A Fluorescent Probe for Rapid, High-Contrast Visualization of Folate-Receptor-Expressing Tumors In Vivo

Koji Numasawa, Kenjiro Hanaoka, Naoko Saito, Yoshifumi Yamaguchi, Takayuki Ikeno, Honami Echizen, Masahiro Yasunaga, Toru Komatsu, Tasuku Ueno, Masayuki Miura, Tetsuo Nagano, Yasuteru Urano

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)

Abstract

Folate receptors (FRs) are membrane proteins involved in folic acid uptake, and the alpha isoform (FR-α) is overexpressed in ovarian and endometrial cancer cells. For fluorescence imaging of FRs in vivo, the near-infrared (NIR) region (650–900 nm), in which tissue penetration is high and autofluorescence is low, is optimal, but existing NIR fluorescent probes targeting FR-α show high non-specific tissue adsorption, and require prolonged washout to visualize tumors. We have designed and synthesized a new NIR fluorescent probe, FolateSiR-1, utilizing a Si-rhodamine fluorophore having a carboxy group at the benzene moiety, coupled to a folate ligand moiety through a negatively charged tripeptide linker. This probe exhibits very low background fluorescence and afforded a tumor-to-background ratio (TBR) of up to 83 in FR-expressing tumor-bearing mice within 30 min. Thus, FolateSiR-1 has the potential to contribute to the research in the field of biology and the clinical medicine.

Original languageEnglish
Pages (from-to)6015-6020
Number of pages6
JournalAngewandte Chemie - International Edition
Volume59
Issue number15
DOIs
Publication statusPublished - 2020 Apr 6
Externally publishedYes

Keywords

  • cancer
  • chromophores
  • fluorescent probes
  • imaging
  • vitamins

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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