Kisspeptin is involved in the regulation of endocrine function and the onset of puberty, with activation of the kisspeptin receptor triggering release of gonadotropin-releasing hormone (GnRH),[7][8] and release of kisspeptin itself being inhibited by oestradiol but enhanced by GnRH.[9] Reductions in kisspeptin levels with age may conversely be one of the reasons behind age-related declines in levels of other endocrine hormones such as luteinizing hormone.[10]
Ligands
No non-peptide ligands for this receptor have yet been discovered, but as of 2009 both selective agonist and antagonist peptides are known.
Kisspeptin-10 analogues modified with amino substitutions[12]
References
↑Lee DK, Nguyen T, O'Neill GP, Cheng R, Liu Y, Howard AD, Coulombe N, Tan CP, Tang-Nguyen AT, George SR, O'Dowd BF (Mar 1999). "Discovery of a receptor related to the galanin receptors". FEBS Letters. 446 (1): 103–7. doi:10.1016/S0014-5793(99)00009-5. PMID10100623.
↑Ohtaki T, Shintani Y, Honda S, Matsumoto H, Hori A, Kanehashi K, Terao Y, Kumano S, Takatsu Y, Masuda Y, Ishibashi Y, Watanabe T, Asada M, Yamada T, Suenaga M, Kitada C, Usuki S, Kurokawa T, Onda H, Nishimura O, Fujino M (May 2001). "Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor". Nature. 411 (6837): 613–7. doi:10.1038/35079135. PMID11385580.
↑Muir AI, Chamberlain L, Elshourbagy NA, Michalovich D, Moore DJ, Calamari A, Szekeres PG, Sarau HM, Chambers JK, Murdock P, Steplewski K, Shabon U, Miller JE, Middleton SE, Darker JG, Larminie CG, Wilson S, Bergsma DJ, Emson P, Faull R, Philpott KL, Harrison DC (Aug 2001). "AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1". The Journal of Biological Chemistry. 276 (31): 28969–75. doi:10.1074/jbc.M102743200. PMID11387329.
↑Kotani M, Detheux M, Vandenbogaerde A, Communi D, Vanderwinden JM, Le Poul E, Brézillon S, Tyldesley R, Suarez-Huerta N, Vandeput F, Blanpain C, Schiffmann SN, Vassart G, Parmentier M (Sep 2001). "The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54". The Journal of Biological Chemistry. 276 (37): 34631–6. doi:10.1074/jbc.M104847200. PMID11457843.
↑Richard N, Corvaisier S, Camacho E, Kottler ML (Jan 2009). "KiSS-1 and GPR54 at the pituitary level: overview and recent insights". Peptides. 30 (1): 123–9. doi:10.1016/j.peptides.2008.09.015. PMID18948153.
↑Liu X, Lee K, Herbison AE (Sep 2008). "Kisspeptin excites gonadotropin-releasing hormone neurons through a phospholipase C/calcium-dependent pathway regulating multiple ion channels". Endocrinology. 149 (9): 4605–14. doi:10.1210/en.2008-0321. PMID18483150.
↑Plant TM, Ramaswamy S, Dipietro MJ (Feb 2006). "Repetitive activation of hypothalamic G protein-coupled receptor 54 with intravenous pulses of kisspeptin in the juvenile monkey (Macaca mulatta) elicits a sustained train of gonadotropin-releasing hormone discharges". Endocrinology. 147 (2): 1007–13. doi:10.1210/en.2005-1261. PMID16282350.
↑Richard N, Galmiche G, Corvaisier S, Caraty A, Kottler ML (Mar 2008). "KiSS-1 and GPR54 genes are co-expressed in rat gonadotrophs and differentially regulated in vivo by oestradiol and gonadotrophin-releasing hormone". Journal of Neuroendocrinology. 20 (3): 381–93. doi:10.1111/j.1365-2826.2008.01653.x. PMID18208554.
Kaiser UB, Kuohung W (Apr 2005). "KiSS-1 and GPR54 as new players in gonadotropin regulation and puberty". Endocrine. 26 (3): 277–84. doi:10.1385/ENDO:26:3:277. PMID16034182.
Seminara SB (2006). "Metastin and its G protein-coupled receptor, GPR54: critical pathway modulating GnRH secretion". Frontiers in Neuroendocrinology. 26 (3–4): 131–8. doi:10.1016/j.yfrne.2005.10.001. PMID16309735.
Tena-Sempere M (2006). "GPR54 and kisspeptin in reproduction". Human Reproduction Update. 12 (5): 631–9. doi:10.1093/humupd/dml023. PMID16731583.
Lee DK, Nguyen T, O'Neill GP, Cheng R, Liu Y, Howard AD, Coulombe N, Tan CP, Tang-Nguyen AT, George SR, O'Dowd BF (Mar 1999). "Discovery of a receptor related to the galanin receptors". FEBS Letters. 446 (1): 103–7. doi:10.1016/S0014-5793(99)00009-5. PMID10100623.
Ohtaki T, Shintani Y, Honda S, Matsumoto H, Hori A, Kanehashi K, Terao Y, Kumano S, Takatsu Y, Masuda Y, Ishibashi Y, Watanabe T, Asada M, Yamada T, Suenaga M, Kitada C, Usuki S, Kurokawa T, Onda H, Nishimura O, Fujino M (May 2001). "Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor". Nature. 411 (6837): 613–7. doi:10.1038/35079135. PMID11385580.
