Target intelligence / Profile preview

Growth hormone-releasing factor receptor (GHRHR)

Target
GHRHR
Molecular classification
G protein-coupled receptor, GPCR, Secretin family GPCR
01

Overview

The growth hormone-releasing factor receptor (GHRHR) is a G-protein-coupled receptor primarily expressed in the anterior pituitary gland. It binds growth hormone-releasing hormone (GHRH) to stimulate the synthesis and release of growth hormone (GH). This process regulates body size, metabolism, and proliferation/differentiation of somatotroph cells. Mutations are associated with isolated growth-hormone deficiency. It signals through cAMP-dependent and Phospholipase C pathways.

02

Mechanism of action

Binding of GHRH activates Gs protein, leading to increased cAMP and PKA activation, ultimately increasing GH gene transcription and release. Activation via βγ-complex leads to PLC activation, DAG & IP3 production, IP3 increases intracellular Ca²⁺ causing vesicle fusion & GH secretion. Opens Na⁺ channels via phosphatidylinositol 4,5-bisphosphate; depolarization opens voltage-dependent Ca²⁺ channels for further GH release.

03

Biological functions

Signal transductionGrowth hormone releaseRegulation of body sizeRegulation of metabolismSomatotroph cell proliferationSomatotroph cell differentiation
04

Disease associations

Isolated growth-hormone deficiency (IGHD)DwarfismConditions involving abnormal GH secretion
05

Safety considerations

Potential for abnormal GH secretionSide effects related to altered GH/IGF-1 levels

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