The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)



Gene Review

KISS1R  -  KISS1 receptor

Homo sapiens

Synonyms: AXOR12, CPPB1, G-protein coupled receptor 54, G-protein coupled receptor OT7T175, GPR54, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of KISS1R


High impact information on KISS1R


Chemical compound and disease context of KISS1R


Biological context of KISS1R


Anatomical context of KISS1R


Associations of KISS1R with chemical compounds

  • One subject with HH, of mixed Turkish-Cypriot and Afro-Caribbean ancestry, was found to be a compound heterozygote for two previously undescribed missense mutations in GPR54: cysteine 223 to arginine (C223R) in the fifth transmembrane helix and arginine 297 to leucine (R297L) in the third extracellular loop [3].
  • Continuous human metastin 45-54 infusion desensitizes G protein-coupled receptor 54-induced gonadotropin-releasing hormone release monitored indirectly in the juvenile male Rhesus monkey (Macaca mulatta): a finding with therapeutic implications [14].
  • Production of metastin and, to a lesser extent, GPR54 are negatively regulated by testosterone and oestrogen, and injecting GPR54 ligands can increase hormone secretion in rodents [15].
  • To address this issue, we cloned GPR54 from the brain of a cichlid fish (tilapia Oreochromis niloticus) and determined its expression in immature and mature males using our newly developed technique: laser-captured microdissection of single digoxigenin-labeled GnRH neurons coupled with real-time quantitative PCR [16].
  • To refine insight into the critical pharmacophore for the activation of GPR54, we have conducted alanine and d-amino acid scanning on a biologically active metastin fragment (45-54) [17].
  • Mutating the corresponding leucine of the alpha(1A)-AR recapitulates the effects observed with L148S GPR54, suggesting the critical importance of this hydrophobic IL2 residue for Class A GPCR functional coupling [18].

