
Publication statusPublished - 2014 Mar 1
Externally publishedYes

Keywords

  • Bivalent effect
  • CXCR4
  • DOTA
  • Radiogallium

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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