Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation
Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation
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DOI：
10.1002/med.10011
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发表时间：
2002-07-01
影响因子：
13.3
通讯作者：
Alonso, M
中科院分区：
文献类型：
--
作者：
Martinez, A;Castro, A;Alonso, M
糖原合成酶-3(GSK-3)最初被描述为参与糖原代谢的关键酶，但现在已知调节一系列细胞功能。这种酶有两种形式，GSK-3pha和GSK-3beta，此前已经被鉴定出来。因此，GSK-3的小分子抑制剂可能有几种治疗用途，包括治疗神经退行性疾病、II型糖尿病、双相情感障碍、中风、癌症和慢性炎症性疾病。鉴于最近有大量文献涉及GSK-3在不同疾病的分子通路中的作用，本文主要综述了为该酶发现或开发的新的GSK-3抑制剂及其化学结构、合成和构效关系，旨在为这些有前途的药物的未来优化提供一些线索。(C)2002年威利期刊公司。
Glycogen synthase kinase 3 (GSK-3) was initially described as a key enzyme involved in glycogen metabolism, but is now known to regulate a diverse array of cell functions. Two forms of the enzyme, GSK-3alpha and GSK-3beta, have been previously identified. Small molecules inhibitors of GSK-3 may, therefore, have several therapeutic uses, including the treatment of neurodegenerative diseases, diabetes type II, bipolar disorders, stroke, cancer, and chronic inflammatory disease. As there is lot of recent literature dealing with the involvement of GSK-3 in the molecular pathways of different diseases, this review is mainly focused on the new GSK-3 inhibitors discovered or specifically developed for this enzyme, their chemical structure, synthesis, and structure-activity relationships, with the aim to provide some clues for the future optimization of these promising drugs. (C) 2002 Wiley Periodicals, Inc.