糖原合成酶激酶-3及其抑制剂研究进展

糖原合成酶激酶-3（glycogen synthase kinase-3，GSK-3）是一种多功能的丝氨酸／苏氨酸蛋白激酶，是细胞内多种信号转导通路中的重要成分，不仅参与细胞内糖代谢过程而且还参与细胞增殖、细胞分化和细胞凋亡等多种重要生理过程。GSK-3活性受多种机制调节，其活性调节异常时可引起多种重大疾病如糖尿病、神经退行性疾病和肿瘤等。GSK-3已成为许多疾病治疗靶点，目前针对GSK-3靶点开发的抑制剂主要是ATP竞争性的小分子GSK-3抑制剂。本文对GSK-3、它与多种重要疾病发生的关系，以及目前开发的GSK-3抑制剂进行了综述。

Glycogen synthase kinase-3 and its inhibitors:a research development

Glycogen synthase kinase-3(GSK-3) is a multifunctional serine/threonine protein kinase,which plays an important role in many cell signaling pathways.GSK-3 takes part not only in glycogen metabolism,but also in cell differentiation,proliferation and apoptosis.The activity of GSK-3 is regulated by many mechanisms.The activity of GSK-3 may be linked to pathology in many diseases such as diabetes mellitus,Alzheimer's disease and tumors.Recent observation identifies GSK-3 as a potential therapeutic target in multiple human pathological processes.Many of GSK-3 inhibitors are small molecules which compete with ATP in the ATP-binding site of GSK-3.This review focuses on the functional properties of GSK-3 and its roles in human pathological process and the development of GSK-3 inhibitors.