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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].
Growth hormone-releasing hormone receptor agonist
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