ArticleThe Journal of biological chemistry2009
Pirenzepine promotes the dimerization of muscarinic M1 receptors through a three-step binding process.
Article in The Journal of biological chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 52 citations in OpenAlex.
- Measuring Membrane Protein Dynamics in Plant Roots Using Fluorescence Correlation Spectroscopy.Methods in molecular biology (Clifton, N.J.) · 2027Article
- Single-molecule methods for characterizing receptor dimers reveal metastable opioid receptor homodimers that induce functional modulation.Nature communications · 2025Article
- Disruption of constitutive CXCR4 oligomers impairs oncogenic properties in lymphoid neoplasms.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Biased signaling due to oligomerization of the G protein-coupled platelet-activating factor receptor.Nature communications · 2022Article
- The MProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Distinct Dopamine D₂ Receptor Antagonists Differentially Impact D₂ Receptor Oligomerization.International journal of molecular sciences · 2019Article
- Oligomerization of a G protein-coupled receptor in neurons controlled by its structural dynamics.Scientific reports · 2018Article
- Muscarinic receptor oligomerization.Neuropharmacology · 2018Review
- Spatial Intensity Distribution Analysis: Studies of G Protein-Coupled Receptor Oligomerisation.Trends in pharmacological sciences · 2018Review
- Effect of green flickering light on myopia development and expression of M1 muscarinic acetylcholine receptor in guinea pigs.International journal of ophthalmology · 2018Article
- A Molecular Basis for Selective Antagonist Destabilization of Dopamine DScientific reports · 2017Article
- Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-selective Antagonist Drugs.The Journal of biological chemistry · 2016Article
- Distinct Agonist Regulation of Muscarinic Acetylcholine M2-M3 Heteromers and Their Corresponding Homomers.The Journal of biological chemistry · 2015Article
- Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization.British journal of pharmacology · 2014Review
- Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors.Biochimica et biophysica acta · 2014Review
- GPCR: G protein complexes--the fundamental signaling assembly.Amino acids · 2013Review
- Determination of lipid raft partitioning of fluorescently-tagged probes in living cells by Fluorescence Correlation Spectroscopy (FCS).Journal of visualized experiments : JoVE · 2012Article
- BRET and Time-resolved FRET strategy to study GPCR oligomerization: from cell lines toward native tissues.Frontiers in endocrinology · 2012Article
- Structural model of ligand-G protein-coupled receptor (GPCR) complex based on experimental double mutant cycle data: MT7 snake toxin bound to dimeric hM1 muscarinic receptor.The Journal of biological chemistry · 2011Article
- The oligomeric state sets GABA(B) receptor signalling efficacy.The EMBO journal · 2011Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ligand binding to G protein-coupled receptors is a complex process that involves sequential receptor conformational changes, ligand translocation, and possibly ligand-induced receptor oligomerization. Binding events at muscarinic acetylcholine receptors are usually interpreted from radioligand binding studies in terms of two-step ligand-induced receptor isomerization. We report here, using a combination of fluorescence approaches, on the molecular mechanisms for Bodipy-pirenzepine binding to enhanced green fluorescent protein (EGFP)-fused muscarinic M1 receptors in living cells. Real time monitoring, under steady-state conditions, of the strong fluorescence energy transfer signal elicited by this interaction permitted a fine kinetic description of the binding process. Time-resolved fluorescence measurements allowed us to identify discrete EGFP lifetime species and to follow their redistribution upon ligand binding. Fluorescence correlation spectroscopy, with EGFP brightness analysis, showed that EGFP-fused muscarinic M1 receptors predominate as monomers in the absence of ligand and dimerize upon pirenzepine binding. Finally, all these experimental data could be quantitatively reconciled into a three-step mechanism, with four identified receptor conformational states. Fast ligand binding to a peripheral receptor site initiates a sequence of conformational changes that allows the ligand to access to inner regions of the protein and drives ligand-receptor complexes toward a high affinity dimeric state.
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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.