RGD Reference Report - The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. - Rat Genome Database

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The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.

Authors: Kotani, M  Detheux, M  Vandenbogaerde, A  Communi, D  Vanderwinden, JM  Le Poul, E  Brezillon, S  Tyldesley, R  Suarez-Huerta, N  Vandeput, F  Blanpain, C  Schiffmann, SN  Vassart, G  Parmentier, M 
Citation: Kotani M, etal., J Biol Chem 2001 Sep 14;276(37):34631-6. Epub 2001 Jul 16.
RGD ID: 1357971
Pubmed: PMID:11457843   (View Abstract at PubMed)
DOI: DOI:10.1074/jbc.M104847200   (Journal Full-text)

Natural peptides displaying agonist activity on the orphan G protein-coupled receptor GPR54 were isolated from human placenta. These 54-, 14,- and 13-amino acid peptides, with a common RF-amide C terminus, derive from the product of KiSS-1, a metastasis suppressor gene for melanoma cells, and were therefore designated kisspeptins. They bound with low nanomolar affinities to rat and human GPR54 expressed in Chinese hamster ovary K1 cells and stimulated PIP(2) hydrolysis, Ca(2+) mobilization, arachidonic acid release, ERK1/2 and p38 MAP kinase phosphorylation, and stress fiber formation but inhibited cell proliferation. Human GPR54 was highly expressed in placenta, pituitary, pancreas, and spinal cord, suggesting a role in the regulation of endocrine function. Stimulation of oxytocin secretion after kisspeptin administration to rats confirmed this hypothesis.

Gene Ontology Annotations    Click to see Annotation Detail View

Biological Process
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
arachidonic acid secretion  IDA 1357971 RGD 
negative regulation of cell population proliferation  IDA 1357971kisspeptin-10 peptide is 100% identical in rat and mouse and humanRGD 
negative regulation of cell population proliferation  IDA 1357971 RGD 
phospholipase C-activating G protein-coupled receptor signaling pathway  IDA 1357971kisspeptin-10 peptide is 100% identical in rat and mouse and humanRGD 
positive regulation of hormone secretion  IDA 1357971 RGD 
positive regulation of MAPK cascade  IDA 1357971 RGD 
positive regulation of stress fiber assembly  IDA 1357971 RGD 

Molecular Function
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
G protein-coupled peptide receptor activity  IPIKISS1 (Homo sapiens)1357971 RGD 
kisspeptin receptor binding  IPIKiss1r (Rattus norvegicus)1357971kisspeptin-10 peptide is 100% identical in rat and mouse and humanRGD 

Objects Annotated

Genes (Rattus norvegicus)
Kiss1  (KiSS-1 metastasis-suppressor)
Kiss1r  (KISS1 receptor)


Additional Information