Homologous regulation of gonadotropin-releasing hormone receptors in cultured pituitary cells

Background: Gonadotropin-Releasing Hormone (GnRH) is a key element in sexual maturation and regulation of the reproductive cycle in the human organism. GnRH interacts with the pituitary cells through the activation of the Gonadotropin Releasing Hormone Receptors (GnRHR). Any impairments/dysfunctions of the GnRH-GnRHR complex lead to the development of various cancer types and disorders. Furthermore, the identification of GnRHR as a potential drug target has led to the development of agonist and antagonist molecules implemented in various treatment protocols. The development of these drugs was based on the information derived from the functional studies of GnRH and GnRHR. Objective: This review aims at shedding light on the versatile function of GnRH and GnRH receptor and offers an apprehensive summary regarding the development of different agonists, antagonists and non-peptide GnRH analogues. Conclusion: The information derived from these studies can enhance our understanding of the GnRH-GnRHR versatile nature and offer valuable insight into the design of new more potent molecules.

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Photoaffinity labeling of gonadotropin releasing hormone receptors in control and desensitized pituitary cells

Biochemical and Biophysical Research Communications ◽

10.1016/0006-291x(84)90572-2 ◽

1984 ◽

Vol 125 (2) ◽

pp. 532-538 ◽

Cited By ~ 11

Author(s):

E. Hazum ◽

I. Schvartz

Keyword(s):

Hormone Receptors ◽

Photoaffinity Labeling ◽

Gonadotropin Releasing Hormone ◽

Pituitary Cells ◽

Releasing Hormone

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Endocrine and molecular milieus of ovarian follicles are diversely affected by human chorionic gonadotropin and gonadotropin-releasing hormone in prepubertal and mature gilts

Scientific Reports ◽

10.1038/s41598-021-91434-6 ◽

2021 ◽

Vol 11 (1) ◽

Author(s):

Adam J. Ziecik ◽

Jan Klos ◽

Katarzyna Gromadzka-Hliwa ◽

Mariola A. Dietrich ◽

Mariola Slowinska ◽

...

Keyword(s):

Chorionic Gonadotropin ◽

Human Chorionic Gonadotropin ◽

Hormone Receptors ◽

Cell Function ◽

Ovarian Follicle ◽

Molecular Transport ◽

Gonadotropin Releasing Hormone ◽

Matrix Remodeling ◽

Releasing Hormone ◽

Serum Gonadotropin

AbstractDifferent strategies are used to meet optimal reproductive performance or manage reproductive health. Although exogenous human chorionic gonadotropin (hCG) and gonadotropin-releasing hormone (GnRH) agonists (A) are commonly used to trigger ovulation in estrous cycle synchronization, little is known about their effect on the ovarian follicle. Here, we explored whether hCG- and GnRH-A-induced native luteinizing hormone (LH) can affect the endocrine and molecular milieus of ovarian preovulatory follicles in pigs at different stages of sexual development. We collected ovaries 30 h after hCG/GnRH-A administration from altrenogest and pregnant mare serum gonadotropin (eCG)-primed prepubertal and sexually mature gilts. Several endocrine and molecular alternations were indicated, including broad hormonal trigger-induced changes in follicular fluid steroid hormones and prostaglandin levels. However, sexual maturity affected only estradiol levels. Trigger- and/or maturity-dependent changes in the abundance of hormone receptors (FSHR and LHCGR) and proteins associated with lipid metabolism and steroidogenesis (e.g., STAR, HSD3B1, and CYP11A1), prostaglandin synthesis (PTGS2 and PTGFS), extracellular matrix remodeling (MMP1 and TIMP1), protein folding (HSPs), molecular transport (TF), and cell function and survival (e.g., VIM) were observed. These data revealed different endocrine properties of exogenous and endogenous gonadotropins, with a potent progestational/androgenic role of hCG and estrogenic/pro-developmental function of LH.

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