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

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

The Growth Hormone Secretagogue Receptor: Its Intracellular Signaling and Regulation

(2014) Yue Yin et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

G Protein and β-Arrestin Signaling Bias at the Ghrelin Receptor

(2014) Tama Evron et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ghrelin Receptor (GHS-R1a) and Its Constitutive Activity in Somatotroph Adenomas: A New Co-targeting Therapy Using GHS-R1a Inverse Agonists and Somatostatin Analogs

(2014) Yves Mear et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Functionally biased signalling properties of 7TM receptors - opportunities for drug development for the ghrelin receptor

(2013) B Sivertsen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Functional selectivity of GPCR signaling in animals

(2013) Lei Zhou et al.   CURRENT OPINION IN CELL BIOLOGY

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

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

Functional Signaling Biases in G Protein-Coupled Receptors: Game Theory and Receptor Dynamics

(2012) S. Maudsley et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Deciphering biased-agonism complexity reveals a new active AT1 receptor entity

(2012) Aude Saulière et al.   Nature Chemical Biology

Ghrelin Influences Novelty Seeking Behavior in Rodents and Men

(2012) Caroline Hansson 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

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

The physiological significance and potential clinical applications of ghrelin

(2011) Takashi Akamizu et al.   European Journal of Internal Medicine

High Constitutive Activity Is an Intrinsic Feature of Ghrelin Receptor Protein

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

Unique Interaction Pattern for a Functionally Biased Ghrelin Receptor Agonist

(2011) Bjørn Sivertsen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The role of ghrelin in GH secretion and GH disorders

(2011) Ralf Nass et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Multiple ligand-specific conformations of the β2-adrenergic receptor

(2011) Alem W Kahsai et al.   Nature Chemical Biology

GSK1614343, a Novel Ghrelin Receptor Antagonist, Produces an Unexpected Increase of Food Intake and Body Weight in Rodents and Dogs

(2011) Vivian J.A. Costantini et al.   NEUROENDOCRINOLOGY

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

Discovery Process and Characterization of Novel Carbohydrazide Derivatives as Potent and Selective GHSR1a Antagonists

(2010) Fabio Maria Sabbatini et al.   ChemMedChem

Functional Selectivity and Biased Receptor Signaling

(2010) T. Kenakin   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Therapeutic potential of β-arrestin- and G protein-biased agonists

(2010) Erin J. Whalen et al.   TRENDS IN MOLECULAR MEDICINE

In VivoCharacterization of High Basal Signaling from the Ghrelin Receptor

(2009) Pia Steen Petersen et al.   ENDOCRINOLOGY

Ghrelin-a novel generation of anti-obesity drug: design, pharmacomodulation and biological activity of ghrelin analogues

(2009) Constance Chollet et al.   JOURNAL OF PEPTIDE SCIENCE

Growth Hormone Secretagogues and Growth Hormone Releasing Peptides Act As Orthosteric Super-Agonists but Not Allosteric Regulators for Activation of the G Protein G o1 by the Ghrelin Receptor

(2009) K. A. Bennett et al.   MOLECULAR PHARMACOLOGY

The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex

(2009) X. J. Yao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

New Trisubstituted 1,2,4-Triazole Derivatives as Potent Ghrelin Receptor Antagonists. 3. Synthesis and Pharmacological in Vitro and in Vivo Evaluations

(2008) Aline Moulin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural diversity of G protein-coupled receptors and significance for drug discovery

(2008) Malin C. Lagerström et al.   NATURE REVIEWS DRUG DISCOVERY

Regulation of ERK1/2 activity by ghrelin-activated growth hormone secretagogue receptor 1A involves a PLC/PKCɛ pathway

(2006) Delphine Mousseaux et al.   BRITISH JOURNAL OF PHARMACOLOGY