ArticleeLife2019
Crystal structure of dopamine receptor D4 bound to the subtype selective ligand, L745870.
Article in eLife, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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
19 citing papers in PubMed, 35 citations in OpenAlex.
- The structure of the dopamine DScience advances · 2026Article
- Molecular Tools to Study and Control Dopaminergic Neurotransmission With Light.Medicinal research reviews · 2025Review
- Synthesis and Biological Characterization of 4,4-Difluoro-3-(phenoxymethyl)piperidine Scaffold as Dopamine 4 Receptor (DChemMedChem · 2025Article
- Novel Potent and Selective Dopamine D4 Receptor Piperidine Antagonists as Potential Alternatives for the Treatment of Glioblastoma.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Exploring the impact of deleterious missense nonsynonymous single nucleotide polymorphisms in the DRD4 gene using computational approaches.Scientific reports · 2025Article
- A fiducial-assisted strategy compatible with resolving small MFS transporter structures in multiple conformations using cryo-EM.Nature communications · 2025Article
- Comparison of the function of two novel human dopamine D2 receptor variants identifies a likely mechanism for their pathogenicity.Biochemical pharmacology · 2024Article
- G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024Article
- Computer-Aided Design and Biological Evaluation of Diazaspirocyclic DACS chemical neuroscience · 2024Article
- Structural genomics of the human dopamine receptor system.Cell research · 2023Article
- Highly Potent and Selective Dopamine DJournal of medicinal chemistry · 2022Article
- Ligand recognition and biased agonism of the D1 dopamine receptor.Nature communications · 2022Article
- Fentanyl Structure as a Scaffold for Opioid/Non-Opioid Multitarget Analgesics.International journal of molecular sciences · 2022Review
- Crystal structure of the αNature communications · 2022Article
- Potent and Subtype-Selective Dopamine DJournal of medicinal chemistry · 2021Article
- Fluorescent ligands for dopamine DScientific reports · 2020Article
- Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine DACS medicinal chemistry letters · 2020Article
- Conformational dynamics of a G protein-coupled receptor helix 8 in lipid membranes.Science advances · 2020Article
- Crystal structure of dopamine receptor D4 bound to the subtype selective ligand, L745870.eLife · 2019Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Multiple subtypes of dopamine receptors within the GPCR superfamily regulate neurological processes through various downstream signaling pathways. A crucial question about the dopamine receptor family is what structural features determine the subtype-selectivity of potential drugs. Here, we report the 3.5-angstrom crystal structure of mouse dopamine receptor D4 (DRD4) complexed with a subtype-selective antagonist, L745870. Our structure reveals a secondary binding pocket extended from the orthosteric ligand-binding pocket to a DRD4-specific crevice located between transmembrane helices 2 and 3. Additional mutagenesis studies suggest that the antagonist L745870 prevents DRD4 activation by blocking the relative movement between transmembrane helices 2 and 3. These results expand our knowledge of the molecular basis for the physiological functions of DRD4 and assist new drug design.
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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.