Gonadotrophin-releasing Hormone Family Related Drug Discovery Products
Creative Biolabs has the assays you can rely on for high throughput screening, lead optimization, characterizing and discovering targets, and uncovering the complexity of disease pathways. We can offer membrane protein in vitro assay kits that save valuable laboratory time and is ideal for high throughput screening.
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
A key regulator of reproductive processes is the decapeptide gonadotrophin-releasing hormone (GnRH) produced in the hypothalamus. It is pulsatilely released from hypothalamic neurons. On the pituitary gonadotrophs, the peptide binds to certain GnRH receptors. The production and secretion of LH and FSH are caused by their activation. Oestradiol and progesterone control the pituitary gland's ability to secrete gonadotrophins in females. The reduction of gonadotrophin secretion during the luteal phase of the menstrual cycle is brought on by these ovarian steroid feedback mechanisms, which also start the mid-cycle LH surge. In the ovary, the gonadotrophins promote gametogenesis and steroidogenesis.
Creative Biolabs offers a range of gonadotrophin-releasing hormone family related assays and products with our well-established high-efficient drug discovery strategy for our clients:
Gonadotrophin-Releasing Hormone GPCR Assays 
GPCR Assay Kits 
GPCR Cell Lines 
GPCR Membranes 
Membrane Protein Tools
Overview of Gonadotrophin-releasing Hormone Family
328 amino acids make up the protein that is encoded by the human pituitary GnRH receptor cDNA. It is a member of the serpentine or seven-transmembrane family of receptors, which makes up the greatest subset of cell surface receptors. These receptors are also referred to as G protein-coupled receptors because they transfer signals via heterotrimeric GTP-binding proteins (G proteins) (GPCR). A number of extra-pituitary organs, including the ovary, testis, placenta, and myometrium, as well as cancerous cells from breast, endometrial, ovarian, and prostate malignancies, have also been found to express GnRH receptor mRNA. GnRH may control cell development and perform paracrine actions in various tissues. The well-known signaling pathways in the pituitary gland are different from the GnRH receptor signaling.
Fig.1 Human GNRHR. (Huirne & Lambalk, 2001)
Signal Transduction
The activation of G9 and G11 proteins by GnRH upon binding to its receptor raises PLC activity. This causes the breakdown of phosphoinositide, which produces inositol phosphates (IP) and diacylglycerol (DAG). It has been demonstrated that ovarian steroids either promote or suppress GnRH-induced IP synthesis. When Ins(1,4,5)P3 binds to particular intracellular receptor channels, the endoplasmic reticulum releases Ca2+. Ca2+ is a crucial intracellular messenger that controls a number of cellular reactions.
Gonadotrophin-releasing Hormone Family Drug Discovery
Although published clinical evidence to date has mostly focused on IVF and prostate cancer, current GnRH antagonists appear to be secure and useful additions to the hormonal arsenal for a variety of illnesses. There is still hope that all of the GnRH agonist therapy's present indications will eventually lend themselves to GnRH antagonist use. Licensed GnRH antagonists are the perfect research instruments for examining the pathophysiology of the human reproductive system in greater detail.
Reference
- Huirne, J.A.; Lambalk, C.B. Gonadotropin-releasing-hormone-receptor antagonists. The Lancet. 2001, 358(9295): 1793-1803.
