Target intelligence / Profile preview

Growth hormone-releasing hormone receptor (GHRHR) (GHRHR)

Target
GHRHR
Molecular classification
G protein-coupled receptor (Class B), Receptor
01

Overview

The growth hormone-releasing hormone receptor (GHRHR) is a member of the Class B G protein-coupled receptor family, primarily localized on the somatotroph cells of the anterior pituitary gland [1, 2]. Its fundamental biological role is to mediate the activity of hypothalamic growth hormone-releasing hormone (GHRH), which triggers the synthesis and pulsatile secretion of growth hormone (GH) through the activation of the adenylyl cyclase/cAMP signaling pathway [1, 8]. Genetic mutations in the GHRHR gene are a major cause of isolated growth hormone deficiency (IGHD), leading to severe growth retardation and pituitary dwarfism [3, 19]. In pharmacological contexts, the receptor is targeted by GHRH analogs such as tesamorelin, which is utilized to treat HIV-associated lipodystrophy by stimulating endogenous GH production to reduce visceral adiposity [6, 11]. Additionally, sermorelin and somatorelin serve as diagnostic and therapeutic agents for assessing pituitary function and treating GH deficiencies [12, 13]. Beyond its pituitary role, GHRHR and its splice variants are overexpressed in several human cancers, where they may act as mitogens, making the receptor a target for research into peptide antagonists for oncology [15, 17].

Other names
GHRFRGHRH-RGrowth hormone-releasing factor receptorGRFRSomatotropin-releasing hormone receptor
02

Mechanism of action

Growth hormone-releasing hormone receptor agonist

03

Biological functions

Signal transductionGrowth hormone secretionSomatotroph proliferationCell proliferation
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Disease associations

Growth hormone deficiencyPituitary dwarfismLipodystrophyCancer
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Safety considerations

Fluid retentionPeripheral edemaArthralgiaHyperglycemiaIncreased insulin resistancePotential for promoting tumor growth
06

Interacting drugs

Tesamorelin

2 more in the full profile.

07

Biomarkers

Growth hormone (GH)Insulin-like growth factor 1 (IGF-1)

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