Ghrelin
clinical trialsAlso known as: Lenomorelin
Ghrelin, a 28-amino-acid peptide primarily secreted by gastric oxyntic cells, acts as the endogenous ligand for the growth hormone secretagogue receptor (GHS-R1a). Its mechanism of action involves binding to GHS-R1a in the hypothalamus and pituitary, stimulating growth hormone (GH) release, while simultaneously activating orexigenic pathways via neuropeptide Y (NPY) and agouti-related peptide (AgRP) neurons to increase appetite and food intake. Ghrelin also modulates energy balance, gastric motility, and glucose metabolism, with its acylated form (via n-octanoylation at Ser-3) being essential for receptor activation. Key research findings from over 12,900 PubMed references demonstrate ghrelin's role in acute and chronic appetite regulation, with elevated levels observed in fasting states and conditions like cachexia and anorexia nervosa. Clinical trials have explored its therapeutic potential in disorders of appetite dysregulation, including cancer cachexia, where ghrelin administration improved food intake and lean body mass. Additionally, ghrelin's GH-releasing properties have been investigated for growth hormone deficiency and muscle wasting, though results vary due to its short half-life and need for acylated forms. Clinically, ghrelin analogs (e.g., lenomorelin) have advanced to Phase II/III trials for cachexia and gastroparesis, showing modest benefits in weight gain and gastric emptying. However, concerns about hyperglycemia, insulin resistance, and potential tumor growth promotion (via GHS-R1a expression in some cancers) limit widespread use. Current evidence supports ghrelin's role as a biomarker for metabolic states but not as a routine therapeutic agent outside investigational settings. For research purposes only — not medical advice.
Key data
C149H249N47O42Research & studies
Ghrelin gene number varies in Actinopterygii: 41 species lost the gene, 98 have one copy, and 12 have two copies.; Among 110 species with the gene, 182 sequences were identified, with transcript variants ranging from 1 to 6 and encoding 1 to 3 isoform proteins.; Teleost ghrelin proteins form three major evolutionary clades, with Salmoniformes orthologs as a distinct monophyletic cluster.; Synteny analysis shows CCDC174 upstream and TATDN2 downstream of ghrelin, and no positive selection sites were detected, indicating strong functional constraint.
High-fat diet decreased both active and total plasma ghrelin and increased liver LEAP2 mRNA expression along with glucose intolerance.; Switching to a standard diet normalized liver LEAP2 mRNA expression and plasma active ghrelin, but not total ghrelin.; High-fat diet caused resistance to [Dpr3]Ghrelin, reversible by switch to standard diet, followed by resistance to palm-LEAP2(1-14).
Ser-Tyr (SY) potentiated ghrelin sensitivity in the dipeptide library screen; SLVNNDDRDSY, corresponding to β-conglycinin (267-277), enhanced ghrelin sensitivity in vitro; Soy-fortelin enhanced ghrelin's orexigenic activity and stimulated food intake in C57BL/6 mice; Orally administered soy-fortelin strongly stimulated food intake in 2-year-old aged mice with low ghrelin sensitivity
Ghrelin is an endogenous GHSR agonist controlling growth hormone secretion and other functions like food intake and glucose homeostasis.; Desacyl-ghrelin does not bind GHSR at physiological levels and its role is less characterized.; A survey of experts led to consensus terms: 'ghrelin', 'desacyl-ghrelin', 'GHSR', and 'LEAP2'.; Standardized nomenclature aims to reduce confusion and miscommunication in the literature.
Basal ghrelin levels are higher in females than in males.; Ghrelin sensitivity changes across the estrus cycle.; Responses to ghrelin are lower in females and depend on ovarian hormone levels.; Ghrelin promotes both homeostatic and hedonic food intake in females.
Ghrelin and its axis components (UAG, AG, GOAT, GHSR) are implicated in tumor growth and progression, though results are inconsistent.; In1-ghrelin, a splice variant, shows potential as a biomarker for cancer progression.; Unacylated ghrelin (UAG) and acylated ghrelin (AG) have unique characteristics that may differentially affect cancer biology.; Understanding the ghrelin axis mechanisms could lead to novel therapeutic approaches for various cancers.
Acyl-ghrelin stimulates adult hippocampal neurogenesis while unacyl-ghrelin inhibits it.; Parkinson's disease patients with dementia have a reduced acyl-ghrelin:unacyl-ghrelin ratio compared to healthy controls and cognitively intact patients.; Restoring acyl-ghrelin signaling may promote pathways supporting memory function.; Enzymes involved in ghrelin acylation and de-acylation are potential targets for treating mood disorders and dementia.
Frequently asked questions
What is Ghrelin?
Ghrelin, a 28-amino-acid peptide primarily secreted by gastric oxyntic cells, acts as the endogenous ligand for the growth hormone secretagogue receptor (GHS-R1a). Its mechanism of action involves binding to GHS-R1a in the hypothalamus and pituitary, stimulating growth hormone (GH) release, while simultaneously activat
How does Ghrelin work?
Endogenous 28-aa 'hunger hormone' from the stomach; activates GHS-R1a to stimulate GH release and appetite.
What is the research status of Ghrelin?
Ghrelin is currently classified as clinical trials, with 13,112 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of Ghrelin?
Ghrelin has a molecular weight of approximately 3370.9 g/mol (formula C149H249N47O42).
Related peptides
Endogenous cyclic peptide that inhibits GH, insulin, glucagon, and gastric secretion via SSTR1-5 receptors.
First-generation ghrelin receptor agonist hexapeptide that stimulates GH release and strongly increases appetite.
Potent GHRP-family ghrelin receptor agonist with studied cardioprotective effects independent of GH release.
Synthetic hexapeptide ghrelin receptor agonist that potently stimulates GH secretion; also raises appetite, cortisol, and prolactin.
Stabilized GHRH analog approved for HIV-associated lipodystrophy; reduces visceral adipose tissue via GH/IGF-1 axis stimulation.
Selective ghrelin receptor (GHS-R1a) agonist that stimulates GH release with minimal effect on cortisol or prolactin.
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