Background: Gonadotropin-Releasing Hormone (GnRH) is a key element in sexual
maturation and regulation of the reproductive cycle in the human organism. GnRH interacts with
the pituitary cells through the activation of the Gonadotropin Releasing Hormone Receptors
(GnRHR). Any impairments/dysfunctions of the GnRH-GnRHR complex lead to the development
of various cancer types and disorders. Furthermore, the identification of GnRHR as a potential
drug target has led to the development of agonist and antagonist molecules implemented in various
treatment protocols. The development of these drugs was based on the information derived from
the functional studies of GnRH and GnRHR.
Objective: This review aims at shedding light on the versatile function of GnRH and GnRH receptor
and offers an apprehensive summary regarding the development of different agonists, antagonists
and non-peptide GnRH analogues.
Conclusion: The information derived from these studies can enhance our understanding of the
GnRH-GnRHR versatile nature and offer valuable insight into the design of new more potent