Issue 26, 2020

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

Abstract

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−1 cm−1 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.

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

Supplementary files

Article information

Article type
Edge Article
Submitted
20 févr. 2020
Accepted
30 mai 2020
First published
17 juin 2020
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2020,11, 6824-6829

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

L. Esteoulle, F. Daubeuf, M. Collot, S. Riché, T. Durroux, D. Brasse, P. Marchand, J. Karpenko, A. S. Klymchenko and D. Bonnet, Chem. Sci., 2020, 11, 6824 DOI: 10.1039/D0SC01018A

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