聚乙二醇化生长激素释放激素的研究进展

The research of development on Pegylation of growth hormone-releasing hormone

生长激素释放激素(growth hormone-releasing hormone,GHRH)又称生长激素释放因子(growth hormone-releasing factor,GRF),是由下丘脑分泌的一种肽类激素,具有促进垂体促生长素细胞合成和释放生长激素(growth hormone,GH)的作用,临床上可以用来治疗矮小症、HIV相关的脂肪营养不良、代谢综合征、艾滋病、创伤等疾病。然而GHRH应用到临床上的最大不足就是体内半衰期比较短(一般10～20min)。为了延长GHRH在体内的半衰期,减少频繁用药给患者带来的不适,须对GHRH进行修饰,以期达到半衰期显著延长,免疫原性有所降低。为此,本文主要综述了GHRH以及GHRH长效修饰的研究进展,尤其是PEG修饰GHRH的最新进展。

Growth hormone releasing hormone （GHRH） also known as growth hormone releasing factor （GRF）, a peptide hormone, is secreted by the hypothalamus and has the function of promoting the synthesis and release of growth hormone. Although it can be used to treat short stature, HIV-associated lipodystrophy, syndrome X, AIDS, trauma and other diseases in clinic, however, the biggest shortcoming of GHRH is the short half life in vivo （usually 10-20 minutes）. In order to extend the half life of GHRH in vivo, reduce the dosing frequency which bring some discomfort to the patients, some measures should be taken to modify the GHRH. This paper mainly reviews the research development of GHRH, polyethylene glycol as well as the modification of GHRH, especially the pegylation of GHRH.