Gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone releasing hormone (LHRH) and luliberin, is synthesized and released from neurons within the hypothalamus []. GnRH is a regulator of reproductive processes, and is responsible for the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary, playing an important role in the control of gonadal function and normal ovarian cyclicity [].There are two major forms of receptor for GnRH, termed GnRHR []and GnRHR2 [], which are members the rhodopsin-like G-protein coupled receptor (GPCR) family. They are expressed on the surface of pituitary gonadotrope cells, as well as lymphocytes, breast, ovary and prostate [, , ]. GnRHR and GnRHR2 couple primarily to Gq/11 []but coupling to Gs and Gi in some systems []. In addition, GnRHR2 may mediate G protein-independent signalling to protein kinases [].Gonadotropin-releasing hormone receptors are of potential therapeutic use in the suppression of prostate cancer and endometriosis, as they have been shown to exert antiproliferative and/or proapoptotic effects on hormone-dependent cancer cells and mediate the effects of cytotoxins [, , , , ]. They may also have application in a number of sex hormone-dependent conditions [, ]. This entry represents the gonadotrophin releasing hormone receptor family and includes GnRHR and GnRHR2.
Gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone releasing hormone (LHRH) and luliberin, is synthesized and released from neurons within the hypothalamus []. GnRH is a regulator of reproductive processes, and is responsible for the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary, playing an important role in the control of gonadal function and normal ovarian cyclicity [].There are two major forms of receptor for GnRH, termed GnRHR []and GnRHR2 [], which are members the rhodopsin-like G-protein coupled receptor (GPCR) family. They are expressed on the surface of pituitary gonadotrope cells, as well as lymphocytes, breast, ovary and prostate [, , ]. GnRHR and GnRHR2 couple primarily to Gq/11 []but coupling to Gs and Gi in some systems []. In addition, GnRHR2 may mediate G protein-independent signalling to protein kinases [].Gonadotropin-releasing hormone receptors are of potential therapeutic use in the suppression of prostate cancer and endometriosis, as they have been shown to exert antiproliferative and/or proapoptotic effects on hormone-dependent cancer cells and mediate the effects of cytotoxins [, , , , ]. They may also have application in a number of sex hormone-dependent conditions [, ]. This entry represents GnRHR2. There is currently some conflict regarding GnRHR2 being a functional protein. In non-hominoid primates and non-mammalian vertebrates GnRHR2 encodes a seven-transmembrane G protein-coupled receptor [, , ]. However, in humans, the N terminus of the predicted protein contains a frameshift and prematurestop codon. GnRHR2 transcription occurs but whether the gene produces a functional C-terminal multi-transmembrane protein is currently unresolved [, , ].
