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

Obese children aged 4-6 displayed decreased fasting and postprandial ghrelin levels in response to a test meal

(2018) Jenny Önnerfält et al.   ACTA PAEDIATRICA

Long-term treatment with the ghrelin receptor antagonist [d-Lys3]-GHRP-6 does not improve glucose homeostasis in nonobese diabetic MKR mice

(2018) Rasha Mosa et al.   AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY

LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor

(2018) Xuecai Ge et al.   Cell Metabolism

Differential functional selectivity and downstream signaling bias of ghrelin receptor antagonists and inverse agonists

(2018) Valerie T. Ramirez et al.   FASEB JOURNAL

Inhibition of ghrelin o-acyltransferase attenuated lipotoxicity by inducing autophagy via AMPK–mTOR pathway

(2018) Shaoren Zhang et al.   Drug Design Development and Therapy

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

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

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

Identification and Characterization of a New Series of Ghrelin O-Acyl Transferase Inhibitors

(2017) Mariko Yoneyama-Hirozane et al.   SLAS Discovery

Capromorelin oral solution (ENTYCE®) increases food consumption and body weight when administered for 4 consecutive days to healthy adult Beagle dogs in a randomized, masked, placebo controlled study

(2016) Bill Zollers et al.   BMC Veterinary Research

Pharmacokinetics and pharmacodynamics of PF-05190457: The first oral ghrelin receptor inverse agonist to be profiled in healthy subjects

(2016) William S. Denney et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretionex vivo

(2016) J Kong et al.   BRITISH JOURNAL OF PHARMACOLOGY

GhrelinO-acyltransferase (GOAT), a specific enzyme that modifies ghrelin with a medium-chain fatty acid

(2016) Masayasu Kojima et al.   JOURNAL OF BIOCHEMISTRY

Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model

(2015) Bitoku Takahashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

2-Aminoalkyl nicotinamide derivatives as pure inverse agonists of the ghrelin receptor

(2015) Bitoku Takahashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Neutralizing circulating ghrelin by expressing a growth hormone secretagogue receptor-based protein protects against high-fat diet-induced obesity in mice

(2015) J Gagnon et al.   GENE THERAPY

Diet-induced obesity causes peripheral and central ghrelin resistance by promoting inflammation

(2015) Farhana Naznin et al.   JOURNAL OF ENDOCRINOLOGY

The Effects of Ghrelin Antagonists [D-Lys3]-GHRP-6 or JMV2959 on Ethanol, Water, and Food Intake in C57BL/6J Mice

(2014) Juan L. Gomez et al.   ALCOHOLISM-CLINICAL AND EXPERIMENTAL RESEARCH

Nesfatin-1 correlates with hypertension in overweight or obese Han Chinese population

(2014) Yanyan Zhao et al.   CLINICAL AND EXPERIMENTAL HYPERTENSION

Identification, Optimization, and Pharmacology of Acylurea GHS-R1a Inverse Agonists

(2014) William McCoull et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Anti-ghrelin Spiegelmer inhibits exogenous ghrelin-induced increases in food intake, hoarding, and neural activation, but not food deprivation-induced increases

(2013) Brett J. W. Teubner et al.   AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY

Immunization Against Active Ghrelin Using Virus-Like Particles for Obesity Treatment

(2013) Sara Andrade et al.   CURRENT PHARMACEUTICAL DESIGN

Actions of Agonists and Antagonists of the ghrelin/GHS-R Pathway on GH Secretion, Appetite, and cFos Activity

(2013) Rim Hassouna et al.   Frontiers in Endocrinology

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

Evidence suggesting that ghrelin O-acyl transferase inhibitor acts at the hypothalamus to inhibit hypothalamo-pituitary-adrenocortical axis function in the rat

(2012) Marcin Rucinski et al.   PEPTIDES

In vitro selection of a peptide antagonist of growth hormone secretagogue receptor using cDNA display

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

Therapeutic potential of anamorelin, a novel, oral ghrelin mimetic, in patients with cancer-related cachexia: a multicenter, randomized, double-blind, crossover, pilot study

(2012) José M. Garcia et al.   SUPPORTIVE CARE IN CANCER

Ablation of ghrelin receptor reduces adiposity and improves insulin sensitivity during aging by regulating fat metabolism in white and brown adipose tissues

(2011) Ligen Lin et al.   AGING CELL

A small molecule antagonist of ghrelin O-acyltransferase (GOAT)

(2011) Amanda L. Garner et al.   CHEMICAL COMMUNICATIONS

Ghrelin neutralization during fasting-refeeding cycle impairs the recuperation of body weight and alters hepatic energy metabolism

(2011) Susana Sangiao-Alvarellos et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Differential distribution of ghrelin-O-acyltransferase (GOAT) immunoreactive cells in the mouse and rat gastric oxyntic mucosa

(2010) Andreas Stengel et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Diet-Induced Obesity Causes Ghrelin Resistance in Arcuate NPY/AgRP Neurons

(2010) Dana I. Briggs et al.   ENDOCRINOLOGY

Glucose and Weight Control in Mice with a Designed Ghrelin O-Acyltransferase Inhibitor

(2010) B. P. Barnett et al.   SCIENCE

Colocalization of ghrelin O-acyltransferase and ghrelin in gastric mucosal cells

(2009) Ichiro Sakata et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Anorexigenic and electrophysiological actions of novel ghrelin receptor (GHS-R1A) antagonists in rats

(2009) Nicolas Salomé et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers

(2009) José M. Garcia et al.   GROWTH HORMONE & IGF RESEARCH

Acylated and desacyl ghrelin stimulate lipid accumulation in human visceral adipocytes

(2009) A Rodríguez et al.   INTERNATIONAL JOURNAL OF OBESITY

Efficacy of Ipamorelin, a Novel Ghrelin Mimetic, in a Rodent Model of Postoperative Ileus

(2009) K. Venkova et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Ghrelin Induces Abdominal Obesity Via GHS-R-Dependent Lipid Retention

(2009) Jeffrey S. Davies et al.   MOLECULAR ENDOCRINOLOGY

Identification of the Acyltransferase that Octanoylates Ghrelin, an Appetite-Stimulating Peptide Hormone

(2008) Jing Yang et al.   CELL

Pharmacological Demarcation of the Growth Hormone, Gut Motility and Feeding Effects of Ghrelin Using a Novel Ghrelin Receptor Agonist

(2008) Graeme L. Fraser et al.   ENDOCRINOLOGY

Inhibition of ghrelin O-acyltransferase (GOAT) by octanoylated pentapeptides

(2008) J. Yang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ghrelin octanoylation mediated by an orphan lipid transferase

(2008) J. A. Gutierrez et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA