Kaidanovich Oksana, Eldar-Finkelman Hagit
Department of Human Genetics and Molecular Medicine, Sackler School of Medicine, Tel-Aviv University, Israel.
Expert Opin Ther Targets. 2002 Oct;6(5):555-61. doi: 10.1517/14728222.6.5.555.
Glycogen synthase kinase-3 (GSK-3) is a ubiquitous cytosolic serine/threonine protein kinase that has been implicated in multiple receptor-mediated intracellular processes. Its unique feature, which distinguishes it from other protein kinases, is that it is constitutively active in resting conditions and acts as a suppressor of signalling pathways. The fact that the function of two key targets of insulin action, glycogen synthase and insulin receptor substrate-1, are suppressed by GSK-3, as well as the fact that GSK-3 activity is higher in diabetic tissues, makes it a promising drug discovery target for insulin resistance and Type 2 diabetes. Thus, the development of GSK-3 inhibitors has received attention as an attempt to control both the spread of the disease and its severity.
糖原合酶激酶-3（GSK-3）是一种普遍存在的胞质丝氨酸/苏氨酸蛋白激酶，参与多种受体介导的细胞内过程。它与其他蛋白激酶不同的独特特征是，在静息状态下具有组成性活性，并作为信号通路的抑制因子发挥作用。GSK-3抑制胰岛素作用的两个关键靶点糖原合酶和胰岛素受体底物-1的功能，以及在糖尿病组织中GSK-3活性更高这一事实，使其成为胰岛素抵抗和2型糖尿病有前景的药物研发靶点。因此，开发GSK-3抑制剂作为控制疾病传播及其严重程度的一种尝试已受到关注。
