ArticleScience (New York, N.Y.)2013
Structural basis for molecular recognition at serotonin receptors.
Article in Science (New York, N.Y.), 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 216 papers.
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Who cites it
216 citing papers in PubMed, 519 citations in OpenAlex.
- Total Synthesis of 8-Hydroxy-dihydroergotamine, the Major Human Metabolite of Dihydroergotamine.Molecules (Basel, Switzerland) · 2026Article
- A structural overview of G-protein-coupled receptors in neurological disorders.Acta pharmacologica Sinica · 2026Review
- Strategic advances for cryo-EM structural studies of small (<100 kDa) GPCRs.Communications biology · 2026Review
- Biased Signaling in Psychedelic Action.Annual review of pharmacology and toxicology · 2026Review
- Conformational Heterogeneity Underlying Divergent Signaling in Class A G Protein-Coupled Receptors.ACS pharmacology & translational science · 2025Review
- Distinctive patterns of G protein coupling induced by the structurally similar 5-HTMolecular pharmacology · 2025Article
- Effects of Membrane Cholesterol on the Structure and Function of Selected Class A GPCRs─Challenges and Future Perspectives.Biochemistry · 2025Review
- Psychedelic compounds directly excite 5-HTTranslational psychiatry · 2025Article
- Structural determinants of G protein subtype selectivity at the serotonin receptor 5-HT1A.Science advances · 2025Article
- 5-HTPharmacological reviews · 2025Review
- In search of a photoswitchable drug for serotonin receptors: a molecular dynamics simulation study.RSC advances · 2025Article
- Human epidermal growth factor receptor 2(Her2)-targeted pH-responsive MR/NIRF bimodal imaging-mediated nano-delivery system for the diagnosis and treatment of undifferentiated thyroid cancer.Drug delivery and translational research · 2025Article
- Hybridization of SMILES and chemical-environment-aware tokens to improve performance of molecular structure generation.Scientific reports · 2025Article
- Activity cliff-aware reinforcement learning for de novo drug design.Journal of cheminformatics · 2025Article
- AnCurrent drug discovery technologies · 2025Article
- Structural Pharmacology of Bufotenine Derivatives in Activating the 5-HTResearch (Washington, D.C.) · 2025Article
- A NiNature communications · 2024Article
- Uncovering the unique characteristics of different groups of 5-HTPharmacological reports : PR · 2024Article
- Genome-wide pan-GPCR cell libraries accelerate drug discovery.Acta pharmaceutica Sinica. B · 2024Review
- Computational Methods for the Discovery and Optimization of TAAR1 and TAAR5 Ligands.International journal of molecular sciences · 2024Review
156 more citing papers are in PubMed but not listed here.
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Authors and funding
23 authors at 6 institutions in 2 countries.
Funding
Abstract
Serotonin or 5-hydroxytryptamine (5-HT) regulates a wide spectrum of human physiology through the 5-HT receptor family. We report the crystal structures of the human 5-HT1B G protein-coupled receptor bound to the agonist antimigraine medications ergotamine and dihydroergotamine. The structures reveal similar binding modes for these ligands, which occupy the orthosteric pocket and an extended binding pocket close to the extracellular loops. The orthosteric pocket is formed by residues conserved in the 5-HT receptor family, clarifying the family-wide agonist activity of 5-HT. Compared with the structure of the 5-HT2B receptor, the 5-HT1B receptor displays a 3 angstrom outward shift at the extracellular end of helix V, resulting in a more open extended pocket that explains subtype selectivity. Together with docking and mutagenesis studies, these structures provide a comprehensive structural basis for understanding receptor-ligand interactions and designing subtype-selective serotonergic drugs.
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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.