Fluorogenic squaraine dendrimers for background-free imaging of integrin receptors in cancer cells.
Fiche publication
Date publication
février 2021
Journal
Chemistry (Weinheim an der Bergstrasse, Germany)
Auteurs
Membres identifiés du Cancéropôle Est :
Dr KLYMCHENKO Andrey
Tous les auteurs :
Ashokkumar P, Collot M, Klymchenko AS
Lien Pubmed
Résumé
To overcome the limited brightness of existing fluorogenic molecular probes for biomolecular targets, we introduce a concept of fluorogenic dendrimer probe, which undergoes polarity-dependent switching due to intramolecular aggregation-caused quenching of its fluorophores. Based on a rational design of dendrimers with four and eight squaraine dyes, we found that octamer bearing dyes through a sufficiently long PEG(8) linker displays >400-fold fluorescence enhancement from water to non-polar dioxane. High extinction coefficient (~2,300,000 M -1 cm -1 ) resulted from eight squaraine dyes and quantum yield (~25%) make this octamer the brightest environment-sensitive fluorogenic molecule reported to date. Its conjugate with cyclic RGD used at low concentration (3 nM) enables integrin-specific fluorescence imaging of cancer cells with high signal-to-background ratio. The developed dendrimer probe is a "golden middle" between molecular probes and nanoparticles, combining small size, turn-on response and high brightness, important for bioimaging.
Mots clés
Dendrimers, Fluorogenic response, aggregation, fluorescent probes, integrin receptor
Référence
Chemistry. 2021 Feb 10;: