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Glycogen Synthase Kinase 3 (GSK3): Its Role and Inhibitors.
Current Topics in Medicinal Chemistry ( IF 3.4 ) Pub Date : 2020-06-30 , DOI: 10.2174/1568026620666200516153136
Pankaj Wadhwa 1 , Priti Jain 1 , Hemant R Jadhav 1
Affiliation  

Glycogen Synthase Kinase 3 (GSK3) is one of the Serine/Threonine protein kinases, which has gained a lot of attention for its role in a variety of pathways. It has two isoforms, GSK3α and GSK3β. However, GSK3β is highly expressed in different areas of the brain and has been implicated in Alzheimer’s disease as it is involved in tau phosphorylation. Due to its high specificity concerning substrate recognition, GSK3 has been considered as an important target. In the last decade, several GSK3 inhibitors have been reported and two molecules are in clinical trials. This review collates the information published in the last decade about the role of GSK3 in Alzheimer’s disease and progress in the development of its inhibitors. Using this collated information, medicinal chemists can strategize and design novel GSK3 inhibitors that could be useful in the treatment of Alzheimer’s disease.



中文翻译:

糖原合酶激酶3(GSK3):其作用和抑制剂。

糖原合酶激酶3(GSK3)是丝氨酸/苏氨酸蛋白激酶之一,由于其在多种途径中的作用而受到广泛关注。它具有两个同工型,GSK3α和GSK3β。然而,GSK3β在大脑的不同区域高度表达,并且由于它与tau磷酸化有关而与阿尔茨海默氏病有关。由于其在底物识别方面的高度特异性,GSK3被认为是重要的靶标。在过去的十年中,已经报道了几种GSK3抑制剂,并且两种分子正在临床试验中。这篇综述收集了过去十年中发表的有关GSK3在阿尔茨海默氏病中的作用及其抑制剂的开发进展的信息。使用此整理的信息,

更新日期:2020-08-21
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