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Target intelligence / Profile preview
Growth Hormone-Releasing Hormone Receptor (GHRHR)
- Target
- GHRHR
- Molecular classification
- G protein-coupled receptor, GPCR, Class B GPCR
01
Overview
The Growth Hormone-Releasing Hormone Receptor (GHRHR) is a Class B G protein-coupled receptor primarily expressed in the anterior pituitary gland. It mediates the effects of growth hormone-releasing hormone (GHRH), stimulating the synthesis and release of growth hormone. GHRHR plays a critical role in growth, metabolism, and development. Mutations in GHRHR can lead to isolated growth-hormone deficiency (IGHD). Dysregulation or overexpression of GHRHR has been implicated in various cancers, making it a potential therapeutic target for antagonists.
02
Mechanism of action
Agonist binding activates Gs protein, leading to increased cAMP production and GH synthesis/release. Antagonists block GHRH binding, inhibiting downstream signaling.
03
Biological functions
Signal transductionGrowth hormone synthesis and releaseSomatotroph proliferation and differentiationMetabolism modulation
04
Disease associations
Isolated growth-hormone deficiency (IGHD)DwarfismCancer (prostate, breast, pancreatic, ovarian)
05
Safety considerations
Potential side effects from modulating growth hormone levelsDevelopment of resistance to antagonistsOff-target effects of small molecule antagonists
06
Interacting drugs
Growth hormone-releasing hormone (GHRH)
2 more in the full profile.
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