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 molecules.

背景：促性腺激素释放激素（GnRH）是性成熟和人类机体生殖周期调控的关键因素。GnRH通过促性腺激素释放激素受体（GnRHR）的激活与垂体细胞相互作用。GnRH-GnRHR复合物的任何损伤/功能障碍都会导致各种癌症类型和疾病的发展。此外，将GnRHR鉴定为潜在的药物靶标已导致开发了在各种治疗方案中实施的激动剂和拮抗剂分子。这些药物的开发是基于从GnRH和GnRHR的功能研究获得的信息。

目的：本综述旨在阐明GnRH和GnRH受体的多功能，并提供有关各种激动剂，拮抗剂和非肽GnRH类似物的发展的综述。

结论：从这些研究中获得的信息可以增强我们对GnRH-GnRHR通用性的理解，并为设计更有效的新分子提供有价值的见解。