The gonadotrophin-releasing hormone receptor (GnRH receptor, GnRHR) mediates the GnRH signaling pathway, which belongs to the class A G protein-coupled receptor (GPCR) family. Two homologous GnRHR have been identified: type I and type II, and they are found in a variety of organs, including the retina, gonad, certain tumor cells, etc., demonstrating that GnRH receptors exert a variety of functions. Additionally, GnRH receptors function differently in different organs. Consequently, a thorough knowledge of GnRH receptor function will aid in promoting their use as a therapeutic target in illness therapy.
Fig.1 Gonadotropin-releasing hormone (GnRH) receptor-targeted chemotherapy.1
Once GnRH binds, the GnRHR undergoes a conformational change and activates G proteins, resulting in the activation of multiple signaling cascades downstream. These receptors primarily interact with G-proteins of the Gq/ll family, activating phospholipase C and mediating GnRH effects on gonadotropin production and secretion. Strong evidence also suggests that GnRH activates other heterotrimeric G-proteins (Gs and Gi), which may affect the production of cAMP, soluble and insoluble guanylyl cyclases, respectively. The GnRH receptor signaling pathway is an important way to regulate reproductive system function. Considering the GnRH receptor signaling pathway contributes to providing an expanded understanding of its function.
Fig.2 The signaling pathway of GnRH receptor.2
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Fig.3 Benefit of our Magic™ in vitro cell-based gonadotrophin-releasing hormone receptor functional assay service.
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Representative Data 1: The functional experiments revealed that both the K1213.32Q and D982.61A mutations nearly completely eliminated the signaling response to agonist stimulation, demonstrating that the GnRH1R polar network residues K1213.32-D982.61 play crucial roles through interacting with ligands. Several mutations in GnRH1R were created to investigate the impact of the hydrophobic environment and N terminus in the binding pocket of GnRH1R. Nevertheless, these mutants showed a considerably lower reduction of GnRH-induced IP accumulation (IC50) by GnRHR antagonist, illustrating that the N terminus of GnRH1R may be involved in ligand binding and ligand binding requires a hydrophobic environment.
Fig.4 Agonist GnRH dose-dependent responses of GnRH1R.3
Representative Data 2: Endometrial stromal cells (EnSC) were exposed for 5 minutes to hCG, PGE2, or Relaxin-2 to assess the activation of Gs-coupled LHCGR, prostanoid EP2 (PTGER2), and relaxin family peptide receptor 1 (RFXP1) receptors. The proportional quantities of cAMP were comparable to those of receptor transcripts, with LHCGR failing to increase intracellular levels beyond the baseline.
Fig.5 cAMP responses in EnSC following stimulation.4
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