ArticleNature chemical biology2011
Inactive-state preassembly of G(q)-coupled receptors and G(q) heterotrimers.
Article in Nature chemical biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 86 papers.
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Who cites it
86 citing papers in PubMed, 159 citations in OpenAlex.
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- G Protein-Mediated Allosteric Modulation of Ligand Binding in Class A GPCRs: Receptor-Ligand-Transducer Ensembles in Disease and Drug Discovery.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Role of Latrophilin-1 and Latrophilin-2 as Downstream Effectors of Androgen Receptor Signaling in Urothelial Tumorigenesis.Cancer reports (Hoboken, N.J.) · 2026Article
- Heterotrimeric G proteins containing Gβ1γ2 subunits exhibit subtype-specific mobility differences in live cells.PloS one · 2026Article
- Conformational Signatures of Preassembled and Active Complexes of 5-HTJournal of chemical information and modeling · 2025Article
- Signal termination of the chemokine receptor CCR9 is governed by an arrestin-independent phosphorylation mechanism.The Journal of biological chemistry · 2025Article
- Latrophilin-1 and latrophilin-2 as androgen receptor-responsive G protein-coupled receptors promote bladder cancer progression.American journal of translational research · 2025Article
- A Structural Proteomics Exploration of Synphilin-1 and Alpha-Synuclein Interaction in Pathogenesis of Parkinson's Disease.Biomolecules · 2024Article
- Latrophilin-3 as a downstream effector of the androgen receptor induces bladder cancer progression.Discover oncology · 2024Article
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- Latrophilins as Downstream Effectors of Androgen Receptors including a Splice Variant, AR-V7, Induce Prostate Cancer Progression.International journal of molecular sciences · 2024Article
- Molecular mechanism of muscarinic acetylcholine receptor M3 interaction with Gq.Communications biology · 2024Article
- Direct interrogation of context-dependent GPCR activity with a universal biosensor platform.Cell · 2024Article
- Direct interrogation of context-dependent GPCR activity with a universal biosensor platform.bioRxiv : the preprint server for biology · 2024Article
- Tongxieyaofang Decotion Alleviates IBS by Modulating CHRM3 and Gut Barrier.Drug design, development and therapy · 2024Article
- Allosteric Regulation of G-Protein-Coupled Receptors: From Diversity of Molecular Mechanisms to Multiple Allosteric Sites and Their Ligands.International journal of molecular sciences · 2023Review
- Two-step structural changes in M3 muscarinic receptor activation rely on the coupled GNature communications · 2023Article
- (-)-Epicatechin Is a Biased Ligand of Apelin Receptor.International journal of molecular sciences · 2022Article
- Multiple roles for cholinergic signaling in pancreatic diseases.World journal of gastroenterology · 2022Review
- Beyond Triphosphates: Reagents and Methods for Chemical Oligophosphorylation.Journal of the American Chemical Society · 2022Review
26 more citing papers are in PubMed but not listed here.
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
G protein-coupled receptors (GPCRs) transmit signals by forming active-state complexes with heterotrimeric G proteins. It has been suggested that some GPCRs also assemble with G proteins before ligand-induced activation and that inactive-state preassembly facilitates rapid and specific G protein activation. However, no mechanism of preassembly has been described, and no functional consequences of preassembly have been demonstrated. Here we show that M(3) muscarinic acetylcholine receptors (M3R) form inactive-state complexes with G(q) heterotrimers in intact cells. The M3R C terminus is sufficient, and a six-amino-acid polybasic sequence distal to helix 8 ((565)KKKRRK(570)) is necessary for preassembly with G(q). Replacing this sequence with six alanine residues prevents preassembly, slows the rate of G(q) activation and decreases steady-state agonist sensitivity. That other G(q)-coupled receptors possess similar polybasic regions and also preassemble with G(q) suggests that these GPCRs may use a common preassembly mechanism to facilitate activation of G(q) heterotrimers.
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Registered trials
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.