Document Detail

International Union of Basic and Clinical Pharmacology. LXXVII. Kisspeptin receptor nomenclature, distribution, and function.
MedLine Citation:
PMID:  21079036     Owner:  NLM     Status:  MEDLINE    
Kisspeptins are members of the Arg-Phe amide family of peptides, which have been identified as endogenous ligands for a G-protein-coupled receptor encoded by a gene originally called GPR54 (also known as AXOR12 or hOT7T175). After this pairing, the gene has been renamed KISS1R. The International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification recommends that the official name for the receptor is the kisspeptin receptor to follow the convention of naming the receptor protein after the endogenous ligand. The endogenous ligand was initially called metastin, after its role as a metastasis suppressor, and is now referred to as kisspeptin-54 (KP-54), a C-terminally amidated 54-amino acid peptide cleaved from the 145-amino acid gene product. Shorter C-terminal cleavage fragments [KP-14, KP-13 and KP-10 (the smallest active fragment)] are also biologically active. Both receptor and peptide are widely expressed in human, rat, and mouse; the receptor sequence shares more than 80% homology in these species. Activation of the kisspeptin receptor by kisspeptin is via coupling to G(q/11) and the phospholipase C pathway, causing Ca(2+) mobilization. Mutations in the KISS1R gene result in hypogonadotropic hypogonadotropism, and targeted disruption of Kiss1r in mice reproduces this phenotype, which led to the discovery of the remarkable ability of the kisspeptin receptor to act as a molecular switch for puberty. In addition to regulating the reproductive axis, the kisspeptin receptor is also implicated in cancer, placentation, diabetes, and the cardiovascular system.
Helen R Kirby; Janet J Maguire; William H Colledge; Anthony P Davenport
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review    
Journal Detail:
Title:  Pharmacological reviews     Volume:  62     ISSN:  1521-0081     ISO Abbreviation:  Pharmacol. Rev.     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2010-11-16     Completed Date:  2011-03-21     Revised Date:  2013-07-03    
Medline Journal Info:
Nlm Unique ID:  0421737     Medline TA:  Pharmacol Rev     Country:  United States    
Other Details:
Languages:  eng     Pagination:  565-78     Citation Subset:  IM    
Clinical Pharmacology Unit, University of Cambridge, Addenbrookes Hospital, Cambridge, United Kingdom.
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MeSH Terms
Organ Specificity
Receptors, G-Protein-Coupled* / chemistry,  classification,  physiology
Structure-Activity Relationship
Terminology as Topic*
Grant Support
PG/09/050/27734//Medical Research Council; PS/02/001//Medical Research Council; //British Heart Foundation
Reg. No./Substance:
0/KISS1R protein, human; 0/Kiss1r protein, mouse; 0/Kiss1r protein, rat; 0/Receptors, G-Protein-Coupled

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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