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Target intelligence / Profile preview
Kisspeptin Receptor (KISS1R)
- Target
- KISS1R
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor, Rhodopsin-type GPCR
01
Overview
The Kisspeptin receptor (KISS1R), also known as GPR54, is a G protein-coupled receptor crucial for reproductive function. It is activated by kisspeptins, peptides derived from the KISS1 gene. KISS1R plays a key role in the regulation of GnRH secretion, thereby controlling LH and FSH release from the pituitary gland. This signaling pathway is essential for puberty onset, sexual maturation, and fertility. Additionally, KISS1R signaling has been implicated in tumor suppression and other physiological processes, including metabolism and placentation.
- Other names
- GPR54KiSS1-derived peptide receptorAXOR12hOT7T175CPPB1HH8
02
Mechanism of action
Agonist binding to KISS1R activates Gq/11 proteins, leading to PLCβ activation, IP3/DAG production, increased intracellular Ca(2+), and activation of PKC and the ERK/MAPK pathway.
03
Biological functions
Reproductive axis regulationGonadotropin-releasing hormone (GnRH) secretionLuteinizing hormone (LH) secretionFollicle-stimulating hormone (FSH) secretionSignal transductionTumor suppression
04
Disease associations
InfertilityPubertal disordersCancer
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