ArticleProceedings of the National Academy of Sciences of the United States of America2019
Stepwise activation of a class C GPCR begins with millisecond dimer rearrangement.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 54 citations in OpenAlex.
- Atomic, structural and molecular insights into GPCR ligand binding and signalling.Nature reviews. Molecular cell biology · 2026Review
- Design of a metabolically-stable peptide therapeutic with triple-hormone-receptor agonist activity.Journal of computer-aided molecular design · 2026Article
- Domain coupling in activation of a family C GPCR.Nature chemical biology · 2025Article
- Delineating the stepwise millisecond allosteric activation mechanism of the class C GPCR dimer mGlu5.Nature communications · 2024Article
- Structural basis of positive allosteric modulation of metabotropic glutamate receptor activation and internalization.Nature communications · 2024Article
- Article
- G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.Signal transduction and targeted therapy · 2024Review
- Identifiability of equilibrium constants for receptors with two to five binding sites.The Journal of general physiology · 2023Article
- Fast functional mapping of ligand-gated ion channels.Communications biology · 2023Article
- Concerted conformational changes control metabotropic glutamate receptor activity.Science advances · 2023Article
- Kinetic fingerprinting of metabotropic glutamate receptors.Communications biology · 2023Article
- Detecting and measuring of GPCR signaling - comparison of human induced pluripotent stem cells and immortal cell lines.Frontiers in endocrinology · 2023Review
- Functional modulation of PTH1R activation and signaling by RAMP2.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Nanobody-based sensors reveal a high proportion of mGlu heterodimers in the brain.Nature chemical biology · 2022Article
- Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2.eLife · 2022Article
- Enlightening activation gating in P2X receptors.Purinergic signalling · 2022Review
- Insights into Fluctuations of Structure of Proteins: Significance of Intermediary States in Regulating Biological Functions.Polymers · 2022Review
- Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state.Nature communications · 2021Article
- Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design.Nature communications · 2021Article
- Structural basis of GABANature · 2021Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
G protein-coupled receptors (GPCRs) are key biological switches that transmit both internal and external stimuli into the cell interior. Among the GPCRs, the "light receptor" rhodopsin has been shown to activate with a rearrangement of the transmembrane (TM) helix bundle within ∼1 ms, while all other receptors are thought to become activated within ∼50 ms to seconds at saturating concentrations. Here, we investigate synchronous stimulation of a dimeric GPCR, the metabotropic glutamate receptor type 1 (mGluR1), by two entirely different methods: (
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.