Glycoprotein 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.
The three gonadotropins, luteinizing hormone (LH), follicle-stimulating hormone (FSH), and chorionic gonadotropin (CG), as well as a fourth nongonadotropin member, thyroid-stimulating hormone (TSH), make up the glycoprotein hormone (GPH) family. The four members are all significant medicinal substances. In women undergoing assisted reproduction, which most frequently involves retrieving oocytes for in vitro fertilization, FSH is used clinically to stimulate the ovaries under controlled conditions. While LH is used to support FSH therapy, it is also utilized to treat hypogonadotropic hypogonadism in males and anovulatory infertility in women. In addition to treating young boys whose testicles do not ordinarily descend into the scrotum, CG is also used to raise sperm count in males and to stimulate ovulation in women.
Fig.1 The glycoprotein hormones. (Vassart, 2004)
Creative Biolabs can provide a wide variety of glycoprotein hormone family related drug discovery assays and products to meet the needs of our clients:
Glycoprotein Hormone GPCR Assays 
GPCR Assay Kits 
GPCR Cell Lines 
GPCR Membranes 
Membrane Protein Tools
Overview of Glycoprotein Hormone Family
According to sequence homology, the G protein-coupled receptors (GPCR) for glycoprotein hormones are members of the Class A, rhodopsin-like GPCR family. These receptors have seven lipophilic, membrane-spanning domains, a relatively short, cytoplasmic carboxy-terminal tail, and large amino-terminal extracellular domains that are necessary for ligand binding. Many leucine rich repeats (LRR), which have been demonstrated to be crucial in the interaction of the receptors with their respective ligands, are present in the extracellular domains of glycoprotein hormones. Glycoprotein hormone receptors have sugar residues on their extracellular domains, just like their hormone ligands. The glycosylation is responsible for the appropriate folding of the receptor during protein synthesis, according to elegant analyses of the role of this glycosylation via mutation of the Asp residues acting as glycosylation sites. TSHR and FSHR are more affected by this than LH/hCGR. Overall, it appears that neither the ligand-binding affinity nor the activation of signal transduction pathways is affected by the receptor's glycosylation status.
Fig.2 Schematic diagram of signaling pathways activated by glycoprotein hormone receptors. (Arey, 2008)
Glycoprotein Hormone Family Drug Discovery
New small molecule allosteric modulators of glycoprotein hormone receptors have evolved with the advent of new synthesis techniques and a better knowledge of GPCR function. Research in this field has shown that it is possible to produce positive and negative modulators that replicate the biological characteristics of native glycoprotein hormones. This is a significant advancement in the creation of therapeutics that are orally active and may be used to treat conditions like cancer, hyperthyroidism, and infertility.
References
- Vassart, G.; et al. A molecular dissection of the glycoprotein hormone receptors. Trends in biochemical sciences. 2004, 29(3): 119-126.
- Arey, B.J. Allosteric modulators of glycoprotein hormone receptors: discovery and therapeutic potential. Endocrine. 2008, 34(1-3): 1-10.
