GnRH Antagonist Small Molecules and Peptides

Gonadotropin-releasing hormone (GnRH) receptors are a group of G_q/11-protein-coupled receptors that are divided into two subtypes; GnRH and GnRH2. GnRH receptors are predominantly expressed by pituitary gonadotrophs and are found at lower concentrations in the ovary, breast, placenta, prostate, heart and kidneys.

GnRH regulates the biosynthesis and secretion of follicle-stimulating hormone (FSH) and luteinising hormone (LH) and the human gene encoding the GnRH receptor is localized on chromosome 4q21.2. GnRH2 is silenced in humans but in other mammals it stimulates sexual behavior and has neuromodulatory activity.