A near-infrared fluorogenic dimer enables background-free imaging of endogenous GPCRs in living mice.

Date publication

juillet 2020

Journal

Chemical science

Auteurs

Membres identifiés du Cancéropôle Est :
Dr BRASSE David , Dr BONNET Dominique , Dr KLYMCHENKO Andrey

Tous les auteurs :
Esteoulle L, Daubeuf F, Collot M, Riché S, Durroux T, Brasse D, Marchand P, Karpenko IA, Klymchenko AS, Bonnet D

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/33033597

Résumé

Fluorescent probes are commonly used in studying G protein-coupled receptors in living cells; however their application to the whole animal receptor imaging is still challenging. To address this problem, we report the design and the synthesis of the first near-infrared emitting fluorogenic dimer with environment-sensitive folding. Due to the formation of non-fluorescent H-aggregates in an aqueous medium, the near-infrared fluorogenic dimer displays a strong turn-on response (up to 140-fold) in an apolar environment and exceptional brightness: 56% quantum yield and ≈444 000 M cm extinction coefficient. Grafted on a ligand of the oxytocin receptor, it allows the unprecedented background-free and target-specific imaging of the naturally expressed receptor in living mice.

Référence

Chem Sci. 2020 Jul 14;11(26):6824-6829