Click‐Functionalized Cyanine Fluorogenic Dimers for Improved Detection of GPCRs: Application to Imaging of ApelinR in Living Cells
Year: 2025
Type: article
Abstract: Fluorogenic dimers enable background-free imaging of biological targets under wash-free conditions owing to a strong fluorescence enhancement in the apolar cell microenvironment. However, it is crucial that the imaging probe interacts solely with the target receptor to avoid nonspecific interactions and ensure detection with a high signal-to-noise ratio. Herein, we describe a convenient and rapid approach for the synthesis of various functionalized cyanine dyes by click chemistry allowing the fine-tuning of the physicochemical and fluorogenic properties of the dimers. A structure-interaction relationship study was conducted for the fluorogenic dimers in the presence of bovine serum albumin (BSA) and liposomes as models of serum proteins and cell membranes. We identified d─Cy─E which combined the lowest nonspecific interactions with the optimal fluorescence turn-on properties. By conjugating d─Cy─E to a peptide ligand of the apelin GPCR, we developed Ap─d─Cy─E, the first fluorescent turn-on probe for the background-free imaging of this receptor in living cells.
Source: Chemistry - A European Journal
Language: English
Subfield: Spectroscopy
Field: Chemistry
Domain: Physical Sciences
Open Access status: hybrid
Estimated APC paid: $4,640
Awards: G1031727345, G164444715, G1921297134, Par-delà les frontières, l'Université de Strasbourg, G2255650664, Cross-talk between the CXCL12 chemokine receptors CXCR4 and ACKR3: contribution of oligomers populations to receptors signaling and function, G2659019386, G2694206344, Façonner les talents en formation et en recherche à l'Université de Strasbourg, G3357951378, G399734812, G471331628, G6136357505, G6276897512, G6803667113, Ecole Universitaire de Recherche Interdisciplinaire sur la Douleur, G7240651115
OpenAlex ID: W4409742468