KiSS1-derived peptide receptor

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KISS1 receptor
Identifiers
Symbols KISS1R ; AXOR12; CPPB1; GPR54; HH8; HOT7T175; KISS-1R
External IDs OMIM604161 MGI2148793 HomoloGene11411 IUPHAR: kisspeptin receptor ChEMBL: 5413 GeneCards: KISS1R Gene
Orthologs
Species Human Mouse
Entrez 84634 114229
Ensembl ENSG00000116014 ENSMUSG00000035773
UniProt Q969F8 Q91V45
RefSeq (mRNA) NM_032551 NM_053244
RefSeq (protein) NP_115940 NP_444474
Location (UCSC) Chr 19:
0.92 – 0.92 Mb
Chr 10:
79.92 – 79.92 Mb
PubMed search [1] [2]

The KiSS1-derived peptide receptor (also known as GPR54 or the Kisspeptin receptor) is a G protein-coupled receptor[1] which binds the peptide hormone kisspeptin (metastin).[2][3][4] Kisspeptin is encoded by the metastasis suppressor gene KISS1, which is expressed in a variety of endocrine and gonadal tissues.[5] Activation of the kisspeptin receptor is linked to the phospholipase C and inositol trisphosphate second messenger cascades inside the cell.[6]

Function[edit]

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[edit]

No non-peptide ligands for this receptor have yet been discovered, but as of 2009 both selective agonist and antagonist peptides are known.

Agonists[edit]

Antagonists[edit]

  • Kisspeptin-10 analogues modified with amino substitutions[12]

References[edit]

  1. ^ 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 (1999). "Discovery of a receptor related to the galanin receptors". FEBS Lett. 446 (1): 103–7. doi:10.1016/S0014-5793(99)00009-5. PMID 10100623. 
  2. ^ 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 (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. 
  3. ^ 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 (2001). "AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1". J. Biol. Chem. 276 (31): 28969–75. doi:10.1074/jbc.M102743200. PMID 11387329. 
  4. ^ 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 (2001). "The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54". J. Biol. Chem. 276 (37): 34631–6. doi:10.1074/jbc.M104847200. PMID 11457843. 
  5. ^ Richard N, Corvaisier S, Camacho E, Kottler ML (January 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. 
  6. ^ Liu X, Lee K, Herbison AE (September 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. PMID 18483150. 
  7. ^ Shahab M, Mastronardi C, Seminara SB, Crowley WF, Ojeda SR, Plant TM (February 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. 
  8. ^ Plant TM, Ramaswamy S, Dipietro MJ (February 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. 
  9. ^ Richard N, Galmiche G, Corvaisier S, Caraty A, Kottler ML (March 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. 
  10. ^ Neal-Perry G, Lebesgue D, Lederman M, Shu J, Zeevalk GD, Etgen AM (May 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. 
  11. ^ Mikkelsen JD, Bentsen AH, Ansel L, Simonneaux V, Juul A (January 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. 
  12. ^ 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 (March 2009). "Discovery of potent kisspeptin antagonists delineate physiological mechanisms of gonadotropin regulation". Journal of Neuroscience 29 (12): 3920–9. doi:10.1523/JNEUROSCI.5740-08.2009. PMC 3035813. PMID 19321788. 

Further reading[edit]

