KISS-Derived Peptide Receptor Antagonists

The kisspeptin receptor (also known as the KISS1 receptor) is a G_q/G₁₁-protein-coupled receptor that signals through stimulation of phospholipase C resulting in Ca²⁺ mobilization. The kisspeptin receptor is found at high concentrations in the pancreas, placenta and brain and there are lower expression levels in the small intestine, kidney, lung, liver and heart.

The kisspeptin receptor plays a key role in the neuroendocrine control of the gonadotrophin axis and has been implicated in the inhibition of metastasis. The human KISS1 receptor gene is localized on chromosome 19p13.3.