Lighting Up the Plasma Membrane: Development and Applications of Fluorescent Ligands for Transmembrane Proteins

Despite the fact that transmembrane proteins represent main therapeutic targets for decades, complete and in-depth knowledge about their biochemical pharmacological profiling is not fully available. In this regard, target-tailored small-molecule fluorescent ligands are a viable approach to fill in missing pieces of puzzle. Such tools, coupled with ability high-precision optical techniques image an unprecedented resolution at single-molecule level, helped unraveling many conundrums related plasma proteins’ life-cycle druggability. Herein, we review recent progress made during last two decades ligand design potential applications fluorescence microscopy voltage-gated ion channels, ligand-gated channels G-coupled protein receptors.