  • Colledge WH (2005). "GPR54 and puberty.". Trends Endocrinol. Metab. 15 (9): 448–53. doi:10.1016/j.tem.2004.09.008. PMID 15519892. 
  • Kaiser UB, Kuohung W (2006). "KiSS-1 and GPR54 as new players in gonadotropin regulation and puberty.". Endocrine 26 (3): 277–84. doi:10.1385/ENDO:26:3:277. PMID 16034182. 
  • 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. PMID 16309735. 
  • Tena-Sempere M (2006). "GPR54 and kisspeptin in reproduction.". Hum. Reprod. Update 12 (5): 631–9. doi:10.1093/humupd/dml023. PMID 16731583. 
  • Cerrato F, Seminara SB (2007). "Human genetics of GPR54.". Reviews in endocrine & metabolic disorders 8 (1): 47–55. doi:10.1007/s11154-007-9027-3. PMID 17334928. 
  • Lee DK, Nguyen T, O'Neill GP, et al. (1999). "Discovery of a receptor related to the galanin receptors.". FEBS Lett. 446 (1): 103–7. doi:10.1016/S0014-5793(99)00009-5. PMID 10100623. 
  • Ohtaki T, Shintani Y, Honda S, et al. (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. 
  • Muir AI, Chamberlain L, Elshourbagy NA, et al. (2001). "AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1.". J. Biol. Chem. 276 (31): 28969–75. doi:10.1074/jbc.M102743200. PMID 11387329. 
  • Clements MK, McDonald TP, Wang R, et al. (2001). "FMRFamide-related neuropeptides are agonists of the orphan G-protein-coupled receptor GPR54.". Biochem. Biophys. Res. Commun. 284 (5): 1189–93. doi:10.1006/bbrc.2001.5098. PMID 11414709. 
  • Kotani M, Detheux M, Vandenbogaerde A, et al. (2001). "The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.". J. Biol. Chem. 276 (37): 34631–6. doi:10.1074/jbc.M104847200. PMID 11457843. 
  • Hori A, Honda S, Asada M, et al. (2001). "Metastin suppresses the motility and growth of CHO cells transfected with its receptor.". Biochem. Biophys. Res. Commun. 286 (5): 958–63. doi:10.1006/bbrc.2001.5470. PMID 11527393. 
  • Ringel MD, Hardy E, Bernet VJ, et al. (2002). "Metastin receptor is overexpressed in papillary thyroid cancer and activates MAP kinase in thyroid cancer cells.". J. Clin. Endocrinol. Metab. 87 (5): 2399. doi:10.1210/jc.87.5.2399. PMID 11994395. 
  • Janneau JL, Maldonado-Estrada J, Tachdjian G, et al. (2002). "Transcriptional expression of genes involved in cell invasion and migration by normal and tumoral trophoblast cells.". J. Clin. Endocrinol. Metab. 87 (11): 5336–9. doi:10.1210/jc.2002-021093. PMID 12414911. 
  • Bo-Abbas Y, Acierno JS, Shagoury JK, et al. (2003). "Autosomal recessive idiopathic hypogonadotropic hypogonadism: genetic analysis excludes mutations in the gonadotropin-releasing hormone (GnRH) and GnRH receptor genes.". J. Clin. Endocrinol. Metab. 88 (6): 2730–7. doi:10.1210/jc.2002-021948. PMID 12788881. 
  • Ikeguchi M, Hirooka Y, Kaibara N (2003). "Quantitative reverse transcriptase polymerase chain reaction analysis for KiSS-1 and orphan G-protein-coupled receptor (hOT7T175) gene expression in hepatocellular carcinoma.". J. Cancer Res. Clin. Oncol. 129 (9): 531–5. doi:10.1007/s00432-003-0469-z. PMID 12898236. 
  • de Roux N, Genin E, Carel JC, et al. (2003). "Hypogonadotropic hypogonadism due to loss of function of the KiSS1-derived peptide receptor GPR54.". Proc. Natl. Acad. Sci. U.S.A. 100 (19): 10972–6. doi:10.1073/pnas.1834399100. PMC 196911. PMID 12944565. 
  • Seminara SB, Messager S, Chatzidaki EE, et al. (2003). "The GPR54 gene as a regulator of puberty.". N. Engl. J. Med. 349 (17): 1614–27. doi:10.1056/NEJMoa035322. PMID 14573733. 
  • Ikeguchi M, Yamaguchi K, Kaibara N (2004). "Clinical significance of the loss of KiSS-1 and orphan G-protein-coupled receptor (hOT7T175) gene expression in esophageal squamous cell carcinoma.". Clin. Cancer Res. 10 (4): 1379–83. doi:10.1158/1078-0432.CCR-1519-02. PMID 14977840. 
  • Bilban M, Ghaffari-Tabrizi N, Hintermann E, et al. (2004). "Kisspeptin-10, a KiSS-1/metastin-derived decapeptide, is a physiological invasion inhibitor of primary human trophoblasts.". J. Cell. Sci. 117 (Pt 8): 1319–28. doi:10.1242/jcs.00971. PMID 15020672. 
  • Grimwood J, Gordon LA, Olsen A, et al. (2004). "The DNA sequence and biology of human chromosome 19.". Nature 428 (6982): 529–35. doi:10.1038/nature02399. PMID 15057824. 

External links[edit]

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