Gonadotrophin-releasing Hormone GPCR Assays
Background of Gonadotrophin-releasing Hormone Receptors
The gonadotropin-releasing hormone receptor (GnRHR), also known as the luteinizing hormone-releasing hormone receptor (LHRHR), is a group of Gq/11-protein-coupled receptors that can mediate the binding and intracellular signaling of GnRH. Genetic mutation and functional disruption of the GnRH receptor may lead to delayed puberty development and even congenital hypogonadotropic hypogonadism (cHH). In this case, the GnRH receptor has served as the important target for infertility and sex steroid-dependent hyperplasias.
Fig.1. Homology model of the inactive human gonadotropin-releasing hormone (GnRH) receptor. (Flanagan, 2017)
Distribution and Function of Gonadotrophin-releasing Hormone Receptors
The expression of GnRH receptors can be detected on the surface of various cell types, such as pituitary gonadotrope cells, lymphocytes, breast, ovary, and prostate. It is primarily responsible for initiating the effects of GnRH upon its release from the hypothalamus to regulate reproductive-related functions and to act back in the progression of certain cancers.
Subtypes and Mechanisms of Gonadotrophin-releasing Hormone Receptors
Gonadotropin-releasing hormone (GnRH) receptors can be divided into two subtypes, including gonadotropin-releasing hormone 1 receptor (GnRHR1) that can be predominantly expressed by pituitary gonadotrophs as well as gonadotropin-releasing hormone 2 receptors (GnRHR2) that is silenced in humans.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| GnRH1 receptor | GnRHR1 |
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| GnRH2 receptor | GnRHR2 |
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Assay List of Gonadotrophin-releasing Hormone Receptor
Creative Biolabs can provide a range of assays of gonadotrophin-releasing hormone receptor. You can choose the assay in the list or contact us for more information:
Published Data
| Paper Title | Gonadotrophin-releasing hormone receptor autoantibodies induce polycystic ovary syndrome-like features in a rat model |
| Journal | Experimental Physiology |
| Published | 2021 |
| Abstract | Studies have shown that gonadotropin-releasing hormone receptor-activating autoantibodies (GnRHR-AAb) have been linked to polycystic ovary syndrome (PCOS). In this paper, we validated the effect of GnRHR-AAb on reproductive function in GnRHR-immunized female rats. All immunized rats produced high titers of GnRHR-AAb targeting a dominant epitope located in the central region of the second extracellular loop of GnRHR. Furthermore, increased pulsatile luteinizing hormone secretion and testosterone concentrations were found in immunized rats. These rats also exhibited various symptoms, such as interrupted estrous cycle, increased ovarian follicular atresia, and activation of insulin signaling in the pituitary gland and ovaries. These symptoms can mimic human patients with PCOS. Our experiments suggest that chronic stimulation of GnRHR by GnRHR-AAb may be a potential etiological mechanism of PCOS. |
| Result |
In conclusion, our series of studies and experiments have demonstrated that GnRHR-AAb may induce reproductive dysfunction by increasing the pulsatile secretion of LH and ovarian androgen production. It is known that GnRHR-AAb can lead to pituitary dysfunction by up-regulating the expression of insulin signaling pathway components. Therefore, our findings provide evidence and new ideas for understanding the pathogenesis of reproductive dysfunction in PCOS and the mechanism of altered insulin signaling pathway in reproductive tissues. Most importantly, targeting GnRHR-AAb may become a new option for PCOS treatment.
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Fig.2. Representative images of the ovaries with Haematoxylin and Eosin staining. (Li, et al., 2021)
References
- Flanagan, C.; Manilall, A. Gonadotropin-releasing hormone (GnRH) receptor structure and GnRH binding. Frontiers in endocrinology. 2017, 8: 274.
- Li, H.; et al. Gonadotrophin‐releasing hormone receptor autoantibodies induce polycystic ovary syndrome‐like features in a rat model. Experimental Physiology. 2021, 106(4): 902-912.
