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The Molecular Basis of G Protein–Coupled Receptor Activation
Open accessAbstract
G protein–coupled receptors (GPCRs) mediate the majority of cellular responses to external stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein and promotes exchange of GTP for GDP, leading to dissociation of the G protein into α and βγ subunits that mediate downstream signals. GPCRs can also activate distinct signaling pathways through arrestins. Active states of GPCRs form by small rearrangements of the ligand-binding, or orthosteric, site that are amplified into larger conformational changes. Molecular understanding of the allosteric coupling between ligand binding and G protein or arrestin interaction is emerging from structures of several GPCRs crystallized in inactive and active states, spectroscopic data, and computer simulations. The coupling is loose, rather than concerted, and agonist binding does not fully stabilize the receptor in an active conformation. Distinct intermediates whose populations are shifted by ligands of different efficacies underlie the complex pharmacology of GPCRs.
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“However, a protein can exist in one conformation in its “inactive” state and another in its “active” state.53–56”
From AlphaFold 2: Why It Works and Its Implications for Understanding the Relationships of Protein Sequence, Structure, and Function (2021) · cites this paper as [55]
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Self-citationThe Energy Landscapes and Motions of Proteins
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Crystal structure of the β2 adrenergic receptor–Gs protein complex
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Metadata
- Authors
- Weis, W. I., & Kobilka, B. K.
- Affiliations
- Stanford Medicine (US)
- Corresponding author
- Kobilka, Brian K.
- Venue
- Annual Review of Biochemistry
- Publisher
- Annual Reviews
- Published
- 2018-06-20
- Volume
- 87
- Issue
- 1
- Pages
- 897-919
- ISSN
- 0066-4154 (ISSN-L)
- 1545-4509
- PMC
- PMC6535337
- OpenAlex
- W2809303314
- Cited by
- 1,227
- References
- 72
- Citations by year
- 2026: 160 · 2025: 191 · 2024: 183 · 2023: 174 · 2022: 151 · 2021: 161 · 2020: 124 · 2019: 71 · 2018: 11
- FWCI
- 9.03
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Annual Review of Biochemistry (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institutes of Health
- National Institute of General Medical Sciences (R01GM083118)
- National Institute of Neurological Disorders and Stroke (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, G protein activation, GTPase activity, arrestin, allosteric communication, receptor conformational change, ligand efficacy, GPCR pharmacology, G protein dissociation
- MeSH terms
- Allosteric Regulation, Binding Sites, Energy Metabolism, Humans, Ligands, Models, Molecular, Protein Conformation, Conserved Sequence, Crystallography, X-Ray, Receptors, G-Protein-Coupled
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