ArticleProceedings of the National Academy of Sciences of the United States of America2018
Translating biased signaling in the ghrelin receptor system into differential in vivo functions.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 67 citations in OpenAlex.
- Deciphering a mechanistic basis for the pathological effect of the GNAO1 E246K variant in neurodevelopmental disorder.BBA advances · 2026Article
- GPCR Biased Signaling in Metabolism.Handbook of experimental pharmacology · 2026Review
- Beyond Hunger: The Structure, Signaling, and Systemic Roles of Ghrelin.International journal of molecular sciences · 2025Review
- GHS-R1a signaling drives anxiety-related behavior by shaping excitability of ventromedial hypothalamic neurons.Nature communications · 2025Article
- The structure and function of the ghrelin receptor coding for drug actions.Nature structural & molecular biology · 2025Article
- The Art of Chilling Out: How Neurons Regulate Torpor.BioEssays : news and reviews in molecular, cellular and developmental biology · 2025Review
- Hunger signalling in the olfactory bulb primes exploration, food-seeking and peripheral metabolism.Molecular metabolism · 2024Article
- Ghrelin Modulates Voltage-Gated CaMolecular pharmacology · 2024Article
- Pharmacological fingerprint of antipsychotic drugs at the serotonin 5-HTMolecular psychiatry · 2024Article
- Ghrelin receptor signaling in health and disease: a biased view.Trends in endocrinology and metabolism: TEM · 2023Review
- Enhanced Bystander BRET (ebBRET) Biosensors as Biophysical Tools to Map the Signaling Profile of Neuropsychiatric Drugs Targeting GPCRs.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Article
- Discovery of a functionally selective ghrelin receptor (GHSRProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Advances in the Development of Nonpeptide Small Molecules Targeting Ghrelin Receptor.Journal of medicinal chemistry · 2022Review
- GαFrontiers in cell and developmental biology · 2022Review
- Structural basis of human ghrelin receptor signaling by ghrelin and the synthetic agonist ibutamoren.Nature communications · 2021Article
- Identification of Key Regions Mediating Human Melatonin Type 1 Receptor Functional Selectivity Revealed by Natural Variants.ACS pharmacology & translational science · 2021Article
- Ackr3-Venus knock-in mouse lights up brain vasculature.Molecular brain · 2021Article
- Ghrelin ameliorates nonalcoholic steatohepatitis induced by chronic low-grade inflammation via blockade of Kupffer cell M1 polarization.Journal of cellular physiology · 2021Article
- Allosteric modulation of ghrelin receptor signaling by lipids.Nature communications · 2021Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 3 countries.
Funding
Abstract
Biased signaling has been suggested as a means of selectively modulating a limited fraction of the signaling pathways for G-protein-coupled receptor family members. Hence, biased ligands may allow modulation of only the desired physiological functions and not elicit undesired effects associated with pharmacological treatments. The ghrelin receptor is a highly sought antiobesity target, since the gut hormone ghrelin in humans has been shown to increase both food intake and fat accumulation. However, it also modulates mood, behavior, growth hormone secretion, and gastric motility. Thus, blocking all pathways of this receptor may give rise to potential side effects. In the present study, we describe a highly promiscuous signaling capacity for the ghrelin receptor. We tested selected ligands for their ability to regulate the various pathways engaged by the receptor. Among those, a biased ligand, YIL781, was found to activate the Gα
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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.