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Gene Review

Gnrhr  -  gonadotropin releasing hormone receptor

Rattus norvegicus

Synonyms: GH1, GnRH receptor, GnRH-R, Gonadotropin-releasing hormone receptor, Lhrhr
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Disease relevance of Gnrhr


Psychiatry related information on Gnrhr


High impact information on Gnrhr

  • The prolonged in vivo inhibition of pituitary GnRH receptor binding and luteinizing hormone secretion by the GnRH antagonist may be mediated by the slower dissociation rate of the antagonist from its specific pituitary membrane receptor site [7].
  • These findings suggest that an agonist concentration-dependent switch in coupling of the GnRH-R between specific G proteins modulates neuronal Ca(2+) signaling via G(s)-cAMP stimulatory and G(i)-cAMP inhibitory mechanisms [8].
  • We have overcome this limitation by transfecting the rat pituitary GH3 cell line with rat GnRH receptor (GnRHR) cDNA driven by a heterologous promoter [9].
  • Taken together, these results indicate that the GnRH receptor activates both G(q) and G(s) signaling to regulate gene expression in L beta T2 cells [10].
  • In contrast to other GPCRs, the GnRH-R does not show rapid desensitization of total inositol (IP) production, and the rates of internalization are exceptionally slow [11].

Chemical compound and disease context of Gnrhr


Biological context of Gnrhr

  • Three different rat GnRH-R cDNA stop codon mutations (one for each reading frame) were also made [11].
  • We studied the expression patterns of GnRH and GnRH receptor (GnRH-R) in the same animals throughout the estrous cycle using real-time PCR [13].
  • No significant changes in the level of hypothalamic GnRH-R mRNA were detected, although fluctuations during the day of proestrus are evident [13].
  • Pituitary GnRH-R displayed a similar pattern of expression, except on estrus, when its mRNA levels declined [13].
  • A reduction of GnRH-R is part of the mechanism of down-regulation of LH secretion by fast or slow GnRH frequencies, but altered frequency also exerts effects on secretory mechanisms at a site distal to the GnRH receptor [14].

Anatomical context of Gnrhr


Associations of Gnrhr with chemical compounds


Physical interactions of Gnrhr


Regulatory relationships of Gnrhr

  • In the presence of transcription inhibitor, GnRH-induced augmentation of GnRH-R mRNA levels was completely abolished [20].
  • We have proposed a model for GnRH self-priming that requires cross-communication between a GnRH receptor-activated protein kinase A pathway and the progesterone receptor (PR) to achieve amplification of the GnRH signal [26].
  • Moreover, galanin also up-regulated GnRH receptor functional parameters (affinity and maximum binding capacity) but was ineffective in potentiating GnRH-induced accumulation of both subunit mRNAs [27].
  • We previously reported that a blockade of GnRH receptor activation inhibited the already-initiated C-kinase pathway(s) [28].

Other interactions of Gnrhr

  • Coupling of the agonist-activated GnRH-R to both G(s) and G(i) proteins was demonstrated by the ability of nanomolar GnRH concentrations to reduce membrane-associated alpha(s) and alpha(i3) levels and of higher concentrations to diminish alpha(i3) levels [8].
  • The beta-arrestin-promoted increase in the k(e) value was diminished by cotransfecting cells with the dominant negative beta-arrestin-(319-418) mutant, whereas WT GnRH-R and stop codon mutant internalization were unaffected [29].
  • This study examined the mechanism underlying the rat GnRH receptor (GnRH-R) internalization pathway by investigating the role of added/extended C-terminal tails and the effect of beta-arrestins and dynamin [29].
  • Castration induced a 3.8-fold elevation in the amounts of GnRH-R mRNA after 3 weeks, whereas alpha, LH beta, and FSH beta mRNAs increased by 6.2-, 7.9-, and 4.2-fold, respectively, compared to corresponding values in intact animals [30].
  • Similarly, administration of ovine PRL (during the first 48 h) to bromocriptine-treated rats produced low GnRH-R concentrations at 72 h [31].

