Lighting Up the Plasma Membrane: Development and Applications of Fluorescent Ligands for Transmembrane Proteins
Carlotta Borgarelli, Yvonne E. Klingl, Abril Escamilla‐Ayala, Sebastian Munck, Ludo Van Den Bosch, Wim M. De Borggraeve, Ermal Ismalaj
Abstract
Despite the fact that transmembrane proteins represent the main therapeutic targets for decades, complete and in-depth knowledge about their biochemical and pharmacological profiling is not fully available. In this regard, target-tailored small-molecule fluorescent ligands are a viable approach to fill in the missing pieces of the puzzle. Such tools, coupled with the ability of high-precision optical techniques to image with an unprecedented resolution at a single-molecule level, helped unraveling many of the conundrums related to plasma proteins' life-cycle and druggability. Herein, we review the recent progress made during the last two decades in fluorescent ligand design and potential applications in fluorescence microscopy of voltage-gated ion channels, ligand-gated ion channels and G-coupled protein receptors.