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High Constitutive Signaling of the Ghrelin Receptor—Identification of a Potent Inverse Agonist
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What this work says
Outgoing claims: the papers this work cites, builds on, or argues with.
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A Colorimetric Assay for Measuring Activation of Gs- and Gq-Coupled Signaling Pathways
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Engineering hybrid genes without the use of restriction enzymes: gene splicing by overlap extension
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Motilin and Clinical Application
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Ghrelin: discovery of the natural endogenous ligand for the growth hormone secretagogue receptor
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Structure−Function Studies on the New Growth Hormone-Releasing Peptide, Ghrelin: Minimal Sequence of Ghrelin Necessary for Activation of Growth Hormone Secretagogue Receptor 1a
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Amide bond replacements incorporated into CCK-B selective "dipeptoids"
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G-protein-coupled receptor of Kaposi's sarcoma-associated herpesvirus is a viral oncogene and angiogenesis activator
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Central nervous system control of food intake
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Ghrelin induces adiposity in rodents
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A role for ghrelin in the central regulation of feeding
inferredcites →https://doi.org/10.1038/374074a0openalex-snapshot
Conversion of antagonist-binding site to metal-ion site in the tachykinin NK-1 receptor
inferredcites →https://doi.org/10.1038/45230openalex-snapshot
Ghrelin is a growth-hormone-releasing acylated peptide from stomach
inferredcites →https://doi.org/10.1053/gast.2001.22158openalex-snapshot
Ghrelin is an appetite-stimulatory signal from stomach with structural resemblance to motilin
inferredcites →https://doi.org/10.1053/gast.2002.35954openalex-snapshot
The role of the gastric afferent vagal nerve in ghrelin-induced feeding and growth hormone secretion in rats
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Plasma Ghrelin Levels after Diet-Induced Weight Loss or Gastric Bypass Surgery
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Agonists and Inverse Agonists for the Herpesvirus 8-encoded Constitutively Active Seven-transmembrane Oncogene Product, ORF-74
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inferredcites →https://doi.org/10.1074/jbc.m205366200openalex-snapshot
Structural Divergence of Human Ghrelin
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inferredcites →https://doi.org/10.1210/en.142.10.4163openalex-snapshot
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inferredcites →https://doi.org/10.1210/endo-106-3-663openalex-snapshot
Structure-Activity Relationships of a Synthetic Pentapeptide that Specifically Releases Growth Hormonein Vitro*
inferredcites →https://doi.org/10.1210/endo-114-5-1537openalex-snapshot
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inferredcites →https://doi.org/10.1210/jc.87.6.2988openalex-snapshot
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inferredcites →https://doi.org/10.1210/me.11.4.415openalex-snapshot
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inferredcites →https://doi.org/10.1210/me.15.1.164openalex-snapshot
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inferredcites →https://doi.org/10.1210/mend.12.1.0051openalex-snapshot
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inferredcites →https://doi.org/10.1523/jneurosci.21-04-01238.2001openalex-snapshot
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inferredcites →https://doi.org/10.1530/eje.0.1410180openalex-snapshot
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A Preprandial Rise in Plasma Ghrelin Levels Suggests a Role in Meal Initiation in Humans
What points at this work
Incoming claims: where this work appears in other papers’ reference lists and arguments.
