Structure–activity relationship of GnRH ligands

Gonadotrophin-releasing hormone (GnRH) and its analogues are clinically valuable for the treatment of a variety of reproductive disorders including infertility, precocious puberty, uterine fibroids, endometriosis and polycystic ovarian disease, and have therapeutic value in the treatment of cancers of the prostate, breast, pancreas, ovary and pituitary (Conn and Crowley, 1991). Understanding of the structure of the GnRH receptor will lay the foundation for the design of a new generation of GnRH analogues, for the regulation of reproductive function and treatment of reproductive disorders. Recent cloning of the GnRH receptor makes it possible to examine how GnRH recognizes and activates its receptor at a molecular level, and allows us to re-examine established but previously untested hypotheses.