Design and Characterization of a Triazole-Based Growth Hormone Secretagogue Receptor Modulator Inhibiting the Glucoregulatory and Feeding Actions of Ghrelin

Molecular mechanism of agonism and inverse agonism in ghrelin receptor

(2022) Jiao Qin et al.   Nature Communications

Liver-expressed antimicrobial peptide 2 functions independently of growth hormone secretagogue receptor in calorie-restricted mice

(2022) Md Nurul Islam et al.   PEPTIDES

The ups and downs of growth hormone secretagogue receptor signaling

(2021) María P Cornejo et al.   FEBS Journal

Liver‐Expressed Antimicrobial Peptide 2 antagonizes the insulinostatic effect of ghrelin in rat isolated pancreatic islets

(2021) Morgane Bayle et al.   FUNDAMENTAL & CLINICAL PHARMACOLOGY

Allosteric modulation of ghrelin receptor signaling by lipids

(2021) Marjorie Damian et al.   Nature Communications

The emerging role of heterodimerisation and interacting proteins in ghrelin receptor function

(2021) Maria L Price et al.   JOURNAL OF ENDOCRINOLOGY

Circulating ghrelin crosses the blood-cerebrospinal fluid barrier via growth hormone secretagogue receptor dependent and independent mechanisms

(2021) Maia Uriarte et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Disrupting the ghrelin-growth hormone axis limits ghrelin's orexigenic but not glucoregulatory actions

(2021) Deepali Gupta et al.   Molecular Metabolism

The complex signaling pathways of the Ghrelin receptor

(2020) Morten Adler Hedegaard et al.   ENDOCRINOLOGY

The GPCR accessory protein MRAP2 regulates both biased signaling and constitutive activity of the ghrelin receptor GHSR1a

(2020) Alix A. J. Rouault et al.   Science Signaling

The Insulinostatic Effect of Ghrelin Requires MRAP2 Expression in δ Cells

(2020) Terry C. Yin et al.   iScience

Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold

(2020) Khoubaib Ben Haj Salah et al.   JOURNAL OF MEDICINAL CHEMISTRY

Metabolic insights from a GHSR-A203E mutant mouse model

(2020) Lola J. Torz et al.   Molecular Metabolism

“A LEAP 2 conclusions? Targeting the ghrelin system to treat obesity and diabetes”

(2020) Deepali Gupta et al.   Molecular Metabolism

Ghrelin Regulation of Glucose Metabolism

(2019) Sarah. M. Gray et al.   JOURNAL OF NEUROENDOCRINOLOGY

Ghrelin: From a gut hormone to a potential therapeutic target for alcohol use disorder

(2019) Mehdi Farokhnia et al.   PHYSIOLOGY & BEHAVIOR

Intra-Islet Ghrelin Signaling does not Regulate Insulin Secretion from Adult Mice

(2019) Sarah. M. Gray et al.   DIABETES

The Ellagitannin Metabolite Urolithin C is a Glucose‐Dependent Regulator of Insulin Secretion through L‐type Calcium Channel Activation

(2019) Morgane Bayle et al.   BRITISH JOURNAL OF PHARMACOLOGY

Pharmacological Modulation of Ghrelin to Induce Weight Loss: Successes and Challenges

(2019) Martha A. Schalla et al.   Current Diabetes Reports

LEAP2 changes with body mass and food intake in humans and mice

(2019) Bharath K. Mani et al.   JOURNAL OF CLINICAL INVESTIGATION

Liver-expressed antimicrobial peptide 2 antagonizes the effect of ghrelin in rodents

(2019) Md Nurul Islam et al.   JOURNAL OF ENDOCRINOLOGY

The Homeostatic Force of Ghrelin

(2018) Shigehisa Yanagi et al.   Cell Metabolism

LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor

(2018) Xuecai Ge et al.   Cell Metabolism

Equilibrium Assays are Required to Accurately Characterize the Activity Profiles of Drugs Modulating Gq-Coupled GPCRs

