title: Labeling and Single-Molecule Methods To Monitor G Protein-Coupled Receptor Dynamics.
abstract: The superfamily of G protein-coupled receptors (GPCRs) mediates a wide range of physiological responses and serves as an important category of drug targets. Earlier biochemical and biophysical studies have shown that GPCRs exist temporally in an ensemble of interchanging conformations. Single-molecule techniques are ideally suited to understand the dynamic signaling and conformational complexity of G protein-coupled receptors (GPCRs). Here, we review the progress in single-molecule studies on GPCRs. We introduce the fundamental technical aspects of single-molecule fluorescence. We also survey the methodologies for labeling GPCRs with biophysical probes, particularly fluorescent dyes, and highlight the relevant chemical biology innovations that can be instrumental for studying GPCRs. Finally, we illustrate how the optical techniques and the labeling schemes have been combined to investigate GPCR signaling and dynamics at the single-molecule level.
authors.affiliation: Laboratory of Chemical Biology and Signal Transduction, The Rockefeller University , 1230 York Avenue, New York, New York 10065, United States.
authors.forename: He
authors.initials: H
authors.lastname: Tian
authors.affiliation: Laboratory of Chemical Biology and Signal Transduction, The Rockefeller University , 1230 York Avenue, New York, New York 10065, United States.
authors.forename: Alexandre
authors.initials: A
authors.lastname: Fürstenberg
authors.affiliation: Laboratory of Chemical Biology and Signal Transduction, The Rockefeller University , 1230 York Avenue, New York, New York 10065, United States.
authors.forename: Thomas
authors.initials: T
authors.lastname: Huber
mesh_terms: D005456:Fluorescent Dyes / Q000737:chemistry; D008856:Microscopy, Fluorescence; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry*; D015398:Signal Transduction
chemical_list: D005456:Fluorescent Dyes; D043562:Receptors, G-Protein-Coupled