ReviewTrends in pharmacological sciences2007
Multiple GPCR conformations and signalling pathways: implications for antagonist affinity estimates.
Review in Trends in pharmacological sciences, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 52 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
52 citing papers in PubMed.
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- How Carvedilol activates βNature communications · 2022Article
- Novel agonist and antagonist radioligands for the GLP-2 receptor. Useful tools for studies of basic GLP-2 receptor pharmacology.British journal of pharmacology · 2022Article
- CellectSeq: In silico discovery of antibodies targeting integral membrane proteins combining in situ selections and next-generation sequencing.Communications biology · 2021Article
- Regulation of mitochondrial metabolism in murine skeletal muscle by the medium-chain fatty acid receptor Gpr84.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2019Article
- The Synthetic Dipeptide Pidotimod Shows a Chemokine-Like Activity through CXC Chemokine Receptor 3 (CXCR3).International journal of molecular sciences · 2019Article
- Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DJournal of medicinal chemistry · 2019Article
- Effect of apelin on cardiac contractility in acute reno-vascular hypertension: The role of apelin receptor and kappa opioid receptor heterodimerization.Iranian journal of basic medical sciences · 2018Article
- Distinct Signaling Patterns of Allosteric Antagonism at the P2YMolecular pharmacology · 2017Article
- The differential effects of low and high doses of apelin through opioid receptors on the blood pressure of rats with renovascular hypertension.Hypertension research : official journal of the Japanese Society of Hypertension · 2017Article
- A single-chain derivative of the relaxin hormone is a functionally selective agonist of the G protein-coupled receptor, RXFP1.Chemical science · 2016Article
- Orthosteric, Allosteric and Biased Signalling at the Relaxin-3 Receptor RXFP3.Neurochemical research · 2016Article
- Allosteric modulation of metabotropic glutamate receptor 4 activates IDO1-dependent, immunoregulatory signaling in dendritic cells.Neuropharmacology · 2016Article
- Structural signatures of DRD4 mutants revealed using molecular dynamics simulations: Implications for drug targeting.Journal of molecular modeling · 2016Article
- The Multitarget Ligand 3-Iodothyronamine Modulates β-Adrenergic Receptor 2 Signaling.European thyroid journal · 2015Article
- Neuropeptide receptor transcript expression levels and magnitude of ionic current responses show cell type-specific differences in a small motor circuit.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2015Article
- International Union of Basic and Clinical Pharmacology. XCV. Recent advances in the understanding of the pharmacology and biological roles of relaxin family peptide receptors 1-4, the receptors for relaxin family peptides.Pharmacological reviews · 2015Review
- Pharmacologically distinct phenotypes of α1B -adrenoceptors: variation in binding and functional affinities for antagonists.British journal of pharmacology · 2014Article
- Tuning up the right signal: chemical and genetic approaches to study GPCR functions.Current opinion in cell biology · 2014Review
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
Antagonist affinity measurements have traditionally been considered important in characterizing the cell-surface receptors present in a particular cell or tissue. A central assumption has been that antagonist affinity is constant for a given receptor-antagonist interaction, regardless of the agonist used to stimulate that receptor or the downstream response that is measured. As a consequence, changes in antagonist affinity values have been taken as initial evidence for the presence of novel receptor subtypes. Emerging evidence suggests, however, that receptors can possess multiple binding sites and the same receptor can show different antagonist affinity measurements under distinct experimental conditions. Here, we discuss several mechanisms by which antagonists have different affinities for the same receptor as a consequence of allosterism, coupling to different G proteins, multiple (but non-interacting) receptor sites, and signal-pathway-dependent pharmacology (where the pharmacology observed varies depending on the signalling pathway measured).
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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.