kisspeptin 234 is a kisspeptin receptor antagonist, with the ability to antagonize kisspeptin-10-induced activation of gpr-54. kisspeptin binds to its cognate receptor (i.e. gpr-54) on neurons that produce gonadotropin-releasing hormone (gnrh), and stimulates their activity, which in turn sends an obligatory signal for gnrh secretion, thereby gating down-stream events supporting reproduction. the development of kisspeptin receptor antagonists may provide a valuable tool for exploring the physiological and pathophysiological roles of kisspeptin in the regulation of reproduction, and could serve as a potential therapeutic agent for treating hormone-dependent disorders of reproduction, such as precocious puberty, endometriosis, as well as metastatic prostate cancer.1. roseweir ak, kauffman as, smith jt, et al. discovery of potent kisspeptin antagonists delineate physiological mechanisms of gonadotropin regulation. journal of neuroscience, 2009, 29(12): 3920-3929.
