促性腺激素释放激素(GnRHs)是调节动物繁殖的关键激素,在哺乳动物中主要以2种形式存在。GnRH Ⅰ调节促性腺激素,GnRH Ⅱ则具有神经调节和促进性行为作用。GnRHs可通过自/旁分泌在生殖组织和肿瘤中发挥作用。但GnRH Ⅰ和GnRH Ⅱ似乎仍有信号的差异,通过I型受体而产生不同的下游效应。配体受体的相互作用和受体构象变化参与受体激活原理已被部分确定。这些研究结果为选择新的促性腺激素释放激素类似物提供潜在的更广泛和更具体的应用前景。另外,通过合成新的促性腺激素释放激素类似物,可在生产中发挥更广泛和更具体的应用。
GnRHs is the pivotal hormone regulating animal reproduction.In mammals,there are two forms of hormone including GnRHⅠ which regulates gonadotropin and GnRHⅡ which appears to be a neuromodulator and stimulates sexual behavior.GnRHs also occurs in reproductive tissues and tumours in which a paracrine/autocrine role is postulated.However,GnRHⅠ and GnRHⅡ still appear to have distinct roles in signalling differentially through the type Ⅰ receptor (ligand-selective-signalling) to have different own stream effects.The ligand-receptor interactions and receptor conformational changes involved in receptor activation have been partly delineated.Together,these findings are setting the scene for generating novel selective GnRH analogues with potential for wider and more specific application.The research progress of GnRH and its receptor Ⅰ in the mammal has been reviewed in this paper.