Target intelligence / Profile preview

Acylated Ghrelin (Acyl-ghrelin)

Target
Acyl-ghrelin
Molecular classification
Peptide Hormone, Lipid-modified Peptide, Secreted Protein
01

Overview

Acylated ghrelin is the biologically active form of the peptide hormone ghrelin, characterized by an octanoyl modification at serine-3. This modification is essential for its high-affinity binding and activation of the growth hormone secretagogue receptor 1a (GHSR1a). Acyl-ghrelin plays a crucial role in appetite regulation, growth hormone secretion, and glucose metabolism, making it a potential therapeutic target for conditions like obesity and cachexia. It is produced in the stomach and rapidly degraded into desacyl-ghrelin. Targeting the acylation process or the GHSR1a receptor is an area of active research.

Other names
Octanoyl-ghrelinGhrelin O-octanoateActive Ghrelin
02

Mechanism of action

Binds to and activates growth hormone secretagogue receptor 1a (GHSR1a), a G protein-coupled receptor, leading to downstream signaling cascades that stimulate appetite, growth hormone release, and modulate glucose metabolism.

03

Biological functions

Appetite stimulationGrowth hormone releaseGlucose metabolism regulationAdipogenesisEnergy homeostasis
04

Disease associations

ObesityCachexiaNeurodegenerative diseasesEating disorders
05

Safety considerations

Potential for metabolic dysregulationUnintended effects on growth hormone axisOff-target effects of GOAT inhibitorsPotential impact on cardiovascular function
06

Interacting drugs

Growth hormone secretagogues (GHS)

1 more in the full profile.

07

Biomarkers

Acyl-ghrelin levels in plasmaGHSR1a expression levels

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