Lighting Up the Plasma Membrane: Development and Applications of Fluorescent Ligands for Transmembrane Proteins |
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| Authors: | Carlotta Borgarelli Yvonne E Klingl Dr Abril Escamilla-Ayala Prof?Dr Sebastian Munck Prof?Dr Ludo Van Den Bosch Prof?Dr Wim M De Borggraeve Dr Ermal Ismalaj |
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| Institution: | 1. Department of Chemistry, Molecular Design and Synthesis, KU Leuven Campus Arenberg Celestijnenlaan 200F –, box 2404, 3001 Leuven, Belgium;2. Department of Neurosciences, Experimental Neurology and Leuven Brain Institute (LBI), KU Leuven Campus Gasthuisberg O&N5 –, box 602 Herestraat 49, 3000 Leuven, Belgium;3. Center for Brain & Disease Research, & VIB BioImaging Core, VIB-KU Leuven Campus Gasthuisberg O&N5 –, box 602 Herestraat 49, 3000 Leuven, Belgium;4. Laboratory of Neurobiology, VIB, Center for Brain &, Disease Research, VIB-KU Leuven Campus Gasthuisberg O&N5 –, box 602 Herestraat 49, 3000 Leuven, Belgium |
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| 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. |
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| Keywords: | fluorescent ligands fluorescence imaging GPCRs ion channels transmembrane receptors |
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