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),[11][12] and release of kisspeptin itself being inhibited by oestradiol but enhanced by GnRH.[13] 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.[14]
Ligands
No non-peptide ligands for this receptor have yet been discovered, but as of 2009 both selective agonist and antagonist peptides are known.
^"Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^"Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^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.
^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.
^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.
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.
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.
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.
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.