The DOI matches its Crossref record; 671 of the 675 references it cites were found in a registry or an index.
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.
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“GPCRs exist as an ensemble of temporally interchanging conformations [85].”
From G protein-coupled receptors function as cell membrane receptors for the steroid hormone 20-hydroxyecdysone (2020) · cites this paper as [85]
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Metadata
- Authors
- Tian, H., Fürstenberg, A., & Huber, T.
- Affiliations
- Rockefeller University (US)
- Corresponding author
- Huber, Thomas
- Venue
- Chemical Reviews
- Publisher
- American Chemical Society (ACS)
- Published
- 2016-06-24
- Volume
- 117
- Issue
- 1
- Pages
- 186-245
- ISSN
- 0009-2665 (ISSN-L)
- 1520-6890
- OpenAlex
- W2460402577
- Cited by
- 114
- References
- 675
- 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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