Premium
A Fluorescent Probe for Rapid, High‐Contrast Visualization of Folate‐Receptor‐Expressing Tumors In Vivo
Author(s) -
Numasawa Koji,
Hanaoka Kenjiro,
Saito Naoko,
Yamaguchi Yoshifumi,
Ikeno Takayuki,
Echizen Honami,
Yasunaga Masahiro,
Komatsu Toru,
Ueno Tasuku,
Miura Masayuki,
Nagano Tetsuo,
Urano Yasuteru
Publication year - 2020
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201914826
Subject(s) - folate receptor , fluorescence , in vivo , fluorophore , chemistry , linker , biophysics , autofluorescence , fluorescence lifetime imaging microscopy , moiety , molecular probe , preclinical imaging , receptor , rhodamine , biochemistry , cancer cell , biology , stereochemistry , cancer , dna , genetics , physics , microbiology and biotechnology , quantum mechanics , computer science , operating system
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.