Regulatory relationships of KISS1R


Other interactions of KISS1R


Analytical, diagnostic and therapeutic context of KISS1R


  1. Role of sequence variations of the GnRH receptor and G protein-coupled receptor 54 gene in male idiopathic hypogonadotropic hypogonadism. Lanfranco, F., Gromoll, J., von Eckardstein, S., Herding, E.M., Nieschlag, E., Simoni, M. Eur. J. Endocrinol. (2005) [Pubmed]
  2. KISS1 metastasis suppression and emergent pathways. Harms, J.F., Welch, D.R., Miele, M.E. Clin. Exp. Metastasis (2003) [Pubmed]
  3. Two novel missense mutations in g protein-coupled receptor 54 in a patient with hypogonadotropic hypogonadism. Semple, R.K., Achermann, J.C., Ellery, J., Farooqi, I.S., Karet, F.E., Stanhope, R.G., O'rahilly, S., Aparicio, S.A. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  4. Metastin receptor is overexpressed in papillary thyroid cancer and activates MAP kinase in thyroid cancer cells. Ringel, M.D., Hardy, E., Bernet, V.J., Burch, H.B., Schuppert, F., Burman, K.D., Saji, M. J. Clin. Endocrinol. Metab. (2002) [Pubmed]
  5. Metastin and its variant forms suppress migration of pancreatic cancer cells. Masui, T., Doi, R., Mori, T., Toyoda, E., Koizumi, M., Kami, K., Ito, D., Peiper, S.C., Broach, J.R., Oishi, S., Niida, A., Fujii, N., Imamura, M. Biochem. Biophys. Res. Commun. (2004) [Pubmed]
  6. Pulsatile administration of low-dose gonadotropin-releasing hormone. Ovulation and pregnancy in women with hypothalamic amenorrhea. Miller, D.S., Reid, R.R., Cetel, N.S., Rebar, R.W., Yen, S.S. JAMA (1983) [Pubmed]
  7. Increased hypothalamic GPR54 signaling: a potential mechanism for initiation of puberty in primates. Shahab, M., Mastronardi, C., Seminara, S.B., Crowley, W.F., Ojeda, S.R., Plant, T.M. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  8. AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1. Muir, A.I., Chamberlain, L., Elshourbagy, N.A., Michalovich, D., Moore, D.J., Calamari, A., Szekeres, P.G., Sarau, H.M., Chambers, J.K., Murdock, P., Steplewski, K., Shabon, U., Miller, J.E., Middleton, S.E., Darker, J.G., Larminie, C.G., Wilson, S., Bergsma, D.J., Emson, P., Faull, R., Philpott, K.L., Harrison, D.C. J. Biol. Chem. (2001) [Pubmed]
  9. The GPR54 gene as a regulator of puberty. Seminara, S.B., Messager, S., Chatzidaki, E.E., Thresher, R.R., Acierno, J.S., Shagoury, J.K., Bo-Abbas, Y., Kuohung, W., Schwinof, K.M., Hendrick, A.G., Zahn, D., Dixon, J., Kaiser, U.B., Slaugenhaupt, S.A., Gusella, J.F., O'Rahilly, S., Carlton, M.B., Crowley, W.F., Aparicio, S.A., Colledge, W.H. N. Engl. J. Med. (2003) [Pubmed]
  10. Hormonal changes in puberty III: Correlation of plasma dehydroepiandrosterone, testosterone, FSH, and LH with stages of puberty and bone age in normal boys and girls and in patients with Addison's disease or hypogonadism or with premature or late adrenarche. Sizonenko, P.C., Paunier, L. J. Clin. Endocrinol. Metab. (1975) [Pubmed]
  11. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. Kotani, M., Detheux, M., Vandenbogaerde, A., Communi, D., Vanderwinden, J.M., Le Poul, E., Brézillon, S., Tyldesley, R., Suarez-Huerta, N., Vandeput, F., Blanpain, C., Schiffmann, S.N., Vassart, G., Parmentier, M. J. Biol. Chem. (2001) [Pubmed]
  12. Cleavage of metastasis suppressor gene product KiSS-1 protein/metastin by matrix metalloproteinases. Takino, T., Koshikawa, N., Miyamori, H., Tanaka, M., Sasaki, T., Okada, Y., Seiki, M., Sato, H. Oncogene (2003) [Pubmed]
  13. Transcriptional expression of genes involved in cell invasion and migration by normal and tumoral trophoblast cells. Janneau, J.L., Maldonado-Estrada, J., Tachdjian, G., Miran, I., Motté, N., Saulnier, P., Sabourin, J.C., Coté, J.F., Simon, B., Frydman, R., Chaouat, G., Bellet, D. J. Clin. Endocrinol. Metab. (2002) [Pubmed]
  14. Continuous human metastin 45-54 infusion desensitizes G protein-coupled receptor 54-induced gonadotropin-releasing hormone release monitored indirectly in the juvenile male Rhesus monkey (Macaca mulatta): a finding with therapeutic implications. Seminara, S.B., Dipietro, M.J., Ramaswamy, S., Crowley, W.F., Plant, T.M. Endocrinology (2006) [Pubmed]
  15. GPR54 and puberty. Colledge, W.H. Trends Endocrinol. Metab. (2004) [Pubmed]
  16. Laser-captured single digoxigenin-labeled neurons of gonadotropin-releasing hormone types reveal a novel G protein-coupled receptor (Gpr54) during maturation in cichlid fish. Parhar, I.S., Ogawa, S., Sakuma, Y. Endocrinology (2004) [Pubmed]
  17. Design and synthesis of downsized metastin (45-54) analogs with maintenance of high GPR54 agonistic activity. Niida, A., Wang, Z., Tomita, K., Oishi, S., Tamamura, H., Otaka, A., Navenot, J.M., Broach, J.R., Peiper, S.C., Fujii, N. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
  18. Disease-causing mutation in GPR54 reveals the importance of the second intracellular loop for class A G-protein-coupled receptor function. Wacker, J.L., Feller, D.B., Tang, X.B., Defino, M.C., Namkung, Y., Lyssand, J.S., Mhyre, A.J., Tan, X., Jensen, J.B., Hague, C. J. Biol. Chem. (2008) [Pubmed]
  19. New insights in the genetics of isolated hypogonadotropic hypogonadism. Iovane, A., Aumas, C., de Roux, N. Eur. J. Endocrinol. (2004) [Pubmed]
  20. Quantitative reverse transcriptase polymerase chain reaction analysis for KiSS-1 and orphan G-protein-coupled receptor (hOT7T175) gene expression in hepatocellular carcinoma. Ikeguchi, M., Hirooka, Y., Kaibara, N. J. Cancer Res. Clin. Oncol. (2003) [Pubmed]
  21. KiSS-1/G protein-coupled receptor 54 metastasis suppressor pathway increases myocyte-enriched calcineurin interacting protein 1 expression and chronically inhibits calcineurin activity. Stathatos, N., Bourdeau, I., Espinosa, A.V., Saji, M., Vasko, V.V., Burman, K.D., Stratakis, C.A., Ringel, M.D. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  22. Discovery of a receptor related to the galanin receptors. Lee, D.K., Nguyen, T., O'Neill, G.P., Cheng, R., Liu, Y., Howard, A.D., Coulombe, N., Tan, C.P., Tang-Nguyen, A.T., George, S.R., O'Dowd, B.F. FEBS Lett. (1999) [Pubmed]
  23. Activation of GPR54 promotes cell cycle arrest and apoptosis of human tumor cells through a specific transcriptional program not shared by other Gq-coupled receptors. Becker, J.A., Mirjolet, J.F., Bernard, J., Burgeon, E., Simons, M.J., Vassart, G., Parmentier, M., Libert, F. Biochem. Biophys. Res. Commun. (2005) [Pubmed]
  24. Coding sequence analysis of GNRHR and GPR54 in patients with congenital and adult-onset forms of hypogonadotropic hypogonadism. Cerrato, F., Shagoury, J., Kralickova, M., Dwyer, A., Falardeau, J., Ozata, M., Van Vliet, G., Bouloux, P., Hall, J.E., Hayes, F.J., Pitteloud, N., Martin, K.A., Welt, C., Seminara, S.B. Eur. J. Endocrinol. (2006) [Pubmed]
WikiGenes - Universities