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Basal interaction of the orphan receptor GPR101 with arrestins leads to constitutive internalization
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The constitutive activity of ghrelin receptors is decreased by co-expression with vasoactive prostanoid receptors when over-expressed in human embryonic kidney 293 cells
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Modeling of human ghrelin receptor (hGHS-R1a) in its close state and validation by molecular docking
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Synthesis and pharmacological evaluation of indolinone derivatives as novel ghrelin receptor antagonists
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High metabolic in vivo stability and bioavailability of a palmitoylated ghrelin receptor ligand assessed by mass spectrometry
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Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model
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Structure–activity relationships of the oxindole growth hormone secretagogues
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Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists
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2-Aminoalkyl nicotinamide derivatives as pure inverse agonists of the ghrelin receptor
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New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center
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Ghrelin but not nesfatin-1 affects certain forms of learning and memory in both rats and mice
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Physiological roles for butyrylcholinesterase: A BChE-ghrelin axis
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Hunger States Switch a Flip-Flop Memory Circuit via a Synaptic AMPK-Dependent Positive Feedback Loop
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The truncated ghrelin receptor polypeptide (GHS-R1b) acts as a dominant-negative mutant of the ghrelin receptor
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Signaling via G proteins mediates tumorigenic effects of GPR87
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Biased signaling: A viable strategy to drug ghrelin receptors for the treatment of obesity
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MRAP2 potentiates GPCR signaling by conserved mechanisms that are disrupted by obesity-associated genetic variants
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Bioorthogonal Labeling of Ghrelin Receptor to Facilitate Studies of Ligand-Dependent Conformational Dynamics
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G protein-coupled receptors: A golden key to the treasure-trove of neurodegenerative diseases
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Chronic Activation of γ2 AMPK Induces Obesity and Reduces β Cell Function
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LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor
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The Homeostatic Force of Ghrelin
inferred← citeshttps://doi.org/10.1016/j.cnd.2022.12.002openalex-snapshot
La régulation de la prise alimentaire au travers des actions antagonistes de la ghréline et du LEAP-2
inferred← citeshttps://doi.org/10.1016/j.coi.2004.03.010openalex-snapshot
Ligand-independent tonic signaling in B-cell receptor function
inferred← citeshttps://doi.org/10.1016/j.coph.2006.08.005openalex-snapshot
Potential of ghrelin as a therapeutic approach for gastrointestinal motility disorders
inferred← citeshttps://doi.org/10.1016/j.cub.2020.08.069openalex-snapshot
Ghrelin Signaling Affects Feeding Behavior, Metabolism, and Memory through the Vagus Nerve
inferred← citeshttps://doi.org/10.1016/j.drugalcdep.2011.01.010openalex-snapshot
Ghrelin receptor antagonism attenuates nicotine-induced locomotor stimulation, accumbal dopamine release and conditioned place preference in mice
inferred← citeshttps://doi.org/10.1016/j.ecl.2009.07.001openalex-snapshot
