ReviewPharmacological reviews2015
What can crystal structures of aminergic receptors tell us about designing subtype-selective ligands?
Review in Pharmacological reviews, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 72 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
72 citing papers in PubMed, 124 citations in OpenAlex.
- A Ligand-Triggered Receptor Conformation Enables the Design of Selective Agonists for the Dopamine 3 Receptor (DJACS Au · 2026Article
- Molecular mechanisms of native ligand selectivity in catecholamine G protein-coupled receptors.Nature communications · 2026Article
- Molecular Tools to Study and Control Dopaminergic Neurotransmission With Light.Medicinal research reviews · 2025Review
- Cryo-EM Structures and AlphaFold3 Models of Histamine Receptors Reveal Diverse Ligand Binding and G Protein Bias.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Uncovering the unique characteristics of different groups of 5-HTPharmacological reports : PR · 2024Article
- A bitopic agonist bound to the dopamine 3 receptor reveals a selectivity site.Nature communications · 2024Article
- Linkers in Bitopic Agonists Shape Bias Profile among Transducers for the Dopamine D2 and D3 Receptors.ACS pharmacology & translational science · 2024Article
- The Discovery of Novel αInternational journal of molecular sciences · 2024Article
- Unraveling Activation-Related Rearrangements and Intrinsic Divergence from Ligand-Specific Conformational Changes of the Dopamine D3 and D2 Receptors.Journal of chemical information and modeling · 2024Review
- Molecular basis of human trace amine-associated receptor 1 activation.Nature communications · 2024Article
- Structure of the dopamine D3 receptor bound to a bitopic agonist reveals a new specificity site in an expanded allosteric pocket.Research square · 2023Article
- Synthesis of bitopic ligands based on fallypride and evaluation of their affinity and selectivity towards dopamine DEuropean journal of medicinal chemistry · 2023Article
- Unraveling activation-related rearrangements and intrinsic divergence from ligand-induced conformational changes of the dopamine D3 and D2 receptors.bioRxiv : the preprint server for biology · 2023Article
- Structural insights into the agonists binding and receptor selectivity of human histamine HNature communications · 2023Article
- Structural studies of serotonin receptor family.BMB reports · 2023Review
- Molecular Basis of Human Trace Amine-Associated Receptor 1 Activation.bioRxiv : the preprint server for biology · 2023Article
- Optical Control of Dopamine D2-like Receptors with Cell-Specific Fast-Relaxing Photoswitches.Journal of the American Chemical Society · 2023Article
- A Novel "Activation Switch" Motif Common to All Aminergic Receptors.Journal of chemical information and modeling · 2023Review
- Neuroprotective Effects of a Serotonin Receptor Peptide Following ShamEndocrinology, diabetes and metabolism journal · 2023Article
- Repeated Traumatic Brain Injury is Associated with Neurotoxic Plasma Autoantibodies Directed against the Serotonin 2A and Alpha 1 Adrenergic Receptors.Endocrinology, diabetes and metabolism journal · 2023Article
12 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 3 institutions in 1 country.
Funding
Abstract
G protein-coupled receptors (GPCRs) are integral membrane proteins that represent an important class of drug targets. In particular, aminergic GPCRs interact with a significant portion of drugs currently on the market. However, most drugs that target these receptors are associated with undesirable side effects, which are due in part to promiscuous interactions with close homologs of the intended target receptors. Here, based on a systematic analysis of all 37 of the currently available high-resolution crystal structures of aminergic GPCRs, we review structural elements that contribute to and can be exploited for designing subtype-selective compounds. We describe the roles of secondary binding pockets (SBPs), as well as differences in ligand entry pathways to the orthosteric binding site, in determining selectivity. In addition, using the available crystal structures, we have identified conformational changes in the SBPs that are associated with receptor activation and explore the implications of these changes for the rational development of selective ligands with tailored efficacy.
Indexed as
Identifiers
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.