KiSS1-derived peptide receptor

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AliasesKISS1R, AXOR12, CPPB1, GPR54, HH8, HOT7T175, KISS-1R, KiSS1-derived peptide receptor, KISS1 receptor
External IDsOMIM: 604161 MGI: 2148793 HomoloGene: 11411 GeneCards: KISS1R
Gene location (Human)
Chromosome 19 (human)
Chr.Chromosome 19 (human)[1]
Chromosome 19 (human)
Genomic location for KISS1R
Genomic location for KISS1R
Band19p13.3Start917,287 bp[1]
End921,005 bp[1]
RefSeq (mRNA)



RefSeq (protein)



Location (UCSC)Chr 19: 0.92 – 0.92 MbChr 10: 79.92 – 79.92 Mb
PubMed search[3][4]
View/Edit HumanView/Edit Mouse

The KiSS1-derived peptide receptor (also known as GPR54 or the Kisspeptin receptor) is a G protein-coupled receptor[5] which binds the peptide hormone kisspeptin (metastin).[6][7][8] Kisspeptin is encoded by the metastasis suppressor gene KISS1, which is expressed in a variety of endocrine and gonadal tissues.[9] Activation of the kisspeptin receptor is linked to the phospholipase C and inositol trisphosphate second messenger cascades inside the cell.[10]


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]


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[16]


  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000116014 - Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000035773 - Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ 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. PMID 10100623. S2CID 38910830.
  6. ^ 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. PMID 11385580. S2CID 205017670.
  7. ^ 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. PMID 11387329.
  8. ^ 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. PMID 11457843.
  9. ^ 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. PMID 18948153. S2CID 22875820.
  10. ^ 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. PMC 6116891. PMID 18483150.
  11. ^ Shahab M, Mastronardi C, Seminara SB, Crowley WF, Ojeda SR, Plant TM (Feb 2005). "Increased hypothalamic GPR54 signaling: a potential mechanism for initiation of puberty in primates". Proceedings of the National Academy of Sciences of the United States of America. 102 (6): 2129–34. doi:10.1073/pnas.0409822102. PMC 548549. PMID 15684075.
  12. ^ 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. PMID 16282350.
  13. ^ 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. PMID 18208554. S2CID 205345039.
  14. ^ Neal-Perry G, Lebesgue D, Lederman M, Shu J, Zeevalk GD, Etgen AM (Aug 2009). "The excitatory peptide kisspeptin restores the luteinizing hormone surge and modulates amino acid neurotransmission in the medial preoptic area of middle-aged rats". Endocrinology. 150 (8): 3699–708. doi:10.1210/en.2008-1667. PMC 2717872. PMID 19423763.
  15. ^ Mikkelsen JD, Bentsen AH, Ansel L, Simonneaux V, Juul A (Jan 2009). "Comparison of the effects of peripherally administered kisspeptins". Regulatory Peptides. 152 (1–3): 95–100. doi:10.1016/j.regpep.2008.10.001. PMID 18940206. S2CID 6587724.
  16. ^ Roseweir AK, Kauffman AS, Smith JT, Guerriero KA, Morgan K, Pielecka-Fortuna J, Pineda R, Gottsch ML, Tena-Sempere M, Moenter SM, Terasawa E, Clarke IJ, Steiner RA, Millar RP (Mar 2009). "Discovery of potent kisspeptin antagonists delineate physiological mechanisms of gonadotropin regulation". The Journal of Neuroscience. 29 (12): 3920–9. doi:10.1523/JNEUROSCI.5740-08.2009. PMC 3035813. PMID 19321788.

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This article incorporates text from the United States National Library of Medicine, which is in the public domain.