Nutrition and Bone Growth in Pediatrics
inferred← citeshttps://doi.org/10.1016/j.ejmech.2022.114308openalex-snapshot
An insight into the multifunctional role of ghrelin and structure activity relationship studies of ghrelin receptor ligands with clinical trials
inferred← citeshttps://doi.org/10.1016/j.ejphar.2009.03.066openalex-snapshot
Anorexigenic and electrophysiological actions of novel ghrelin receptor (GHS-R1A) antagonists in rats
inferred← citeshttps://doi.org/10.1016/j.ejphar.2010.06.018openalex-snapshot
Involvement of tryptophan W276 and of two surrounding amino acid residues in the high constitutive activity of the ghrelin receptor GHS-R1a
inferred← citeshttps://doi.org/10.1016/j.ejphar.2010.10.042openalex-snapshot
Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors
inferred← citeshttps://doi.org/10.1016/j.ejphar.2015.01.001openalex-snapshot
Pharmacological lineage analysis revealed the binding affinity of broad-spectrum substance P antagonists to receptors for gonadotropin-releasing peptide
inferred← citeshttps://doi.org/10.1016/j.ejphar.2024.176880openalex-snapshot
In vitro pharmacological characterization of growth hormone secretagogue receptor ligands using the dynamic mass redistribution and calcium mobilization assays
inferred← citeshttps://doi.org/10.1016/j.eplepsyres.2023.107234openalex-snapshot
Differential impact of a ghrelin receptor antagonist or inverse agonist in the electrical kindling model of epilepsy
inferred← citeshttps://doi.org/10.1016/j.febslet.2004.08.088openalex-snapshot
Signal transduction mechanism of the seabream growth hormone secretagogue receptor
inferred← citeshttps://doi.org/10.1016/j.febslet.2008.06.030openalex-snapshot
Molecular mechanism of Zn2+agonism in the extracellular domain of GPR39
inferred← citeshttps://doi.org/10.1016/j.febslet.2012.06.034openalex-snapshot
Exogenous and endogenous ghrelin counteracts GLP‐1 action to stimulate cAMP signaling and insulin secretion in islet β‐cells
inferred← citeshttps://doi.org/10.1016/j.jdiacomp.2025.109062openalex-snapshot
Role of rs490683 variant in the promoter region of the ghrelin receptor gene on body weight and metabolic syndrome after a partial meal replacement hypocaloric diet
inferred← citeshttps://doi.org/10.1016/j.jmgm.2006.11.002openalex-snapshot
Proteometric study of ghrelin receptor function variations upon mutations using amino acid sequence autocorrelation vectors and genetic algorithm-based least square support vector machines
inferred← citeshttps://doi.org/10.1016/j.lfs.2022.120316openalex-snapshot
Therapeutic potential of GHSR-1A antagonism in alcohol dependence, a review
inferred← citeshttps://doi.org/10.1016/j.mce.2008.01.003openalex-snapshot
Ghrelin enhances the proliferating effect of thyroid stimulating hormone in FRTL-5 thyroid cells
inferred← citeshttps://doi.org/10.1016/j.mce.2008.12.006openalex-snapshot
The constitutive activity of the ghrelin receptor attenuates apoptosis via a protein kinase C-dependent pathway
inferred← citeshttps://doi.org/10.1016/j.mce.2011.02.017openalex-snapshot
The role of the central ghrelin system in reward from food and chemical drugs
inferred← citeshttps://doi.org/10.1016/j.mce.2011.03.021openalex-snapshot
The role of ghrelin in GH secretion and GH disorders
inferred← citeshttps://doi.org/10.1016/j.mce.2011.08.034openalex-snapshot
The truncated ghrelin receptor polypeptide (GHS-R1b) is localized in the endoplasmic reticulum where it forms heterodimers with ghrelin receptors (GHS-R1a) to attenuate their cell surface expression
inferred← citeshttps://doi.org/10.1016/j.mce.2016.07.016openalex-snapshot
Ghrelin binding to serum albumin and its biological impact
inferred← citeshttps://doi.org/10.1016/j.mce.2016.09.027openalex-snapshot
Hypothalamic regulation of body growth and appetite by ghrelin-derived peptides during balanced nutrition or undernutrition
inferred← citeshttps://doi.org/10.1016/j.mce.2019.110573openalex-snapshot
Development of a novel fluorescent ligand of growth hormone secretagogue receptor based on the N-Terminal Leap2 region
