Capromorelin: a ghrelin receptor agonist and novel therapy for stimulation of appetite in dogs
Sign Up to like & getrecommendations! Published in 2018 at "Veterinary Medicine and Science"
DOI: 10.1002/vms3.83
Abstract: Abstract Ghrelin is a hormone, secreted from cells in the stomach, which is important in the regulation of appetite and food intake in mammals. It exerts its action by binding to a specific G‐protein‐coupled receptor,… read more here.
Keywords: medicine; ghrelin receptor; stimulation appetite; appetite dogs ... See more keywords
Ghrelin and Motilin Control Systems in GI Physiology and Therapeutics.
Sign Up to like & getrecommendations! Published in 2017 at "Handbook of experimental pharmacology"
DOI: 10.1007/164_2016_104
Abstract: Ghrelin and motilin are released from gastrointestinal endocrine cells during hunger, to act through G protein-coupled receptors that have closely related amino acid sequences. The actions of ghrelin are more complex than motilin because ghrelin… read more here.
Keywords: motilin; ghrelin receptor; ghrelin motilin; physiology ... See more keywords
Plasma levels of acylated ghrelin in patients with insulinoma and expression of ghrelin and its receptor in insulinomas
Sign Up to like & getrecommendations! Published in 2020 at "Endocrine"
DOI: 10.1007/s12020-020-02233-4
Abstract: Background Insulinoma is a subtype of pancreatic neuroendocrine tumors. Many patients with insulinoma are obese due to frequent food intake. Ghrelin is associated with obesity and blood levels of insulin. It is not clear if… read more here.
Keywords: ghrelin receptor; ghrelin; patients insulinoma; expression ghrelin ... See more keywords
An insight into the multifunctional role of ghrelin and structure activity relationship studies of ghrelin receptor ligands with clinical trials.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114308
Abstract: Ghrelin is a multifunctional gastrointestinal acylated peptide, primarily synthesized in the stomach and regulates the secretion of growth hormone and energy homeostasis. It plays a central role in modulating the diverse biological, physiological and pathological… read more here.
Keywords: ghrelin receptor; receptor ligands; ghrelin structure; ligands clinical ... See more keywords
Hippocampus ghrelin receptor signaling promotes socially-mediated learned food preference
Sign Up to like & getrecommendations! Published in 2018 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2017.11.039
Abstract: ABSTRACT Social cues are potent regulators of feeding behavior, yet the neurobiological mechanisms through which social cues influence food intake are poorly understood. Here we investigate the hypothesis that the appetite‐promoting gut‐derived hormone, ghrelin, signals… read more here.
Keywords: ghrelin receptor; food preference; stfp; food ... See more keywords
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00828
Abstract: Muscle atrophy and cachexia are common comorbidities among patients suffering from cancer, chronic obstructive pulmonary disease and several other chronic diseases. The peptide hormone ghrelin exerts pleiotropic effects including the stimulation of growth hormone secretion… read more here.
Keywords: ghrelin receptor; receptor full; growth; full agonists ... See more keywords
Structure-Activity Study of Ghrelin(1-8) Resulting in High Affinity Fluorine-Bearing Ligands for the Ghrelin Receptor.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b00164
Abstract: The ghrelin receptor, also known as the growth hormone secretagogue receptor 1a (GHS-R1a), is a G-protein-coupled receptor that is differentially expressed in healthy tissue and several cancers, including prostate, testicular, and ovarian. Selectively targeting the… read more here.
Keywords: ghrelin receptor; affinity; structure activity; receptor ... See more keywords
MRAP2 regulates ghrelin receptor signaling and hunger sensing
Sign Up to like & getrecommendations! Published in 2017 at "Nature Communications"
DOI: 10.1038/s41467-017-00747-6
Abstract: Ghrelin is the only known circulating orexigenic hormone. It is primarily secreted by the stomach and acts at its receptor, the growth hormone secretagogue receptor 1a (GHSR1a), in the hypothalamus to signal hunger and promote… read more here.
Keywords: ghrelin receptor; regulates ghrelin; hunger; melanocortin receptor ... See more keywords
Structure of an antagonist-bound ghrelin receptor reveals possible ghrelin recognition mode
Sign Up to like & getrecommendations! Published in 2020 at "Nature Communications"
DOI: 10.1038/s41467-020-17554-1
Abstract: Ghrelin is a gastric peptide hormone with important physiological functions. The unique feature of ghrelin is its Serine 3 acyl-modification, which is essential for ghrelin’s activity. However, it remains to be elucidated why the acyl-modification… read more here.
Keywords: ghrelin receptor; structure antagonist; ghrelin; antagonist bound ... See more keywords
Allosteric modulation of ghrelin receptor signaling by lipids
Sign Up to like & getrecommendations! Published in 2021 at "Nature Communications"
DOI: 10.1038/s41467-021-23756-y
Abstract: The membrane is an integral component of the G protein-coupled receptor signaling machinery. Here we demonstrate that lipids regulate the signaling efficacy and selectivity of the ghrelin receptor GHSR through specific interactions and bulk effects.… read more here.
Keywords: ghrelin receptor; modulation ghrelin; receptor signaling; receptor ... See more keywords
Pharmacokinetics and pharmacodynamics of PF‐05190457: The first oral ghrelin receptor inverse agonist to be profiled in healthy subjects
Sign Up to like & getrecommendations! Published in 2017 at "British Journal of Clinical Pharmacology"
DOI: 10.1111/bcp.13127
Abstract: AIM To evaluate safety, tolerability and pharmacokinetics of oral PF-05190457, an oral ghrelin receptor inverse agonist, in healthy adults. METHODS Single (SAD) and multiple ascending dose (MAD) studies were randomised, placebo-controlled, double-blind studies. Thirty-five healthy… read more here.
Keywords: receptor inverse; ghrelin receptor; inverse agonist; ghrelin ... See more keywords