(2018) Sara Bdioui et al.   MOLECULAR PHARMACOLOGY

Ghrelin and LEAP-2: Rivals in Energy Metabolism

(2018) Omar Al-Massadi et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Rational Design, Synthesis and Pharmacological Characterization of Novel Ghrelin Receptor Inverse Agonists as Potential Treatment against Obesity-related Metabolic Diseases

(2018) Antoine Daina et al.   JOURNAL OF MEDICINAL CHEMISTRY

N-Terminal Liver-Expressed Antimicrobial Peptide 2 (LEAP2) Region Exhibits Inverse Agonist Activity toward the Ghrelin Receptor

(2018) Céline M’Kadmi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Brain accessibility delineates the central effects of circulating ghrelin

(2018) Mario Perello et al.   JOURNAL OF NEUROENDOCRINOLOGY

From Belly to Brain: Targeting the Ghrelin Receptor in Appetite and Food Intake Regulation

(2017) Ken Howick et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Therapeutic Potential of Targeting the Ghrelin Pathway

(2017) Gustav Colldén et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Ghrelin as a Survival Hormone

(2017) Bharath K. Mani et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center

(2016) Mathieu Maingot et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

New trisubstituted 1,2,4-triazoles as ghrelin receptor antagonists

(2015) Anne-Laure Blayo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Agonism, Antagonism, and Inverse Agonism Bias at the Ghrelin Receptor Signaling

(2015) Céline M'Kadmi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ghrelin receptor conformational dynamics regulate the transition from a preassembled to an active receptor:Gq complex

(2015) Marjorie Damian et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ghrelin

(2015) T.D. Müller et al.   Molecular Metabolism

Small Molecule Ghrelin Receptor Inverse Agonists and Antagonists

(2014) Kimberly O. Cameron et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate

(2014) Samit K. Bhattacharya et al.   ACS Medicinal Chemistry Letters

Heterodimerization with Its Splice Variant Blocks the Ghrelin Receptor 1a in a Non-signaling Conformation

(2013) Sophie Mary et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Physiologic Concentrations of Exogenously Infused Ghrelin Reduces Insulin Secretion Without Affecting Insulin Sensitivity in Healthy Humans

(2013) Jenny Tong et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist

(2012) Aline Moulin et al.   AMINO ACIDS

An Aromatic Region To Induce a Switch between Agonism and Inverse Agonism at the Ghrelin Receptor

(2012) Sylvia Els et al.   JOURNAL OF MEDICINAL CHEMISTRY

Apo-Ghrelin Receptor Forms Heteromers with DRD2 in Hypothalamic Neurons and Is Essential for Anorexigenic Effects of DRD2 Agonism

(2012) Andras Kern et al.   NEURON

Ghrelin Indirectly Activates Hypophysiotropic CRF Neurons in Rodents

(2012) Agustina Cabral et al.   PLoS One

Ligands and signaling proteins govern the conformational landscape explored by a G protein-coupled receptor

(2012) S. Mary et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

High Constitutive Activity Is an Intrinsic Feature of Ghrelin Receptor Protein

(2011) Marjorie Damian et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Homogeneous time-resolved fluorescence-based assay to screen for ligands targeting the growth hormone secretagogue receptor type 1a

(2010) Jean-Philippe Leyris et al.   ANALYTICAL BIOCHEMISTRY

Ghrelin Suppresses Glucose-Stimulated Insulin Secretion and Deteriorates Glucose Tolerance in Healthy Humans

(2010) J. Tong et al.   DIABETES

Identification and Functional Analysis of Novel Human Growth Hormone Secretagogue Receptor (GHSR) Gene Mutations in Japanese Subjects with Short Stature

(2010) Hiroshi Inoue et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

In VivoCharacterization of High Basal Signaling from the Ghrelin Receptor

(2009) Pia Steen Petersen et al.   ENDOCRINOLOGY