Analytical, diagnostic and therapeutic context of Gnrhr


  1. Rat gonadotropin-releasing hormone receptor expressed in insect cells induces activation of adenylyl cyclase. Delahaye, R., Manna, P.R., Bérault, A., Berreur-Bonnenfant, J., Berreur, P., Counis, R. Mol. Cell. Endocrinol. (1997) [Pubmed]
  2. Pituitary gonadotropin-releasing hormone (GnRH) receptor responses to GnRH in hypothalamus-lesioned rats: inhibition of responses by hyperprolactinemia and evidence that testosterone and estradiol modulate gonadotropin secretion at postreceptor sites. Pieper, D.R., Gala, R.R., Schiff, M.A., Regiani, S.R., Marshall, J.C. Endocrinology (1984) [Pubmed]
  3. Expression of gonadotropin-releasing hormone receptor mRNA in the rat ventral prostate and dunning R3327 PAP adenocarcinoma before and after castration. Tieva, A., Wilkström, P., Olofsson, J.I., Bergh, A., Damber, J.E. Prostate (1999) [Pubmed]
  4. Unexpected effects of epitope and chimeric tags on gonadotropin-releasing hormone receptors: implications for understanding the molecular etiology of hypogonadotropic hypogonadism. Brothers, S.P., Janovick, J.A., Conn, P.M. J. Clin. Endocrinol. Metab. (2003) [Pubmed]
  5. Gonadotropin releasing hormone agonist provokes homologous receptor microaggregation: an early event in seven-transmembrane receptor mediated signaling. Janovick, J.A., Conn, P.M. Endocrinology (1996) [Pubmed]
  6. Gonadotropin-releasing hormone binding sites in ovaries of normal cycling and persistent-estrus rats. Köves, K., Gottschall, P.E., Arimura, A. Biol. Reprod. (1989) [Pubmed]
  7. Pituitary receptor site blockade by a gonadotropin-releasing hormone antagonist in vivo: mechanism of action. Heber, D., Dodson, R., Swerdloff, R.S., Channabasavaiah, K., Stewart, J.M. Science (1982) [Pubmed]
  8. An agonist-induced switch in G protein coupling of the gonadotropin-releasing hormone receptor regulates pulsatile neuropeptide secretion. Krsmanovic, L.Z., Mores, N., Navarro, C.E., Arora, K.K., Catt, K.J. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  9. A mechanism for the differential regulation of gonadotropin subunit gene expression by gonadotropin-releasing hormone. Kaiser, U.B., Sabbagh, E., Katzenellenbogen, R.A., Conn, P.M., Chin, W.W. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  10. Involvement of both G(q/11) and G(s) proteins in gonadotropin-releasing hormone receptor-mediated signaling in L beta T2 cells. Liu, F., Usui, I., Evans, L.G., Austin, D.A., Mellon, P.L., Olefsky, J.M., Webster, N.J. J. Biol. Chem. (2002) [Pubmed]
  11. Gonadotropin-releasing hormone receptors with intracellular carboxyl-terminal tails undergo acute desensitization of total inositol phosphate production and exhibit accelerated internalization kinetics. Heding, A., Vrecl, M., Bogerd, J., McGregor, A., Sellar, R., Taylor, P.L., Eidne, K.A. J. Biol. Chem. (1998) [Pubmed]
  12. Suppression of pulsatile LH secretion, pituitary GnRH receptor content and pituitary responsiveness to GnRH by hyperprolactinemia in the male rat. Fox, S.R., Hoefer, M.T., Bartke, A., Smith, M.S. Neuroendocrinology (1987) [Pubmed]
  13. Differential gonadotropin-releasing hormone (GnRH) and GnRH receptor messenger ribonucleic acid expression patterns in different tissues of the female rat across the estrous cycle. Schirman-Hildesheim, T.D., Bar, T., Ben-Aroya, N., Koch, Y. Endocrinology (2005) [Pubmed]
  14. The frequency of gonadotropin-releasing hormone stimulation determines the number of pituitary gonadotropin-releasing hormone receptors. Katt, J.A., Duncan, J.A., Herbon, L., Barkan, A., Marshall, J.C. Endocrinology (1985) [Pubmed]
  15. Structure-activity relations of successful pharmacologic chaperones for rescue of naturally occurring and manufactured mutants of the gonadotropin-releasing hormone receptor. Janovick, J.A., Goulet, M., Bush, E., Greer, J., Wettlaufer, D.G., Conn, P.M. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  16. Negative regulation of gonadotropin-releasing hormone and gonadotropin-releasing hormone receptor gene expression by a gonadotrophin-releasing hormone agonist in the rat hypothalamus. Han, Y.G., Kang, S.S., Seong, J.Y., Geum, D., Suh, Y.H., Kim, K. J. Neuroendocrinol. (1999) [Pubmed]
  17. Nucleotide sequence analysis of mRNAs predicts that rat pituitary and gonadal gonadotropin-releasing hormone receptor proteins have identical primary structure. Moumni, M., Kottler, M.L., Counis, R. Biochem. Biophys. Res. Commun. (1994) [Pubmed]