Muir AI, Chamberlain L, Elshourbagy NA, Michalovich D, Moore DJ, Calamari A, Szekeres PG, Sarau HM, Chambers JK, Murdock P, Steplewski K, Shabon U, Miller JE, Middleton SE, Darker JG, Larminie CG, Wilson S, Bergsma DJ, Emson P, Faull R, Philpott KL, Harrison DC (Aug 2001). "AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1". The Journal of Biological Chemistry. 276 (31): 28969–75. doi:10.1074/jbc.M102743200. PMID11387329.
Clements MK, McDonald TP, Wang R, Xie G, O'Dowd BF, George SR, Austin CP, Liu Q (Jun 2001). "FMRFamide-related neuropeptides are agonists of the orphan G-protein-coupled receptor GPR54". Biochemical and Biophysical Research Communications. 284 (5): 1189–93. doi:10.1006/bbrc.2001.5098. PMID11414709.
Kotani M, Detheux M, Vandenbogaerde A, Communi D, Vanderwinden JM, Le Poul E, Brézillon S, Tyldesley R, Suarez-Huerta N, Vandeput F, Blanpain C, Schiffmann SN, Vassart G, Parmentier M (Sep 2001). "The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54". The Journal of Biological Chemistry. 276 (37): 34631–6. doi:10.1074/jbc.M104847200. PMID11457843.
Hori A, Honda S, Asada M, Ohtaki T, Oda K, Watanabe T, Shintani Y, Yamada T, Suenaga M, Kitada C, Onda H, Kurokawa T, Nishimura O, Fujino M (Sep 2001). "Metastin suppresses the motility and growth of CHO cells transfected with its receptor". Biochemical and Biophysical Research Communications. 286 (5): 958–63. doi:10.1006/bbrc.2001.5470. PMID11527393.
Ringel MD, Hardy E, Bernet VJ, Burch HB, Schuppert F, Burman KD, Saji M (May 2002). "Metastin receptor is overexpressed in papillary thyroid cancer and activates MAP kinase in thyroid cancer cells". The Journal of Clinical Endocrinology and Metabolism. 87 (5): 2399. doi:10.1210/jc.87.5.2399. PMID11994395.
Janneau JL, Maldonado-Estrada J, Tachdjian G, Miran I, Motté N, Saulnier P, Sabourin JC, Coté JF, Simon B, Frydman R, Chaouat G, Bellet D (Nov 2002). "Transcriptional expression of genes involved in cell invasion and migration by normal and tumoral trophoblast cells". The Journal of Clinical Endocrinology and Metabolism. 87 (11): 5336–9. doi:10.1210/jc.2002-021093. PMID12414911.
Bo-Abbas Y, Acierno JS, Shagoury JK, Crowley WF, Seminara SB (Jun 2003). "Autosomal recessive idiopathic hypogonadotropic hypogonadism: genetic analysis excludes mutations in the gonadotropin-releasing hormone (GnRH) and GnRH receptor genes". The Journal of Clinical Endocrinology and Metabolism. 88 (6): 2730–7. doi:10.1210/jc.2002-021948. PMID12788881.
Ikeguchi M, Hirooka Y, Kaibara N (Sep 2003). "Quantitative reverse transcriptase polymerase chain reaction analysis for KiSS-1 and orphan G-protein-coupled receptor (hOT7T175) gene expression in hepatocellular carcinoma". Journal of Cancer Research and Clinical Oncology. 129 (9): 531–5. doi:10.1007/s00432-003-0469-z. PMID12898236.
Seminara SB, Messager S, Chatzidaki EE, Thresher RR, Acierno JS, Shagoury JK, Bo-Abbas Y, Kuohung W, Schwinof KM, Hendrick AG, Zahn D, Dixon J, Kaiser UB, Slaugenhaupt SA, Gusella JF, O'Rahilly S, Carlton MB, Crowley WF, Aparicio SA, Colledge WH (Oct 2003). "The GPR54 gene as a regulator of puberty". The New England Journal of Medicine. 349 (17): 1614–27. doi:10.1056/NEJMoa035322. PMID14573733.
Ikeguchi M, Yamaguchi K, Kaibara N (Feb 2004). "Clinical significance of the loss of KiSS-1 and orphan G-protein-coupled receptor (hOT7T175) gene expression in esophageal squamous cell carcinoma". Clinical Cancer Research. 10 (4): 1379–83. doi:10.1158/1078-0432.CCR-1519-02. PMID14977840.
Bilban M, Ghaffari-Tabrizi N, Hintermann E, Bauer S, Molzer S, Zoratti C, Malli R, Sharabi A, Hiden U, Graier W, Knöfler M, Andreae F, Wagner O, Quaranta V, Desoye G (Mar 2004). "Kisspeptin-10, a KiSS-1/metastin-derived decapeptide, is a physiological invasion inhibitor of primary human trophoblasts". Journal of Cell Science. 117 (Pt 8): 1319–28. doi:10.1242/jcs.00971. PMID15020672.
External links
"KiSS1-Derived Peptide Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.