糖尿病治疗新靶点糖原合成酶激酶-3抑制剂的研究进展  

A new target for diabetes therapy:advances in the research of glycogen synthase kinase-3 inhibitors

作　　者：刘率男[1] 申竹芳[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所,北京100050

出　　处：《药学学报》2007年第12期1227-1231,共5页Acta Pharmaceutica Sinica

摘　　要：糖原合成酶激酶-3(glycogen synthase kinase-3,GSK-3)属丝氨酸/苏氨酸类激酶,最早是作为一种能磷酸化并抑制糖原合成酶活性的蛋白激酶而被发现的。已发现在某些人类疾病中GSK-3的活性异常升高,如糖尿病、阿尔茨海默病及其他一些神经退行性疾病。现已找到了一些小分子GSK-3抑制剂主要是通过使GSK-3的丝氨酸位点磷酸化,从而抑制其活性。GSK-3活性被抑制后,能影响胰岛素信号传导、葡萄糖代谢及糖原的合成。因此开发GSK-3抑制剂已成为研究抗糖尿病药物的一个新思路。本文主要介绍GSK-3与糖尿病的联系及近年来GSK-3抑制剂在抗糖尿病作用方面的研究进展。Glycogen synthase kinase-3（GSK-3） is a serine / threonine kinase,originally identified as a protein kinase by its ability to phosphorylate and inactivate glycogen synthase.It was found that the overexpression of GSK-3 is associated with some diseases,such as diabetes,Alzheimer disease and other neurodegenerative diseases.Some pharmacological inhibitors of GSK-3 have been demonstrated to mimic insulin signaling,adjust glycogen synthesis and glucose metabolism,and improve insulin resistance.So GSK-3 inhibitors are realized as a new approach of treating diabetes.This review summarizes current advances in research of GSK-3 inhibitors as a new therapeutic approach for diabetes.

关 键 词：糖原合成酶激酶-3 糖原合成 胰岛素信号通路 胰岛素抵抗 糖尿病 

分 类 号：R963[医药卫生—微生物与生化药学]