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 functions in vertebrates. The synthesis of ghrelin receptor ligands after the finding of growth hormone secretagogue developed from Met-enkephalin led to reveal the endogenous ligand ghrelin and the receptors. Subsequently, many peptides, small molecules and peptidomimetics focusing on the ghrelin receptor, GHS-R1a, were derived. In this review, the key features of ghrelin's structure, forms, its bio-physiological functions, pathological roles and therapeutic potential have been highlighted. A few peptidomimetics and pseudo peptide synthetic perspectives have also been discussed to make ghrelin receptor ligands, clinical trials and their success.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2022.114308 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Intranasal delivery of a ghrelin mimetic engages the brain ghrelin signalling system in mice.
Endocrinology
January 2025
Department of Physiology/Endocrine, Institute of Neuroscience and Physiology, The Sahlgrenska Academy at the University of Gothenburg, Sweden.
Ghrelin, the endogenous ligand of the growth hormone secretagogue receptor (GHSR), promotes food intake, other feeding behaviours and stimulates growth hormone (GH) release from the pituitary. Growth hormone secretagogues (GHS), such as GHRP-6 and MK-0677, are synthetic GHSR ligands that activate orexigenic Neuropeptide Y neurons that co-express Agouti-Related Peptide (AgRP) in the arcuate nucleus of the hypothalamus when administered systemically. Systemic GHRP-6 also stimulates GH release in humans and rats.
View Article and Find Full Text PDFReal-time detection of somatostatin release from single islets reveals hypersecretion in type 2 diabetes.
Acta Physiol (Oxf)
February 2025
Department of Medical Cell Biology, Uppsala University, Uppsala, Sweden.
Aim: Somatostatin from pancreatic δ-cells is a paracrine regulator of insulin and glucagon secretion, but the release kinetics and whether secretion is altered in diabetes is unclear. This study aimed to improve understanding of somatostatin secretion by developing a tool for real-time detection of somatostatin release from individual pancreatic islets.
Methods: Reporter cells responding to somatostatin with cytoplasmic Ca concentration ([Ca]) changes were generated by co-expressing somatostatin receptor SSTR2, the G-protein Gα15 and a fluorescent Ca sensor in HeLa cells.
Ghrelin Promotes Lipid Uptake into White Adipose Tissue via Endothelial Growth Hormone Secretagogue-Receptor in Mice.
Nutrients
December 2024
Division of Nephrology, Endocrinology and Metabolism, Department of Internal Medicine, Keio University School of Medicine, Shinjuku-ku, Tokyo 160-8582, Japan.
: Endothelial peroxisome proliferator-activated receptor gamma (PPARγ) regulates adipose tissue by facilitating lipid uptake into white adipocytes, but the role of endothelial lipid transport in systemic energy balance remains unclear. Ghrelin conveys nutritional information through the central nervous system and increases adiposity, while deficiency in its receptor, growth hormone secretagogue-receptor (GHSR), suppresses adiposity on a high-fat diet. This study aims to examine the effect of ghrelin/GHSR signaling in the endothelium on lipid metabolism.
View Article and Find Full Text PDFInvestigation of the association between therapeutic effectiveness of anamorelin and Glasgow prognostic score in patients with cancer cachexia: a competing risk analysis.
Invest New Drugs
January 2025
Department of Pharmacy, Aichi Cancer Center Hospital, 1-1, Kanokoden, Chikusa-Ku, Nagoya, Aichi, 464-8681, Japan.
Anamorelin, a highly selective ghrelin receptor agonist, enhances appetite and increases lean body mass in patients with cancer cachexia. However, the predictors of its therapeutic effectiveness are uncertain. This study aimed to investigate the association between the Glasgow prognostic score (GPS), used for classifying the severity of cancer cachexia, the therapeutic effectiveness of anamorelin, and the feasibility of early treatment based on cancer types.
View Article and Find Full Text PDFLoss-of-function GHSR variants are associated with short stature and low IGF-I.
J Clin Endocrinol Metab
January 2025
Division of Pediatric Endocrinology, Department of Pediatrics, Willem-Alexander Children's Hospital, Leiden University Medical Centre, Leiden, The Netherlands.
Context: The growth hormone (GH) secretagogue receptor, encoded by GHSR, is expressed on somatotrophs of the pituitary gland. Stimulation with its ligand ghrelin, as well as its constitutive activity, enhances GH secretion. Studies in knock-out mice suggest that heterozygous loss-of-function of GHSR is associated with decreased GH response to fasting, but patient observations in small case reports have been equivocal.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!