A Fluorescent Probe for Rapid, High-Contrast Visualization of Folate-Receptor-Expressing Tumors Inâ
Vivo.
Angew Chem Int Ed Engl
; 59(15): 6015-6020, 2020 04 06.
Article
em En
| MEDLINE
| ID: mdl-31984590
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 inâ
vivo, the near-infrared (NIR) region (650-900â
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 30â
min. Thus, FolateSiR-1 has the potential to contribute to the research in the field of biology and the clinical medicine.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Regulação Neoplásica da Expressão Gênica
/
Imagem Molecular
/
Receptores de Folato com Âncoras de GPI
/
Razão Sinal-Ruído
/
Corantes Fluorescentes
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Ano de publicação:
2020
Tipo de documento:
Article