ArticleBritish journal of pharmacology2017
Design and validation of the first cell-impermeant melatonin receptor agonist.
Article in British journal of pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
25 citing papers in PubMed, 60 citations in OpenAlex.
- Melatonin Interventions in Autism Spectrum Disorder: Sleep Regulation, Behavioral Outcomes, and Challenges Across the Lifespan.Molecular neurobiology · 2025Review
- Mitochondrial Localization and Function of Adenosine Receptors.International journal of biological sciences · 2025Article
- Cancer Cells Show Higher Sensitivity to Melatonin-Tamoxifen Drug Conjugates than to Combination of Melatonin and Tamoxifen.ACS omega · 2024Article
- Synthesis and Fluorescence Properties of 4-Cyano and 4-Formyl Melatonin as Putative Melatoninergic Ligands.ACS omega · 2023Article
- The Therapeutic Potential of Antioxidants in Chemotherapy-Induced Peripheral Neuropathy: Evidence from Preclinical and Clinical Studies.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2023Review
- GPCRs in Intracellular Compartments: New Targets for Drug Discovery.Biomolecules · 2022Review
- Design and Validation of the First Family of Photo-Activatable Ligands for Melatonin Receptors.Journal of medicinal chemistry · 2022Article
- Luminogenic HiBiT Peptide-Based NanoBRET Ligand Binding Assays for Melatonin Receptors.ACS pharmacology & translational science · 2022Article
- Melatonin Receptors: A Key Mediator in Animal Reproduction.Veterinary sciences · 2022Review
- Melatonin Signaling Pathways Implicated in Metabolic Processes in Human Granulosa Cells (KGN).International journal of molecular sciences · 2022Article
- Functional Investigation of Melatonin Receptor Activation by Homogenous cAMP Assay.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Development of a novel in vitro assay to screen for neuroprotective drugs against iatrogenic neurite shortening.PloS one · 2021Article
- Structural insights into emergent signaling modes of G protein-coupled receptors.The Journal of biological chemistry · 2020Review
- The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion.Pharmacology research & perspectives · 2020Review
- Melatonin in type 2 diabetes mellitus and obesity.Nature reviews. Endocrinology · 2019Review
- Melatonin Target Proteins: Too Many or Not Enough?Frontiers in endocrinology · 2019Review
- GPCR signalling from within the cell.British journal of pharmacology · 2018Review
- Intracellular GPCRs Play Key Roles in Synaptic Plasticity.ACS chemical neuroscience · 2018Review
- Melatonin receptors: molecular pharmacology and signalling in the context of system bias.British journal of pharmacology · 2018Review
- Immune-pineal axis - acute inflammatory responses coordinate melatonin synthesis by pinealocytes and phagocytes.British journal of pharmacology · 2018Review
Corrections and comments
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Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
Abstract
background and purposeThe paradigm that GPCRs are able to prolong or initiate cellular signalling through intracellular receptors recently emerged. Melatonin binds to G protein-coupled MT EXPERIMENTAL APPROACH: We therefore designed and synthesized a series of hydrophilic melatonin receptor ligands coupled to the Cy3 cyanin fluorophore to reliably monitor its inability to penetrate cells. Two compounds, one lipophilic and one hydrophilic, were then functionally characterized in terms of their affinity for human and murine melatonin receptors expressed in HEK293 cells and their signalling efficacy. KEY
resultsAmong the different ligands, ICOA-13 showed the desired properties as it was cell-impermeant and bound to human and mouse MT CONCLUSIONS AND IMPLICATIONS: We report here the first cell-impermeant melatonin receptor agonist, ICOA-13, which allows us to discriminate between signalling events initiated at the cell surface and intracellular compartments. Detection of mitochondrial MT
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What Socratic 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 Socratic graph.