KiSS1-derived peptide receptor

KISS1R
Identifiers
Aliases	KISS1R, AXOR12, CPPB1, GPR54, HH8, HOT7T175, KISS-1R, KiSS1-derived peptide receptor, KISS1 receptor
External IDs	OMIM: 604161; MGI: 2148793; HomoloGene: 11411; GeneCards: KISS1R; OMA:KISS1R - orthologs
Gene location (Human)
Chr.	Chromosome 19 (human)
End	921,005 bp
Gene location (Mouse)
Chr.	Chromosome 10 (mouse)
End	79,758,107 bp
RNA expression pattern
	Top expressed in
	pons; ; endothelial cell; ; hypothalamus; ; Brodmann area 23; ; pancreatic ductal cell; ; cartilage tissue; ; superior vestibular nucleus; ; nucleus accumbens; ; blood; ; cingulate gyrus;
	Top expressed in
	granulocyte; ; substantia nigra; ; embryo; ; embryo; ; primary visual cortex; ; neuron; ; dentate gyrus of hippocampal formation granule cell; ; superior frontal gyrus; ; right kidney; ; cerebellar cortex;
	More reference expression data
	n/a
Gene ontology
Molecular function	G protein-coupled peptide receptor activity; G protein-coupled receptor activity; neuropeptide receptor activity; signal transducer activity; protein binding;
Cellular component	integral component of membrane; intracellular membrane-bounded organelle; membrane; plasma membrane; integral component of plasma membrane; cell surface; cilium;
Biological process	phospholipase C-activating G protein-coupled receptor signaling pathway; signal transduction; neuropeptide signaling pathway; G protein-coupled receptor signaling pathway;
	Sources:Amigo / QuickGO
Orthologs
	84634
	114229
	ENSG00000116014
	ENSMUSG00000035773
	Q969F8
	Q91V45
	NM_032551
	NM_053244; NM_001359010
	NP_115940
	NP_444474; NP_001345939
	Wikidata
View/Edit Human	View/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]

Kisspeptins are neuropeptides synthesized in the hypothalamus and encoded by the KISS1 gene. The KISS1 gene encodes the G protein-coupled receptor 54 (known as KISS1R or GPR54) and plays a crucial role in regulating reproduction, pubertal maturation, and metabolic function.^[11]^[12]^[13] KISS1 neurons located in the arcuate nucleus (ARC) of the mediobasal hypothalamus (MBH) project to GnRH neurons in the median eminence, which expresses KISS1R, to stimulate LH secretions in a pulsatile manner from the anterior pituitary to initiate ovulation/ pubertal maturation.^[14]^[15]^[16] The KISS1 and KISS1R/GPR54 genes have been detected in the brain, pituitary, placenta, pancreas, liver, and small intestine.^[14]

^ ^a ^b ^c GRCh38: Ensembl release 89: ENSG00000116014 – Ensembl, May 2017
^ ^a ^b ^c GRCm38: Ensembl release 89: ENSMUSG00000035773 – Ensembl, May 2017
^ "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, et al. (March 1999). "Discovery of a receptor related to the galanin receptors". FEBS Letters. 446 (1): 103–107. doi:10.1016/S0014-5793(99)00009-5. PMID 10100623. S2CID 38910830.
^ Ohtaki T, Shintani Y, Honda S, Matsumoto H, Hori A, Kanehashi K, et al. (May 2001). "Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor". Nature. 411 (6837): 613–617. Bibcode:2001Natur.411..613O. doi:10.1038/35079135. PMID 11385580. S2CID 205017670.
^ Muir AI, Chamberlain L, Elshourbagy NA, Michalovich D, Moore DJ, Calamari A, et al. (August 2001). "AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1". The Journal of Biological Chemistry. 276 (31): 28969–28975. doi:10.1074/jbc.M102743200. PMID 11387329.
^ Kotani M, Detheux M, Vandenbogaerde A, Communi D, Vanderwinden JM, Le Poul E, et al. (September 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): 34631–34636. doi:10.1074/jbc.M104847200. PMID 11457843.
^ 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): 123–129. doi:10.1016/j.peptides.2008.09.015. PMID 18948153. S2CID 22875820.
^ 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): 4605–4614. doi:10.1210/en.2008-0321. PMC 6116891. PMID 18483150.
^ Roseweir AK, Millar RP (2008-11-05). "The role of kisspeptin in the control of gonadotrophin secretion". Human Reproduction Update. 15 (2): 203–212. doi:10.1093/humupd/dmn058. PMID 19109311.
^ Tolson KP, Garcia C, Yen S, Simonds S, Stefanidis A, Lawrence A, et al. (July 2014). "Impaired kisspeptin signaling decreases metabolism and promotes glucose intolerance and obesity". The Journal of Clinical Investigation. 124 (7): 3075–3079. doi:10.1172/jci71075. PMC 4071390. PMID 24937427.
^ Song WJ, Mondal P, Wolfe A, Alonso LC, Stamateris R, Ong BW, et al. (April 2014). "Glucagon regulates hepatic kisspeptin to impair insulin secretion". Cell Metabolism. 19 (4): 667–681. doi:10.1016/j.cmet.2014.03.005. PMC 4058888. PMID 24703698.
^ ^a ^b Yeo SH, Colledge WH (2018-04-26). "The Role of Kiss1 Neurons As Integrators of Endocrine, Metabolic, and Environmental Factors in the Hypothalamic-Pituitary-Gonadal Axis". Frontiers in Endocrinology. 9: 188. doi:10.3389/fendo.2018.00188. PMC 5932150. PMID 29755406.
^ Navarro VM, Castellano JM, Fernández-Fernández R, Barreiro ML, Roa J, Sanchez-Criado JE, et al. (October 2004). "Developmental and hormonally regulated messenger ribonucleic acid expression of KiSS-1 and its putative receptor, GPR54, in rat hypothalamus and potent luteinizing hormone-releasing activity of KiSS-1 peptide". Endocrinology. 145 (10): 4565–4574. doi:10.1210/en.2004-0413. PMID 15242985. S2CID 14817781.
^ De Bond JP, Tolson KP, Nasamran C, Kauffman AS, Smith JT (October 2016). "Unaltered Hypothalamic Metabolic Gene Expression in Kiss1r Knockout Mice Despite Obesity and Reduced Energy Expenditure". Journal of Neuroendocrinology. 28 (10). doi:10.1111/jne.12430. PMC 5083214. PMID 27601011. S2CID 3542864.

