ArticleACS chemical biology2012
Ondansetron and granisetron binding orientation in the 5-HT(3) receptor determined by unnatural amino acid mutagenesis.
Article in ACS chemical biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed, 40 citations in OpenAlex.
- Ferroptosis in Septic Cardiomyopathy Is Alleviated by Ondansetron: The Critical Role of the HTR3A-ATF3 Axis in Mitochondrial and Oxidative Homeostasis.Biomedicines · 2026Article
- Quetiapine competitively inhibits 5-HTThe Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2025Article
- Molecular Mechanisms of Nicergoline from Ergot Fungus in Blocking Human 5-HT3A Receptor.Journal of microbiology and biotechnology · 2024Article
- Structural basis for partial agonism in 5-HTNature structural & molecular biology · 2024Article
- Hexahexyloxycalix[6]arene, a Conformationally Adaptive Host for the Complexation of Linear and Branched Alkylammonium Guests.Molecules (Basel, Switzerland) · 2023Article
- 5-HTInternational journal of molecular sciences · 2023Article
- Controlling Doxorubicin Release from a Peptide Hydrogel through Fine-Tuning of Drug-Peptide Fiber Interactions.Biomacromolecules · 2022Article
- Hydroxy Pentacyclic Triterpene Acid, Kaempferol, Inhibits the Human 5-Hydroxytryptamine Type 3A Receptor Activity.International journal of molecular sciences · 2022Article
- High-resolution structures of multiple 5-HTeLife · 2020Article
- Molecular mechanism of setron-mediated inhibition of full-length 5-HTNature communications · 2019Article
- PharmGKB summary: Ondansetron and tropisetron pathways, pharmacokinetics and pharmacodynamics.Pharmacogenetics and genomics · 2019Article
- 5-HTAmerican journal of physiology. Gastrointestinal and liver physiology · 2019Article
- A systematic investigation of the maximum tolerated dose of cytotoxic chemotherapy with and without supportive care in mice.BMC cancer · 2017Article
- A systematic analysis of atomic protein-ligand interactions in the PDB.MedChemComm · 2017Article
- The binding orientations of structurally-related ligands can differ; A cautionary note.Neuropharmacology · 2017Article
- Conjugated nitrosoalkenes as Michael acceptors in carbon-carbon bond forming reactions: a review and perspective.Beilstein journal of organic chemistry · 2017Review
- Novel mechanism of modulation at a ligand-gated ion channel; action of 5-Cl-indole at the 5-HTBritish journal of pharmacology · 2016Article
- Cation-π interactions: computational analyses of the aromatic box motif and the fluorination strategy for experimental evaluation.Physical chemistry chemical physics : PCCP · 2015Article
- The binding characteristics and orientation of a novel radioligand with distinct properties at 5-HT3A and 5-HT3AB receptors.Neuropharmacology · 2014Article
- Functional probes of drug-receptor interactions implicated by structural studies: Cys-loop receptors provide a fertile testing ground.Journal of medicinal chemistry · 2014Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The serotonin type 3 receptor (5-HT(3)R) is a ligand-gated ion channel found in the central and peripheral nervous systems. The 5-HT(3)R is a therapeutic target, and the clinically available drugs ondansetron and granisetron inhibit receptor activity. Their inhibitory action is through competitive binding to the native ligand binding site, although the binding orientation of the drugs at the receptor has been a matter of debate. Here we heterologously express mouse 5-HT(3)A receptors in Xenopus oocytes and use unnatural amino acid mutagenesis to establish a cation-π interaction for both ondansetron and granisetron to tryptophan 183 in the ligand binding pocket. This cation-π interaction establishes a binding orientation for both ondansetron and granisetron within the binding pocket.
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What OpenQuestion holds
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.