ArticleBiophysical journal2009
Single-channel kinetic analysis for activation and desensitization of homomeric 5-HT(3)A receptors.
Article in Biophysical journal, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed.
- The serotonin-gated 5-HT3 receptor: a tale of functions and structures of a prototypical pentameric ligand-gated ion channel.Acta pharmacologica Sinica · 2026Review
- Mapping the molecular motions of 5-HTeLife · 2024Article
- Structural basis for partial agonism in 5-HTNature structural & molecular biology · 2024Article
- Efficiently Differentiating Agonists and Competitive Antagonists for Weak Allosteric Protein-Ligand Interactions with Linear Response Theory.ACS omega · 2023Article
- Ligand-Dependent Intramolecular Motion of Native Nicotinic Acetylcholine Receptors Determined in Living Myotube Cells via Diffracted X-ray Tracking.International journal of molecular sciences · 2023Article
- Intestinal enteroendocrine cells rely on ryanodine and IPThe Journal of physiology · 2023Article
- The nematode serotonin-gated chloride channel MOD-1: A novel target for anthelmintic therapy.The Journal of biological chemistry · 2022Article
- Tyrosine phosphorylation differentially fine-tunes ionotropic and metabotropic responses of human α7 nicotinic acetylcholine receptor.Cellular and molecular life sciences : CMLS · 2021Article
- Article
- Asymmetric opening of the homopentameric 5-HTNature communications · 2021Article
- Molecular Simulations of Hydrophobic Gating of Pentameric Ligand Gated Ion Channels: Insights into Water and Ions.The journal of physical chemistry. B · 2021Article
- Structure, Function and Physiology of 5-Hydroxytryptamine Receptors Subtype 3.Sub-cellular biochemistry · 2021Review
- DecipheringFrontiers in cellular neuroscience · 2021Article
- Orthosteric and Allosteric Activation of Human 5-HTBiophysical journal · 2020Article
- Mechanism of calcium potentiation of the α7 nicotinic acetylcholine receptor.The Journal of general physiology · 2020Article
- Microsecond-timescale simulations suggest 5-HT-mediated preactivation of the 5-HTProceedings of the National Academy of Sciences of the United States of America · 2020Article
- A New Antagonist ofFrontiers in neuroscience · 2020Article
- Modeling a Nociceptive Neuro-Immune Synapse Activated by ATP and 5-HT in Meninges: Novel Clues on Transduction of Chemical Signals Into Persistent or Rhythmic Neuronal Firing.Frontiers in cellular neuroscience · 2020Article
- Evidence for an effect of receptor density on ligand occupancy and agonist ECScientific reports · 2019Article
- A population of gut epithelial enterochromaffin cells is mechanosensitive and requires Piezo2 to convert force into serotonin release.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
The 5-HT(3)A receptor is a member of the Cys-loop family of ligand-gated ion channels. To perform kinetic analysis, we mutated the 5-HT3A subunit to obtain a high-conductance form so that single-channel currents can be detected. At all 5-HT concentrations (> 0.1 microM), channel activity appears as openings in quick succession that form bursts, which coalesce into clusters. By combining single-channel and macroscopic data, we generated a kinetic model that perfectly describes activation, deactivation, and desensitization. The model shows that full activation arises from receptors with three molecules of agonist bound. It reveals an earlier conformational change of the fully liganded receptor that occurs while the channel is still closed. From this pre-open closed state, the receptor enters into an open-closed cycle involving three open states, which form the cluster whose duration parallels the time constant of desensitization. A similar model lacking the pre-open closed state can describe the data only if the opening rates are fixed to account for the slow activation rate. The application of the model to M4 mutant receptors shows that position 10' contributes to channel opening and closing rates. Thus, our kinetic model provides a foundation for understanding structural bases of activation and drug action.
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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.