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25 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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GHSR
growth hormone secretagogue receptor
Chromosome 3 · 3q26.31
NCBI Gene: 2693Ensembl: ENSG00000121853.4HGNC: HGNC:4267UniProt: Q92847
171PubMed Papers
21Diseases
13Drugs
2Pathogenic Variants
FUNCTIONAL ROLE
Receptor
RESEARCH IMPACT
Trending
CLINICAL
FDA Approved TargetOMIM Disease Gene
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
positive regulation of multicellular organism growthG protein-coupled receptor activitygrowth hormone-releasing hormone receptor activityneuron projectionshort stature due to GHSR deficiencynon-small cell lung carcinomaAbnormality of the skeletal systemshort stature due to partial GHR deficiency
✦AI Summary

GHSR (growth hormone secretagogue receptor) is a G-protein-coupled receptor that serves as the specific receptor for ghrelin, a 28-amino acid acylated peptide hormone primarily produced in the stomach 1. Upon ghrelin binding, GHSR stimulates growth hormone release from the pituitary and regulates appetite and energy balance 1. The receptor is expressed throughout the brain, particularly in the hypothalamus, and mediates ghrelin's effects on feeding behavior and metabolic processes 23. GHSR exhibits unique ligand-independent constitutive activity, making it an attractive therapeutic target 4. The ghrelin-GHSR system demonstrates complex roles in disease states: it contributes to hyperglycemia and insulin resistance in type 2 diabetes 5, while paradoxically showing anti-inflammatory properties in rheumatoid arthritis through PI3K/AKT pathway modulation 6. The receptor also influences mental health disorders by affecting neurotransmitter systems including dopamine, GABA, and serotonin 2. Clinically, GHSR shows promise as a therapeutic target for obesity, with genetic or pharmacological blockade demonstrating protective effects against diet-induced obesity in a sexually dimorphic manner 4. The system's involvement in cancer progression and metabolic disorders highlights its significance in multiple pathophysiological processes 7.

Sources cited
1
GHSR is the receptor for ghrelin, a 28-amino acid acylated peptide that stimulates growth hormone release
PMID: 10604470
2
GHSR is expressed in brain regions including hypothalamus and mediates ghrelin's effects on neurotransmitter systems and mental health
PMID: 40226675
3
GHSR is expressed in hypothalamic neurons and shows selective colocalization with other metabolic receptors
PMID: 39737802
4
GHSR has ligand-independent constitutive activity and genetic/pharmacological blockade shows sexually dimorphic effects on diet-induced obesity
PMID: 38796563
5
Ghrelin-GHSR system contributes to hyperglycemia and insulin resistance in type 2 diabetes
PMID: 41069857
6
GHSR shows anti-inflammatory properties in rheumatoid arthritis through PI3K/AKT pathway modulation
PMID: 40339721
7
GHSR is involved in cancer progression processes including metastasis and proliferation
PMID: 28238732
Disease Associationsⓘ21
short stature due to GHSR deficiencyOpen Targets
0.67Moderate
non-small cell lung carcinomaOpen Targets
0.50Moderate
Abnormality of the skeletal systemOpen Targets
0.49Moderate
short stature due to partial GHR deficiencyOpen Targets
0.40Weak
fibromyalgiaOpen Targets
0.39Weak
colorectal cancerOpen Targets
0.39Weak
cancerOpen Targets
0.39Weak
gastric cancerOpen Targets
0.37Weak
Malignant Pancreatic NeoplasmOpen Targets
0.37Weak
pancreatic neoplasmOpen Targets
0.37Weak
CachexiaOpen Targets
0.37Weak
genetic disorderOpen Targets
0.34Weak
connective tissue diseaseOpen Targets
0.30Weak
ileusOpen Targets
0.29Weak
gastroparesisOpen Targets
0.28Weak
Disorder of carbohydrate metabolismOpen Targets
0.26Weak
inborn carbohydrate metabolic disorderOpen Targets
0.26Weak
Escherichia coli InfectionsOpen Targets
0.23Weak
renal osteodystrophyOpen Targets
0.20Weak
Short statureOpen Targets
0.12Weak
Growth hormone deficiency, isolated partialUniProt
Pathogenic Variants2
NM_198407.2(GHSR):c.517T>C (p.Cys173Arg)Likely pathogenic
not provided
★☆☆☆2023→ Residue 173
NM_198407.2(GHSR):c.6G>A (p.Trp2Ter)Pathogenic
Short stature due to growth hormone secretagogue receptor deficiency
☆☆☆☆2009→ Residue 2
View on ClinVar ↗
Drug Targets13
ANAMORELINPhase III
Ghrelin receptor agonist
Disorder of carbohydrate metabolism
ANAMORELIN HYDROCHLORIDEApproved
Ghrelin receptor agonist
cancer
CAPROMORELINPhase II
Ghrelin receptor agonist
IBUTAMORENApproved
Ghrelin receptor agonist
fibromyalgia
IBUTAMOREN MESYLATEPhase II
Ghrelin receptor agonist
MACIMORELINApproved
Ghrelin receptor agonist
MACIMORELIN ACETATEPhase I
Ghrelin receptor agonist
PF-5190457Phase II
Ghrelin receptor inverse agonist
alcohol dependence
RELAMORELINPhase III
Ghrelin receptor agonist
gastroparesis
TABIMORELINPhase II
Cytochrome P450 3A4 inhibitor
TZP-102Phase II
Ghrelin receptor agonist
ULIMORELINPhase II
Ghrelin receptor agonist
ULIMORELIN HYDROCHLORIDEPhase III
Ghrelin receptor agonist
ileus
Related Genes
GNB1Protein interaction99%GNAQProtein interaction97%GNAI1Protein interaction97%MBOAT4Protein interaction95%GNG2Protein interaction95%GNA11Protein interaction94%
Tissue Expression6 tissues
Brain
100%
Bone Marrow
0%
Heart
0%
Ovary
0%
Liver
0%
Lung
0%
Gene Interaction Network
Click a node to explore
GHSRGNB1GNAQGNAI1MBOAT4GNG2GNA11
PROTEIN STRUCTURE
Preparing viewer…
PDB9UY3 · 2.52 Å · EM
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.03LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.69 [0.47–1.03]
RankingsWhere GHSR stands among ~20K protein-coding genes
  • #2,576of 20,598
    Most Researched171 · top quartile
  • #466of 1,025
    FDA-Approved Drug Targets3
  • #4,258of 5,498
    Most Pathogenic Variants2
  • #10,235of 17,882
    Most Constrained (LOEUF)1.03
Genes detectedGHSR
Sources retrieved25 papers
Response time—
📄 Sources
25â–¼
1
Ghrelin is a growth-hormone-releasing acylated peptide from stomach.
PMID: 10604470
Nature · 1999
1.00
2
The Pathologic Roles and Therapeutic Implications of Ghrelin/GHSR System in Mental Disorders.
PMID: 40226675
Depress Anxiety · 2024
0.90
3
Obesity as the Sequel of Childhood Stunting: Ghrelin and GHSR Gene Polymorphism Explained.
PMID: 29950536
Acta Med Indones · 2018
0.80
4
Hunger, ghrelin and the gut.
PMID: 29366626
Brain Res · 2018
0.76
5
Lipids modulate the dynamics of GPCR:β-arrestin interaction.
PMID: 40442125
Nat Commun · 2025
0.72