inferred← citeshttps://doi.org/10.1016/j.mce.2024.112367openalex-snapshot
The adipose tissue melanocortin 3 receptor is targeted by ghrelin and leptin and may be a therapeutic target in obesity
inferred← citeshttps://doi.org/10.1016/j.molmet.2018.09.007openalex-snapshot
Ghrelin transport across the blood–brain barrier can occur independently of the growth hormone secretagogue receptor
inferred← citeshttps://doi.org/10.1016/j.molmet.2019.02.005openalex-snapshot
Dopamine neuronal protection in the mouse Substantia nigra by GHSR is independent of electric activity
inferred← citeshttps://doi.org/10.1016/j.molmet.2020.101004openalex-snapshot
Metabolic insights from a GHSR-A203E mutant mouse model
inferred← citeshttps://doi.org/10.1016/j.molmet.2020.101128openalex-snapshot
“A LEAP 2 conclusions? Targeting the ghrelin system to treat obesity and diabetes”
inferred← citeshttps://doi.org/10.1016/j.molpha.2025.100100openalex-snapshot
Constitutive activity among orphan G protein-coupled receptors: Molecular mechanisms and pharmacological perspectives
inferred← citeshttps://doi.org/10.1016/j.neubiorev.2016.11.021openalex-snapshot
Is there a role for ghrelin in central dopaminergic systems? Focus on nigrostriatal and mesocorticolimbic pathways
inferred← citeshttps://doi.org/10.1016/j.neubiorev.2020.10.017openalex-snapshot
THE INTRIGUING LIGAND-DEPENDENT AND LIGAND-INDEPENDENT ACTIONS OF THE GROWTH HORMONE SECRETAGOGUE RECEPTOR ON REWARD-RELATED BEHAVIORS
inferred← citeshttps://doi.org/10.1016/j.neuint.2013.06.014openalex-snapshot
Ghrelin amplifies the nicotine-induced dopamine release in the rat striatum
inferred← citeshttps://doi.org/10.1016/j.neuropharm.2009.06.024openalex-snapshot
Lean mean fat reducing “ghrelin” machine: Hypothalamic ghrelin and ghrelin receptors as therapeutic targets in obesity
inferred← citeshttps://doi.org/10.1016/j.neuropharm.2010.12.024openalex-snapshot
Ghrelin-induced activation of cAMP signal transduction and its negative regulation by endocannabinoids in the hippocampus
inferred← citeshttps://doi.org/10.1016/j.neuropharm.2017.11.039openalex-snapshot
Hippocampus ghrelin receptor signaling promotes socially-mediated learned food preference
inferred← citeshttps://doi.org/10.1016/j.neuropharm.2023.109643openalex-snapshot
Pharmacological GHSR (ghrelin receptor) blockade reduces alcohol binge-like drinking in male and female mice
inferred← citeshttps://doi.org/10.1016/j.neuroscience.2018.09.027openalex-snapshot
Ghrelin Recruits Specific Subsets of Dopamine and GABA Neurons of Different Ventral Tegmental Area Sub-nuclei
inferred← citeshttps://doi.org/10.1016/j.neuroscience.2019.05.067openalex-snapshot
Acute But Not Chronic Calorie Restriction Defends against Stress-Related Anxiety and Despair in a GHS-R1a-Dependent Manner
inferred← citeshttps://doi.org/10.1016/j.npep.2017.12.001openalex-snapshot
Blocking constitutive activity of GHSR1a in the lateral amygdala facilitates acquisition of conditioned taste aversion
inferred← citeshttps://doi.org/10.1016/j.nut.2009.09.013openalex-snapshot
Focus on the short- and long-term effects of ghrelin on energy homeostasis
inferred← citeshttps://doi.org/10.1016/j.pbb.2016.12.009openalex-snapshot
Intermittent access to a nutritionally complete high-fat diet attenuates alcohol drinking in rats
inferred← citeshttps://doi.org/10.1016/j.pcl.2011.07.008openalex-snapshot
Nutrition and Bone Growth in Pediatrics
inferred← citeshttps://doi.org/10.1016/j.peptides.2005.04.025openalex-snapshot
Ghrelin induces feeding in the mesolimbic reward pathway between the ventral tegmental area and the nucleus accumbens
inferred← citeshttps://doi.org/10.1016/j.peptides.2011.04.014openalex-snapshot
Physiological roles of preproghrelin-derived peptides in GH secretion and feeding
inferred← citeshttps://doi.org/10.1016/j.peptides.2011.05.014openalex-snapshot
Central mechanisms involved in the orexigenic actions of ghrelin
inferred← citeshttps://doi.org/10.1016/j.peptides.2011.07.021openalex-snapshot
