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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The Caenorhabditis elegans D2-like dopamine receptor DOP-2 physically interacts with GPA-14, a Gαi subunit
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Background
A human antibody against human endothelin receptor type A that exhibits antitumor potency
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“G protein-coupled receptors are the most pharmacologically active and extensively studied targets [9,10].”
Background
Revisiting the Sweet Taste Receptor T1R2-T1R3 through Molecular Dynamics Simulations Coupled with a Noncovalent Interactions Analysis
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“When neurotransmitters bind to these receptors, they cause a conformational change that results in activation of heterotrimeric G proteins, which in turn modulate the activity of effector proteins (Wettschureck and Offermanns 2005; Rosenbaum et al. 2009).”
Background
Structural Basis for the β-Adrenergic Receptor Subtype Selectivity of the Representative Agonists and Antagonists
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Desensitization and Trafficking of μ-Opioid Receptors in Locus Ceruleus Neurons: Modulation by Kinases
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Dimer-Dependent Intrinsic/Basal Activity of the Class B G Protein-Coupled Receptor PAC1 Promotes Cellular Anti-Apoptotic Activity through Wnt/β-Catenin Pathways that Are Associated with Dimer Endocytosis
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Adrenergic Signaling at the Interface of Allergic Asthma and Viral Infections
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Negative Feedback Phosphorylation of Gγ Subunit Ste18 and the Ste5 Scaffold Synergistically Regulates MAPK Activation in Yeast
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Identification of Alkaloids from Corydalis yanhusuo W. T. Wang as Dopamine D1 Receptor Antagonists by Using CRE-Luciferase Reporter Gene Assay
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“Because calcium mobilization occurs early in the signalling pathway, the FLIPR assay measures the early events of GPCR activation, including agonist–GPCR binding, G-protein activation, and second messenger release [27].”
Background
Human G protein-coupled receptor 30 is N-glycosylated and N-terminal domain asparagine 44 is required for receptor structure and activity
de Valdivia, E. G., Sandén, C., Kahn, R., Olde, B., & Leeb-Lundberg, L. M. F. (2019) · Bioscience Reports · doi:10.1042/bsr20182436 · Cited by 22
An Integrated Pan-Cancer Analysis and Structure-Based Virtual Screening of GPR15
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“G protein-coupled receptors (GPCRs), also known as seven-transmembrane domain receptors, constitute the largest family of cell signaling receptors [1].”
Background
Exploring the Activation Mechanism of a Metabotropic Glutamate Receptor Homodimer via Molecular Dynamics Simulation
Lei, T., Hu, Z., Ding, R., Chen, J., Li, S., Zhang, F., Pu, X., & Zhao, N. (2019) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.9b00425 · Cited by 22
Computational Investigations on the Binding Mode of Ligands for the Cannabinoid-Activated G Protein-Coupled Receptor GPR18
Neumann, A., Engel, V., Mahardhika, A. B., Schoeder, C. T., Namasivayam, V., Kieć‐Kononowicz, K., & Müller, C. E. (2020) · Biomolecules · doi:10.3390/biom10050686 · Cited by 23
Dysregulation of Ephrin receptor and PPAR signaling pathways in neural progenitor cells infected by Zika virus
Raman, S. N. T., Latreille, E., Gao, J., Zhang, W., Wu, J., Russell, M. S., Walrond, L. D., Cyr, T. D., Lavoie, J. R., Safronetz, D., et al. (2020) · Emerging Microbes & Infections · doi:10.1080/22221751.2020.1818631 · Cited by 22
“The G proteins α , β and γ are known transducers of the largest family of plasma membrane receptor molecules in eukaryotes called the G protein-coupled receptors (GPCR) [21].”
Influential
PAC1 Receptors: Shapeshifters in Motion
Liao, C., May, V., & Li, J. (2018) · Journal of Molecular Neuroscience · doi:10.1007/s12031-018-1132-0 · Cited by 23
“…to detect a multitude of extracellular instructional cues from neurotransmitters, hormones, paracrine regulators, light, odorants and tastants (Rosenbaum et al. 2009; Wacker et al. 2017; Katritch et al. 2013); hence, GPCRs are critical homeostatic regulators of nearly all physiological…”
Membrane interaction of the N-terminal domain of chemokine receptor CXCR1
Haldar, S., Raghuraman, H., Namani, T., Rajarathnam, K., & Chattopadhyay, A. (2010) · Biochimica et Biophysica Acta (BBA) - Biomembranes · doi:10.1016/j.bbamem.2010.02.029 · Cited by 22
Identification and CRISPR-Cas9 validation of a novel β-adrenergic-like octopamine receptor mutation associated with amitraz resistance in Varroa destructor
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HTR6 and SSTR3 targeting to primary cilia
Barbeito, P., & Garcia-Gonzalo, F. R. (2021) · Biochemical Society Transactions · doi:10.1042/bst20191005 · Cited by 20

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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