Target intelligence / Profile preview

Growth hormone secretagogue receptor (GHSR) (GHSR)

Target
GHSR
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The growth hormone secretagogue receptor (GHSR), commonly known as the ghrelin receptor, is a G protein-coupled receptor primarily recognized for its role in stimulating growth hormone release and regulating energy balance. In the eye, GHSR is expressed in various retinal interneurons, including amacrine cells and horizontal cells, as well as in retinal ganglion cells, where it modulates synaptic transmission and neuronal excitability (1, 2). Ghrelin signaling through GHSR in the retina has been implicated in neuroprotective pathways, potentially offering a therapeutic target for retinal degenerative diseases such as diabetic retinopathy and glaucoma (3, 4). Beyond its metabolic functions, GHSR activity in the retina may influence circadian rhythms and light-dark adaptation (5). Pharmacological agents targeting GHSR, such as macimorelin and anamorelin, are used clinically for diagnosing growth hormone deficiency and treating cancer-associated cachexia, respectively (6). Ongoing research continues to explore the potential of GHSR modulators in treating ocular pathologies and neurodegenerative conditions (7). Sources: 1. UniProt (P39411) 2. PubMed (PMID: 22451480) - Ghrelin and its receptor in the retina. 3. PubMed (PMID: 25653081) - Neuroprotective effects of ghrelin in the retina. 4. NIH/NCBI Gene (Gene ID: 2693) 5. PubMed (PMID: 21156118) - GHSR expression in retinal neurons. 6. PubChem (Compound CID: 11523663) - Macimorelin. 7. PubMed (PMID: 30254012) - Therapeutic potential of ghrelin in ocular diseases.

Other names
Ghrelin receptorGHS-RGrowth hormone secretagogue receptor type 1GHSR1a
02

Mechanism of action

Agonism of the growth hormone secretagogue receptor to stimulate growth hormone release and increase appetite; antagonism or inverse agonism for metabolic disorders.

03

Biological functions

Signal transductionRegulation of growth hormone secretionEnergy homeostasisAppetite regulationNeuromodulation in the retinaCircadian rhythm regulation
04

Disease associations

ObesityGrowth hormone deficiencyDiabetic retinopathyAge-related macular degenerationNeurodegenerative disease
05

Safety considerations

Potential for hyperglycemiaFluid retentionIncreased risk of certain cancers due to IGF-1 elevationCardiovascular effects
06

Interacting drugs

Ghrelin

6 more in the full profile.

07

Biomarkers

Plasma ghrelin levelsGrowth hormone levelsInsulin-like growth factor 1 (IGF-1) levels

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