Ghrelin and appetite control in humans—Potential application in the treatment of obesity
inferred← citeshttps://doi.org/10.1016/j.peptides.2011.09.006openalex-snapshot
Genetic studies on the ghrelin, growth hormone secretagogue receptor (GHSR) and ghrelin O-acyl transferase (GOAT) genes
inferred← citeshttps://doi.org/10.1016/j.peptides.2017.12.015openalex-snapshot
Ghrelin regulation of glucose metabolism
inferred← citeshttps://doi.org/10.1016/j.peptides.2020.170388openalex-snapshot
Effects of microbiome changes on endocrine ghrelin signaling – A systematic review
inferred← citeshttps://doi.org/10.1016/j.peptides.2025.171367openalex-snapshot
The role of leptin and ghrelin in the regulation of appetite in obesity
inferred← citeshttps://doi.org/10.1016/j.pharmthera.2004.08.008openalex-snapshot
Mutant G-protein-coupled receptors as a cause of human diseases
inferred← citeshttps://doi.org/10.1016/j.pharmthera.2008.02.008openalex-snapshot
Ghrelin is a physiological regulator of insulin release in pancreatic islets and glucose homeostasis
inferred← citeshttps://doi.org/10.1016/j.pharmthera.2008.07.005openalex-snapshot
Constitutive activation of G protein-coupled receptors and diseases: Insights into mechanisms of activation and therapeutics
inferred← citeshttps://doi.org/10.1016/j.pharmthera.2021.108044openalex-snapshot
Naturally occurring mutations in G protein-coupled receptors associated with obesity and type 2 diabetes mellitus
inferred← citeshttps://doi.org/10.1016/j.pharmthera.2026.109056openalex-snapshot
GPCR crosstalk beyond obligate dimerisation: Effector coincidence detection, compartmentation, and pharmacological implications
inferred← citeshttps://doi.org/10.1016/j.phrs.2004.02.004openalex-snapshot
Emerging aspects of pharmacotherapy for obesity and metabolic syndrome
inferred← citeshttps://doi.org/10.1016/j.physbeh.2006.05.022openalex-snapshot
Ghrelin and the short- and long-term regulation of appetite and body weight
inferred← citeshttps://doi.org/10.1016/j.physbeh.2010.10.017openalex-snapshot
Signaling through the ghrelin receptor modulates hippocampal function and meal anticipation in mice
inferred← citeshttps://doi.org/10.1016/j.physbeh.2016.03.039openalex-snapshot
Ghrelin: A link between memory and ingestive behavior
inferred← citeshttps://doi.org/10.1016/j.physbeh.2026.115357openalex-snapshot
The role of ghrelin receptor constitutive activity in fear memory: hippocampal excitability, long-term potentiation, and behavioral implications
inferred← citeshttps://doi.org/10.1016/j.plipres.2009.04.002openalex-snapshot
Ghrelin – Defender of fat
inferred← citeshttps://doi.org/10.1016/j.psj.2021.101204openalex-snapshot
Capromorelin, a ghrelin receptor agonist, increases feed intake and body weight gain in broiler chickens (Gallus gallus domesticus)
inferred← citeshttps://doi.org/10.1016/j.psj.2022.101945openalex-snapshot
Systemic infusion of exogenous ghrelin in male broiler chickens (Gallus gallus domesticus). The effect of pulse frequency, doses, and ghrelin forms on feed intake, average daily gain, corticosterone, and growth hormone concentrations
inferred← citeshttps://doi.org/10.1016/j.regpep.2009.04.002openalex-snapshot
Targeting the ghrelin receptor to regulate food intake
inferred← citeshttps://doi.org/10.1016/j.regpep.2010.06.005openalex-snapshot
Proghrelin peptides: Desacyl ghrelin is a powerful inhibitor of acylated ghrelin, likely to impair physiological effects of acyl ghrelin but not of obestatin
inferred← citeshttps://doi.org/10.1016/j.regpep.2010.08.002openalex-snapshot
Mutational analysis of predicted extracellular domains of human growth hormone secretagogue receptor 1a
inferred← citeshttps://doi.org/10.1016/j.tem.2017.10.001openalex-snapshot
Ghrelin as a Survival Hormone
inferred← citeshttps://doi.org/10.1016/j.tem.2019.07.001openalex-snapshot
Ghrelin-Mediated Hippocampal Neurogenesis: Implications for Health and Disease
inferred← citeshttps://doi.org/10.1016/j.tips.2004.01.010openalex-snapshot
Constitutive ghrelin receptor activity as a signaling set-point in appetite regulation
