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Structure-activity relationship (SAR) studies of synthetic glycogen synthase kinase-3 beta inhibitors: A critical review

机译:合成糖原合成酶激酶-3β抑制剂的结构 - 活性关系(SAR)研究:临界评论

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摘要

Glycogen Synthase Kinase-3 (GSK-3) is a constitutively dynamic, omnipresent serine/threonine protein kinase regularly called as a "multitasking kinase" due to its pliable function in diverse signaling pathways. It exists in two isoforms i.e., GSK-3 alpha and GSK-3 beta Inhibition of GSK-3 may be useful in curing various diseases such as Alzheimer's disease, type II diabetes, mood disorders, cancers, chronic inflammatory agents, stroke, bipolar disorders and so on, but the approach poses significant challenges. Lithium was the first GSK-3 beta inhibitor to be used for therapeutic outcome and has been effectively used for many years. In recent years, a large number of structurally diverse potent GSK-3 beta inhibitors are reported. The present review focuses on the recent developments in the area of medicinal chemistry to explore the diverse chemical structures of potent GSK-3 beta inhibitors and also describes its structure-activity relationships (SAR) and molecular binding interactions of favorable applicability in various diseases. (C) 2018 Elsevier Masson SAS. All rights reserved.
机译:糖原合成酶激酶-3(GSK-3)是由于其在不同信号通路中的柔韧函数中,具有规则地称为“多任务激酶”的组成型动力,无所不连的丝氨酸/苏氨酸蛋白激酶。它存在于两种同种型中,即GSK-3的GSK-3α和GSK-3β抑制可用于治愈各种疾病,如阿尔茨海默病,II型糖尿病,情绪障碍,癌症,慢性炎症剂,中风,双相紊乱等等,但这种方法造成了重大挑战。锂是第一个用于治疗结果的GSK-3β抑制剂,并有效地使用多年。近年来,报告了大量结构性多样化的GSK-3β抑制剂。本综述重点介绍了药用化学领域的最新发展,探讨了有效的GSK-3β抑制剂的多样化化学结构,并描述了其结构 - 活性关系(SAR)和各种疾病中有利适用性的分子结合相互作用。 (c)2018年Elsevier Masson SAS。版权所有。

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  • 作者单位

    Wuhan Inst Technol Sch Mat Sci &

    Engn Engn Res Ctr Environm Mat &

    Membrane Technol Hube Wuhan;

    Wuhan Inst Technol Sch Mat Sci &

    Engn Engn Res Ctr Environm Mat &

    Membrane Technol Hube Wuhan;

    Wuhan Inst Technol Sch Mat Sci &

    Engn Engn Res Ctr Environm Mat &

    Membrane Technol Hube Wuhan;

    Wuhan Inst Technol Sch Mat Sci &

    Engn Engn Res Ctr Environm Mat &

    Membrane Technol Hube Wuhan;

    Wuhan Inst Technol Sch Mat Sci &

    Engn Engn Res Ctr Environm Mat &

    Membrane Technol Hube Wuhan;

    Wuhan Inst Technol Sch Mat Sci &

    Engn Engn Res Ctr Environm Mat &

    Membrane Technol Hube Wuhan;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

    GSK-3 beta; Synthetic analogs; SAR; Molecular docking;

    机译:GSK-3 beta;合成类似物;SAR;分子对接;

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