Cited by 114Receptor Mechanisms and SignalingAdvanced Fluorescence Microscopy TechniquesNeuroscience and Neuropharmacology Research

Labeling and Single-Molecule Methods To Monitor G Protein-Coupled Receptor Dynamics

Tian, He, Fürstenberg, Alexandre, Huber, Thomas·2017·Chemical Reviews

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.

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Crossref · 10.1021/acs.chemrev.6b00084

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Authors
Tian, H., Fürstenberg, A., & Huber, T.
Affiliations
Rockefeller University (US)
Corresponding author
Huber, Thomas
Venue
Chemical Reviews
Published
2016-06-24
Volume
117
Issue
1
Pages
186-245
ISSN
  • 0009-2665 (ISSN-L)
  • 1520-6890
OpenAlex
W2460402577
Cited by
114
References
671
Citations by year
2026: 4 · 2025: 7 · 2024: 6 · 2023: 9 · 2022: 13 · 2021: 11 · 2020: 10 · 2019: 19 · 2018: 14 · 2017: 20 · 2016: 1
FWCI
1.66
Type
journal article
Language
en
Open access
closed
Locations
  • Chemical Reviews (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • National Eye Institute (R01 EY012049)
  • Novo Nordisk
  • Danica Foundation
  • Robertson Foundation
  • Crowley Family Fund
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Biophysics › Advanced Fluorescence Microscopy Techniques
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords
G protein-coupled receptors, single-molecule fluorescence, fluorescent dyes, chemical labeling, G protein-coupled receptor signaling, single-molecule fluorescence microscopy, chemical biology
MeSH terms
Fluorescent Dyes, Microscopy, Fluorescence, Signal Transduction, Receptors, G-Protein-Coupled

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