inferred← citeshttps://doi.org/10.1016/j.tips.2004.02.012openalex-snapshot
Principles: Receptor theory in pharmacology
inferred← citeshttps://doi.org/10.1016/j.yfrne.2004.03.002openalex-snapshot
Ghrelin?a hormone with multiple functions
inferred← citeshttps://doi.org/10.1016/j.yfrne.2009.10.008openalex-snapshot
Ghrelin in the regulation of body weight and metabolism
inferred← citeshttps://doi.org/10.1016/j.ygcen.2013.06.003openalex-snapshot
Changes in the ghrelin hormone pathway maybe part of an unusual gastric system in monotremes
inferred← citeshttps://doi.org/10.1016/j.ygcen.2014.07.021openalex-snapshot
Identification, tissue distribution and functional characterization of the ghrelin receptor in West African lungfish, Protopterus annectens
inferred← citeshttps://doi.org/10.1016/j.ygcen.2017.07.004openalex-snapshot
Biased signaling of G protein-coupled receptors – From a chemokine receptor CCR7 perspective
inferred← citeshttps://doi.org/10.1016/s0083-6729(06)77004-2openalex-snapshot
The Growth Hormone Secretagogue Receptor
inferred← citeshttps://doi.org/10.1016/s0083-6729(06)77005-4openalex-snapshot
Basic Aspects of Ghrelin Action
inferred← citeshttps://doi.org/10.1016/s0083-6729(06)77008-xopenalex-snapshot
Ghrelin Gene‐Related Peptides Modulate Rat White Adiposity
inferred← citeshttps://doi.org/10.1016/s1098-3597(05)80069-9openalex-snapshot
The metabolic syndrome,hyperlipidemia, and insulin resistance
inferred← citeshttps://doi.org/10.1017/cbo9780511541643.010openalex-snapshot
Ghrelin: an orexigenic signal from the stomach
inferred← citeshttps://doi.org/10.1021/acs.analchem.9b03845openalex-snapshot
Early Detection of Growth Hormone Secretagogue Receptor Antagonists Exploiting Their Atypical Behavior in Competitive Assays
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.5c00342openalex-snapshot
Selective Coupling of Aminophosphole-Based Fluorophores to Unprotected Peptides through P–S Bond Formation
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.1c02191openalex-snapshot
Advances in the Development of Nonpeptide Small Molecules Targeting Ghrelin Receptor
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.8b00794openalex-snapshot
Rational Design, Synthesis, and Pharmacological Characterization of Novel Ghrelin Receptor Inverse Agonists as Potential Treatment against Obesity-Related Metabolic Diseases
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.8b01644openalex-snapshot
N-Terminal Liver-Expressed Antimicrobial Peptide 2 (LEAP2) Region Exhibits Inverse Agonist Activity toward the Ghrelin Receptor
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.8b01809openalex-snapshot
The Chimera That Curbs Appetite
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.9b02122openalex-snapshot
Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold
inferred← citeshttps://doi.org/10.1021/acsptsci.3c00088openalex-snapshot
Discovery of Ghrelin(1–8) Analogues with Improved Stability and Functional Activity for PET Imaging
inferred← citeshttps://doi.org/10.1021/jm058053kopenalex-snapshot
Construction of Human Ghrelin Receptor (hGHS-R1a) Model Using a Fragmental Prediction Approach and Validation through Docking Analysis
inferred← citeshttps://doi.org/10.1021/jm300414bopenalex-snapshot
An Aromatic Region To Induce a Switch between Agonism and Inverse Agonism at the Ghrelin Receptor
inferred← citeshttps://doi.org/10.1021/jm5003183openalex-snapshot
Small Molecule Ghrelin Receptor Inverse Agonists and Antagonists
inferred← citeshttps://doi.org/10.1021/jm500610nopenalex-snapshot
Identification, Optimization, and Pharmacology of Acylurea GHS-R1a Inverse Agonists
inferred← citeshttps://doi.org/10.1038/ijo.2009.17openalex-snapshot
Ghrelin and the growth hormone secretagogue receptor in growth and development
inferred← citeshttps://doi.org/10.1038/ijo.2016.235openalex-snapshot
Patterned feeding induces neuroendocrine, behavioral and genetic changes that promote palatable food intake
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