Cited by 2,534Receptor Mechanisms and SignalingProtein Kinase Regulation and GTPase SignalingNeuroscience and Neuropharmacology Research

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The structure and function of G-protein-coupled receptors

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Rosenbaum, Daniel M., Rasmussen, Søren G. F., Kobilka, Brian K.·2009·Nature

DOI 10.1038/nature08144PMC PMC3967846

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Abstract

G-protein-coupled receptors (GPCRs) mediate most of our physiological responses to hormones, neurotransmitters and environmental stimulants, and so have great potential as therapeutic targets for a broad spectrum of diseases. They are also fascinating molecules from the perspective of membrane-protein structure and biology. Great progress has been made over the past three decades in understanding diverse GPCRs, from pharmacology to functional characterization in vivo. Recent high-resolution structural studies have provided insights into the molecular mechanisms of GPCR activation and constitutive activity.

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Background

Authors: Rosenbaum, D. M., Rasmussen, S. G. F., & Kobilka, B. K.
Affiliations: Stanford Medicine (US)
ORCID: Rasmussen, Søren G. F.
Kobilka, Brian K.
Venue: Nature
Publisher: Springer Science and Business Media LLC
Published: 2009-05
Volume: 459
Issue: 7245
Pages: 356-363
ISSN: 0028-0836 (ISSN-L)
1476-4687
DOI: 10.1038/nature08144
PMC: PMC3967846
OpenAlex: W1988097700
Cited by: 2,534
References: 73
Citations by year: 2026: 108 · 2025: 171 · 2024: 175 · 2023: 140 · 2022: 196 · 2021: 177 · 2020: 150 · 2019: 172 · 2018: 122 · 2017: 136 · 2016: 132 · 2015: 120 · 2014: 133 · 2013: 135 · 2012: 146
FWCI: 11.79
Type: journal article
Language: en
Open access: green
europepmc.org
Licence: www.springer.com/tdm (tdm)
Locations: Nature (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
RePEc: Research Papers in Economics (submittedVersion)
Funders: Lundbeckfonden (R19-2008-2113)
National Institute of General Medical Sciences (F32GM082028, R01GM083118)
National Institute of Neurological Disorders and Stroke (R01NS28471, R01NS028471)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords: G protein-coupled receptors, GPCR structure, GPCR activation, constitutive activity, membrane protein structure, therapeutic target, hormone signaling, neurotransmitter signaling
MeSH terms: Animals, Cytoplasm, Humans, Protein Conformation, Signal Transduction, Conserved Sequence, Receptors, G-Protein-Coupled, Opsins

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The structure and function of G-protein-coupled receptors

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