[refGRCh38Ensembl-1] GRCh38: Ensembl release 89: ENSG00000116014 – Ensembl, May 2017

[refGRCm38Ensembl-2] 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.

[pmid10100623-5] Lee DK, Nguyen T, O'Neill GP, Cheng R, Liu Y, Howard AD, et al. (March 1999). "Discovery of a receptor related to the galanin receptors". FEBS Letters. 446 (1): 103–107. doi:10.1016/S0014-5793(99)00009-5. PMID 10100623. S2CID 38910830.

[pmid11385580-6] Ohtaki T, Shintani Y, Honda S, Matsumoto H, Hori A, Kanehashi K, et al. (May 2001). "Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor". Nature. 411 (6837): 613–617. Bibcode:2001Natur.411..613O. doi:10.1038/35079135. PMID 11385580. S2CID 205017670.

[pmid11387329-7] Muir AI, Chamberlain L, Elshourbagy NA, Michalovich D, Moore DJ, Calamari A, et al. (August 2001). "AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1". The Journal of Biological Chemistry. 276 (31): 28969–28975. doi:10.1074/jbc.M102743200. PMID 11387329.

[pmid11457843-8] Kotani M, Detheux M, Vandenbogaerde A, Communi D, Vanderwinden JM, Le Poul E, et al. (September 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): 34631–34636. doi:10.1074/jbc.M104847200. PMID 11457843.

[pmid18948153-9] 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): 123–129. doi:10.1016/j.peptides.2008.09.015. PMID 18948153. S2CID 22875820.

[pmid18483150-10] 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): 4605–4614. doi:10.1210/en.2008-0321. PMC 6116891. PMID 18483150.

[11] Roseweir AK, Millar RP (2008-11-05). "The role of kisspeptin in the control of gonadotrophin secretion". Human Reproduction Update. 15 (2): 203–212. doi:10.1093/humupd/dmn058. PMID 19109311.

[12] Tolson KP, Garcia C, Yen S, Simonds S, Stefanidis A, Lawrence A, et al. (July 2014). "Impaired kisspeptin signaling decreases metabolism and promotes glucose intolerance and obesity". The Journal of Clinical Investigation. 124 (7): 3075–3079. doi:10.1172/jci71075. PMC 4071390. PMID 24937427.

[13] Song WJ, Mondal P, Wolfe A, Alonso LC, Stamateris R, Ong BW, et al. (April 2014). "Glucagon regulates hepatic kisspeptin to impair insulin secretion". Cell Metabolism. 19 (4): 667–681. doi:10.1016/j.cmet.2014.03.005. PMC 4058888. PMID 24703698.

[:0-14] Yeo SH, Colledge WH (2018-04-26). "The Role of Kiss1 Neurons As Integrators of Endocrine, Metabolic, and Environmental Factors in the Hypothalamic-Pituitary-Gonadal Axis". Frontiers in Endocrinology. 9: 188. doi:10.3389/fendo.2018.00188. PMC 5932150. PMID 29755406.

[15] Navarro VM, Castellano JM, Fernández-Fernández R, Barreiro ML, Roa J, Sanchez-Criado JE, et al. (October 2004). "Developmental and hormonally regulated messenger ribonucleic acid expression of KiSS-1 and its putative receptor, GPR54, in rat hypothalamus and potent luteinizing hormone-releasing activity of KiSS-1 peptide". Endocrinology. 145 (10): 4565–4574. doi:10.1210/en.2004-0413. PMID 15242985. S2CID 14817781.

[16] De Bond JP, Tolson KP, Nasamran C, Kauffman AS, Smith JT (October 2016). "Unaltered Hypothalamic Metabolic Gene Expression in Kiss1r Knockout Mice Despite Obesity and Reduced Energy Expenditure". Journal of Neuroendocrinology. 28 (10). doi:10.1111/jne.12430. PMC 5083214. PMID 27601011. S2CID 3542864.

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