ArticleJournal of medicinal chemistry2016
Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists.
Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 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.
The trial behind it
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
31 citing papers in PubMed, 52 citations in OpenAlex.
- Biased Allosteric Modulation in GPCR Drug Discovery.Handbook of experimental pharmacology · 2026Review
- Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery.Nature reviews. Drug discovery · 2025Review
- Molecular Glues: A New Approach to Modulating GPCR Signaling Bias.Biochemistry · 2025Review
- Biased Dopamine DBiomolecules & therapeutics · 2024Article
- Unveiling the Differences in Signaling and Regulatory Mechanisms between Dopamine DInternational journal of molecular sciences · 2023Review
- The histamine H3 receptor modulates dopamine D2 receptor-dependent signaling pathways and mouse behaviors.The Journal of biological chemistry · 2023Article
- Association of Polymorphism within the Putative miRNA Target Site in the 3'UTR Region of theInternational journal of environmental research and public health · 2022Article
- Ligand-directed bias of G protein signaling at the dopamine DCell chemical biology · 2022Article
- Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties.Nature neuroscience · 2022Article
- Synthesis and In Vitro Evaluation of Novel Dopamine Receptor DBiomolecules · 2021Article
- Potent and Subtype-Selective Dopamine DJournal of medicinal chemistry · 2021Article
- New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine DScientific reports · 2021Article
- Dopamine D1 Receptor in Cancer.Cancers · 2020Review
- Transcriptomic approach predicts a major role for transforming growth factor beta type 1 pathway in L-Dopa-induced dyskinesia in parkinsonian rats.Genes, brain, and behavior · 2020Article
- Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation.Molecular psychiatry · 2020Article
- 2016 Philip S. Portoghese Medicinal Chemistry Lectureship: Designing Bivalent or Bitopic Molecules for G-Protein Coupled Receptors. The Whole Is Greater Than the Sum of Its Parts.Journal of medicinal chemistry · 2020Article
- A kinetic method for measuring agonist efficacy and ligand bias using high resolution biosensors and a kinetic data analysis framework.Scientific reports · 2020Article
- A structural basis for how ligand binding site changes can allosterically regulate GPCR signaling and engender functional selectivity.Science signaling · 2020Article
- Dopamine Receptor Subtypes, Physiology and Pharmacology: New Ligands and Concepts in Schizophrenia.Frontiers in pharmacology · 2020Review
- Designing Functionally Selective Noncatechol Dopamine DACS chemical neuroscience · 2019Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
Biased ligands (also known as functionally selective ligands) of G protein-coupled receptors are valuable tools for dissecting the roles of G protein-dependent and independent signaling pathways in health and disease. Biased ligands have also been increasingly pursued by the biomedical community as promising therapeutics with improved efficacy and reduced side effects compared with unbiased ligands. We previously discovered first-in-class β-arrestin-biased agonists of dopamine D2 receptor (D2R) by extensively exploring multiple regions of aripiprazole, a balanced D2R agonist. In our continuing efforts to identify biased agonists of D2R, we unexpectedly discovered a G protein-biased agonist of D2R, compound 1, which is the first G protein-biased D2R agonist from the aripiprazole scaffold. We designed and synthesized novel analogues to explore two regions of 1 and conducted structure-functional selectivity relationship (SFSR) studies. Here we report the discovery of 1, findings from our SFSR studies, and characterization of novel G protein-biased D2R agonists.
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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.