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Target intelligence / Profile preview
Growth Hormone Secretagogue Receptor (GHS-R)
- Target
- GHS-R
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The Growth Hormone Secretagogue Receptor (GHSR), also known as the ghrelin receptor, is a G protein-coupled receptor that mediates the effects of growth hormone secretagogues, including the endogenous ligand ghrelin. GHSR plays a central role in stimulating growth hormone release, regulating appetite and energy homeostasis, modulating glucose and lipid metabolism, influencing gastrointestinal motility and secretion, protecting neuronal and cardiovascular cells, and regulating immune function. Targeted by drugs aiming to treat conditions like cachexia/anorexia nervosa, cardiovascular diseases, metabolic syndrome, age-related decline in GH/IGF axis, and potentially neurodegenerative disorders. Antagonists/inverse agonists are being explored for obesity treatment due to their ability to suppress appetite.
- Other names
- ghrelin receptorGHSR
02
Mechanism of action
Agonists bind to GHSR, activating G proteins (primarily Gαq/11), increasing intracellular calcium levels, and stimulating growth hormone secretion. Antagonists/inverse agonists suppress appetite.
03
Biological functions
Growth hormone release stimulationAppetite regulationEnergy homeostasisGlucose and lipid metabolism modulationGastrointestinal motility and secretion regulationNeuroprotectionCardioprotectionImmune system modulationSignal transduction
04
Disease associations
CachexiaAnorexia nervosaCardiovascular diseasesMetabolic syndromeObesityNeurodegenerative disorders
05
Safety considerations
Potential cardiovascular effectsOff-target effects due to widespread tissue expressionUnintended consequences of appetite manipulation
06
Interacting drugs
Ghrelin
2 more in the full profile.
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