Description
Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (K
is = 1.81 and 1.45 nM for rat and human receptors, respectively). It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC
50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose. Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.
References
[1] M. KOTANI. The Metastasis Suppressor Gene KiSS-1 Encodes Kisspeptins, the Natural Ligands of the Orphan G Protein-coupled Receptor GPR54*[J]. The Journal of Biological Chemistry, 2001, 1 1: 34631-34636. DOI:
10.1074/jbc.m104847200[2] J. VIKMAN B. A. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets[J]. Diabetes, Obesity & Metabolism, 2009, 11 s4: 197-201. DOI:
10.1111/j.1463-1326.2009.01116.x[3] M L GOTTSCH. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse.[J]. Endocrinology, 2004, 145 9: 4073-4077. DOI:
10.1210/en.2004-0431
