It is a member of the seven-transmembrane, G-protein coupled receptor (GPCR) family and is activated by the peptide hormone gonadotropin-releasing hormone (GnRH) or the synthetic agonist. The GnRHR is expressed on the surface of pituitary gonadotrope cells as well as lymphocytes, breast, ovary, and prostate. Its activity is critical for successful reproductive function. Several diseases are associated with a dysfunction of this receptor or the corresponding signaling cascade.
You may include any references to papers as in: the use of JSmol in Proteopedia [1] or to the article describing Jmol [2] to the rescue.
Biological Function
The gonadotropin releasing hormone 1 receptor is activated by GnRH which acts upon GnRHRs as the key regulator of puberty and reproduction. This peptide hormone is produced in the hypothalamus but gets secreted and acts upon GnRHRs in the anterior pituitary to exert its effects on reproductive maturation. The activation of the receptor, associates with G-proteins, leads to the releasing of gonadotropic luteinizing hormone (LH) and follicle stimulating hormone (FSH) by activating several signaling cascades. These pathways mainly corresponds to the inositol 1,4,5-triphosphate (IP3) and diacylglycerol (DAG), MAPK, and adenyl cyclase pathways. [3]
Disease
A mutation or a dysfonctionnement of the receptor could cause disease like idiopati hypogonadotropic hypogonadism (HH) which corresponds to a hypogonadism. [4]
Relevance
One of the main using of the couple GnRH - GnRHR in the medicine field is for fertility preservation [5]. Indeed a mutation of the receptor gene sometimes lead to failure of detectable ligand binding
Structural highlights
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- ↑ Hanson, R. M., Prilusky, J., Renjian, Z., Nakane, T. and Sussman, J. L. (2013), JSmol and the Next-Generation Web-Based Representation of 3D Molecular Structure as Applied to Proteopedia. Isr. J. Chem., 53:207-216. doi:https://dx.doi.org/10.1002/ijch.201300024
- ↑ Herraez A. Biomolecules in the computer: Jmol to the rescue. Biochem Mol Biol Educ. 2006 Jul;34(4):255-61. doi: 10.1002/bmb.2006.494034042644. PMID:21638687 doi:10.1002/bmb.2006.494034042644
- ↑ Torrealday S, Lalioti MD, Guzeloglu-Kayisli O, Seli E. Characterization of the gonadotropin releasing hormone receptor (GnRHR) expression and activity in the female mouse ovary. Endocrinology. 2013 Oct;154(10):3877-87. doi: 10.1210/en.2013-1341. Epub 2013 Aug, 2. PMID:23913446 doi:https://dx.doi.org/10.1210/en.2013-1341
- ↑ Meysing AU, Kanasaki H, Bedecarrats GY, Acierno JS Jr, Conn PM, Martin KA, Seminara SB, Hall JE, Crowley WF Jr, Kaiser UB. GNRHR mutations in a woman with idiopathic hypogonadotropic hypogonadism highlight the differential sensitivity of luteinizing hormone and follicle-stimulating hormone to gonadotropin-releasing hormone. J Clin Endocrinol Metab. 2004 Jul;89(7):3189-98. doi: 10.1210/jc.2003-031808. PMID:15240592 doi:https://dx.doi.org/10.1210/jc.2003-031808
- ↑ Torrealday S, Lalioti MD, Guzeloglu-Kayisli O, Seli E. Characterization of the gonadotropin releasing hormone receptor (GnRHR) expression and activity in the female mouse ovary. Endocrinology. 2013 Oct;154(10):3877-87. doi: 10.1210/en.2013-1341. Epub 2013 Aug, 2. PMID:23913446 doi:https://dx.doi.org/10.1210/en.2013-1341