  18. Progesterone together with estrogen attenuates homologous upregulation of gonadotropin-releasing hormone receptor mRNA in primary cultured rat pituitary cells. Cheon, M., Park, D., Park, Y., Kam, K., Park, S.D., Ryu, K. Endocrine (2001) [Pubmed]
  19. Position of Pro and Ser near Glu7.32 in the extracellular loop 3 of mammalian and nonmammalian gonadotropin-releasing hormone (GnRH) receptors is a critical determinant for differential ligand selectivity for mammalian GnRH and chicken GnRH-II. Wang, C., Yun, O., Maiti, K., Oh, D.Y., Oh, d.a. .Y., Kim, K.K., Chae, C.H., Lee, C.J., Seong, J.Y., Kwon, H.B. Mol. Endocrinol. (2004) [Pubmed]
  20. Homologous upregulation of gonadotropin-releasing hormone receptor mRNA occurs through transcriptional activation rather than modulation of mRNA stability. Cheon, M., Park, D., Park, Y., Kam, K., Park, S.D., Ryu, K. Endocrine (2000) [Pubmed]
  21. Protein kinase C-mediated gonadotropin-releasing hormone receptor sequestration is associated with uncoupling of phosphoinositide hydrolysis. Huckle, W.R., Hawes, B.E., Conn, P.M. J. Biol. Chem. (1989) [Pubmed]
  22. Pituitary gonadotropin-releasing hormone receptor content in rats with polycystic ovaries. Carriere, P.D., Brawer, J.R., Farookhi, R. Biol. Reprod. (1988) [Pubmed]
  23. Functional and morphological characterization of four cell lines derived from GH3 cells stably transfected with gonadotropin-releasing hormone receptor complementary deoxyribonucleic acid. Stanislaus, D., Janovick, J.A., Jennes, L., Kaiser, U.B., Chin, W.W., Conn, P.M. Endocrinology (1994) [Pubmed]
  24. Chimeric GnRH-LH receptors and LH receptors lacking C-terminus palmitoylation sites do not localize to plasma membrane rafts. Lei, Y., Hagen, G.M., Smith, S.M., Barisas, B.G., Roess, D.A. Biochem. Biophys. Res. Commun. (2005) [Pubmed]
  25. Stable transfection of GH3 cells with rat gonadotropin-releasing hormone receptor complementary deoxyribonucleic acid results in expression of a receptor coupled to cyclic adenosine 3',5'-monophosphate-dependent prolactin release via a G-protein. Kuphal, D., Janovick, J.A., Kaiser, U.B., Chin, W.W., Conn, P.M. Endocrinology (1994) [Pubmed]
  26. Activation of the progesterone receptor by the gonadotropin-releasing hormone self-priming signaling pathway. Turgeon, J.L., Waring, D.W. Mol. Endocrinol. (1994) [Pubmed]
  27. Stimulation of luteinizing hormone subunit gene expression by pulsatile intracerebroventricular microinjection of galanin in female rats. Gajewska, A., Zwierzchowski, L., Kochman, K. J. Neuroendocrinol. (2004) [Pubmed]
  28. Effect of GnRH antagonists on phorbol ester-induced LH release from rat pituitary gonadotrophs. Saito, S., Izumi, S., Umeuchi, M., Makino, T., Tsujimoto, G., Nozawa, S. Endocr. J. (1994) [Pubmed]
  29. The rat gonadotropin-releasing hormone receptor internalizes via a beta-arrestin-independent, but dynamin-dependent, pathway: addition of a carboxyl-terminal tail confers beta-arrestin dependency. Heding, A., Vrecl, M., Hanyaloglu, A.C., Sellar, R., Taylor, P.L., Eidne, K.A. Endocrinology (2000) [Pubmed]
  30. Expression of gonadotropin-releasing hormone (GnRH) receptor gene is altered by GnRH agonist desensitization in a manner similar to that of gonadotropin beta-subunit genes in normal and castrated rat pituitary. Lerrant, Y., Kottler, M.L., Bergametti, F., Moumni, M., Blumberg-Tick, J., Counis, R. Endocrinology (1995) [Pubmed]
  31. Hyperprolactinemia inhibits gonadotropin-releasing hormone (GnRH) stimulation of the number of pituitary GnRH receptors. Garcia, A., Herbon, L., Barkan, A., Papavasiliou, S., Marshall, J.C. Endocrinology (1985) [Pubmed]
  32. Expression of gonadotropin-releasing hormone receptor and effect of gonadotropin-releasing hormone analogue on proliferation of cultured gastric smooth muscle cells of rats. Chen, L., He, H.X., Sun, X.D., Zhao, J., Liu, L.H., Huang, W.Q., Zhang, R.Q. World J. Gastroenterol. (2004) [Pubmed]
  33. Dynamic regulation of gonadotropin-releasing hormone receptor mRNA levels in the anterior pituitary gland during the rat estrous cycle. Bauer-Dantoin, A.C., Hollenberg, A.N., Jameson, J.L. Endocrinology (1993) [Pubmed]
  34. Regulation of rat pituitary gonadotropin-releasing hormone receptor mRNA levels in vivo and in vitro. Kaiser, U.B., Jakubowiak, A., Steinberger, A., Chin, W.W. Endocrinology (1993) [Pubmed]
  35. Estrogen regulation of gonadotropin-releasing hormone receptor messenger RNA in female rat pituitary tissue. Quiñones-Jenab, V., Jenab, S., Ogawa, S., Funabashi, T., Weesner, G.D., Pfaff, D.W. Brain Res. Mol. Brain Res. (1996) [Pubmed]
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