par Kotani, M.;Detheux, Michel;Vandenbogaerde, A.;Communi, David ;Vanderwinden, Jean-Marie ;Le Poul, Emmanuel;Brezillion, Stephane;Tyldesley, R.;Suarez Gonzalez, Nathalie ;Vandeput, F.;Blanpain, Cédric ;Schiffmann, Serge N. ;Vassart, Gilbert ;Parmentier, Marc
Référence The Journal of biological chemistry, 276, 37, page (34631-34638)
Publication Publié, 2001
Référence The Journal of biological chemistry, 276, 37, page (34631-34638)
Publication Publié, 2001
Article révisé par les pairs
Résumé : | 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. |