Growth hormone secretagogue receptor type 1

Function

G protein-coupled receptor specific to ghrelin, an appetite-regulating peptide hormone commonly found in stomach. Upon activation, stimulates appetite and promotes growth hormone secretion. Also binds other growth hormone releasing peptides (GHRP) (e.g. Met-enkephalin and GHRP-6) as well as non-peptide, low molecular weight secretagogues (e.g. L-692, 429, MK-0677, adenosine).

Classification

Family (Pfam)

PF00001 7tm_1

InterPro

GHS-R/MTLR, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM

Functional cluster

Membrane Transporters & GPCRs

Experimental structures · PDB · 10

• 6KO5 X-ray 3.30A
• 7F83 X-ray 2.94A
• 7F9Y EM 2.90A
• 7F9Z EM 3.20A
• 7NA7 EM 2.70A
• 7NA8 EM 2.70A
• 7W2Z EM 2.80A
• 8JSR EM 2.90A
• 9UY3 EM 2.52A
• 9V2N EM 2.63A

A predicted model is available from AlphaFold.

Gene Ontology · 54

• GO:0009986 cell surface
• GO:0098978 glutamatergic synapse
• GO:0045121 membrane raft
• GO:0043005 neuron projection
• GO:0005886 plasma membrane
• GO:0098794 postsynapse
• GO:0098685 Schaffer collateral - CA1 synapse
• GO:0097060 synaptic membrane
• GO:0004930 G protein-coupled receptor activity
• GO:0001616 growth hormone secretagogue receptor activity
• GO:0016520 growth hormone-releasing hormone receptor activity
• GO:0042802 identical protein binding
• GO:0017046 peptide hormone binding
• GO:0008154 actin polymerization or depolymerization
• GO:0008343 adult feeding behavior
• GO:1990314 cellular response to insulin-like growth factor stimulus
• GO:0071222 cellular response to lipopolysaccharide
• GO:0097067 cellular response to thyroid hormone stimulus
• GO:0046697 decidualization
• GO:0007186 G protein-coupled receptor signaling pathway
• GO:0036321 ghrelin secretion
• GO:0030252 growth hormone secretion
• GO:0009755 hormone-mediated signaling pathway
• GO:0007611 learning or memory
• GO:0032099 negative regulation of appetite
• GO:0050728 negative regulation of inflammatory response
• GO:0032691 negative regulation of interleukin-1 beta production
• GO:0032715 negative regulation of interleukin-6 production
• GO:0090327 negative regulation of locomotion involved in locomotory behavior
• GO:2000110 negative regulation of macrophage apoptotic process
• GO:0010700 negative regulation of norepinephrine secretion
• GO:0032720 negative regulation of tumor necrosis factor production
• GO:0032100 positive regulation of appetite
• GO:1904000 positive regulation of eating behavior
• GO:0045923 positive regulation of fatty acid metabolic process
• GO:0040018 positive regulation of multicellular organism growth
• GO:0120058 positive regulation of small intestinal transit
• GO:1904349 positive regulation of small intestine smooth muscle contraction
• GO:1903672 positive regulation of sprouting angiogenesis
• GO:1905564 positive regulation of vascular endothelial cell proliferation
• GO:0099170 postsynaptic modulation of chemical synaptic transmission
• GO:1905333 regulation of gastric motility
• GO:0060123 regulation of growth hormone secretion
• GO:0043134 regulation of hindgut contraction
• GO:0098696 regulation of neurotransmitter receptor localization to postsynaptic specialization membrane
• GO:0099175 regulation of postsynapse organization
• GO:0051969 regulation of transmission of nerve impulse
• GO:0071548 response to dexamethasone
• GO:0032355 response to estradiol
• GO:0032354 response to follicle-stimulating hormone
• GO:0060416 response to growth hormone
• GO:0009725 response to hormone
• GO:1902065 response to L-glutamate
• GO:0007283 spermatogenesis

Disease associations

• short stature due to GHSR deficiency MONDO:0014403

Drugs targeting this protein · 10

• CAPROMORELIN agonist
• ULIMORELIN HYDROCHLORIDE agonist
• ANAMORELIN HYDROCHLORIDE agonist
• IBUTAMOREN MESYLATE agonist
• MACIMORELIN ACETATE agonist
• MACIMORELIN agonist
• TABIMORELIN agonist
• PF-5190457 inverse agonist
• RELAMORELIN agonist
• TZP-102 agonist

Related proteins · sequence + function similarity

• Growth hormone secretagogue receptor type 1 1.00
• Growth hormone secretagogue receptor type 1 1.00
• Growth hormone secretagogue receptor type 1 1.00
• Growth hormone secretagogue receptor type 1 0.99
• Growth hormone secretagogue receptor type 1 0.99
• Neuromedin-U receptor 1 0.83
• Neuromedin-U receptor 2 0.83
• Neuromedin-U receptor 2 0.82
• Neurotensin receptor type 1 0.82
• Neuromedin-U receptor 2 0.82
• Neuromedin-U receptor 1 0.82
• Neuromedin-U receptor 1 0.81

Co-cited proteins · studied together in the literature

• Growth hormone secretagogue receptor type 1 1 shared papers
• Motilin receptor 1 shared papers
• Growth hormone secretagogue receptor type 1 1 shared papers
• Appetite-regulating hormone 2 shared papers
• Appetite-regulating hormone 1 shared papers
• Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 2 shared papers
• Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 2 shared papers

Literature · 9 cited papers

• The structure and function of the ghrelin receptor coding for drug actions. Nat. Struct. Mol. Biol. · 2025
• Molecular mechanism of agonism and inverse agonism in ghrelin receptor. Nat. Commun. · 2022
• Recessive isolated growth hormone deficiency and mutations in the ghrelin receptor. J. Clin. Endocrinol. Metab. · 2009
• Loss of constitutive activity of the growth hormone secretagogue receptor in familial short stature. J. Clin. Invest. · 2006
• The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
• Genomic structure and transcriptional regulation of the human growth hormone secretagogue receptor. Endocrinology · 2001
• Growth hormone secretagogue receptor family members and ligands. Endocrine · 2001
• Ghrelin is a growth-hormone-releasing acylated peptide from stomach. Nature · 1999
• A receptor in pituitary and hypothalamus that functions in growth hormone release. Science · 1996