Medina Miguel, Castro Ana
Neuropharma SA, Avenida de la Industria 52, 28760 Tres Cantos, Madrid, Spain.
Curr Opin Drug Discov Devel. 2008 Jul;11(4):533-43.
It is just over a quarter of a century since the original identification and characterization of glycogen synthase kinase-3 (GSK-3), a major protein kinase that is involved in the regulation of glucose metabolism. GSK-3 modulates the function of a diverse series of proteins, as well as being associated with a wide variety of human disorders, including neurodegenerative diseases, stroke, bipolar disorder, diabetes and cancer. Not surprisingly, GSK-3 has attracted significant attention as a therapeutic target and as a means to understand the molecular basis of these disorders. Small-molecule GSK-3 inhibitors have now started to reach clinical development for the treatment of various disorders.
糖原合酶激酶-3(GSK-3)最初被鉴定和表征距今不过二十五年多一点,它是一种主要的蛋白激酶,参与葡萄糖代谢的调节。GSK-3调节一系列不同蛋白质的功能,还与多种人类疾病相关,包括神经退行性疾病、中风、双相情感障碍、糖尿病和癌症。不出所料,GSK-3作为治疗靶点以及理解这些疾病分子基础的一种手段,已引起了极大关注。小分子GSK-3抑制剂现已开始进入治疗各种疾病的临床开发阶段。