KiSS1-derived peptide receptor

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KISS1 receptor
Identifiers
SymbolsKISS1R; AXOR12; GPR54; HOT7T175
External IDsOMIM: 604161 MGI: 2148793 HomoloGene: 11411 IUPHAR: KiSS1 GeneCards: KISS1R Gene
Orthologs
SpeciesHumanMouse
Entrez84634114229
EnsemblENSG00000116014ENSMUSG00000035773
UniProtQ969F8Q91V45
RefSeq (mRNA)NM_032551NM_053244
RefSeq (protein)NP_115940NP_444474
Location (UCSC)Chr 19:
0.87 - 0.87 Mb		Chr 10:
79.32 - 79.33 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

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.

Agonists

Antagonists

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

References

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Further reading

  • 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 Freely accessible. 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

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

Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
de:KiSS1-Rezeptor
  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. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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