糖原合成酶激酶-3:糖尿病的潜在靶点

IF 3.3 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Bioorganic & Medicinal Chemistry Pub Date : 2023-09-07 DOI:10.1016/j.bmc.2023.117406
Divya M. Teli, Anuradha K. Gajjar
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引用次数: 0

摘要

β细胞功能障碍引起的循环葡萄糖水平升高是ii型糖尿病的一个关键标志。糖原合成酶激酶-3 (GSK-3)被认为是一种参与糖原代谢控制的酶。因此,GSK-3抑制剂已经在体外和动物模型中探索了抗糖尿病作用。此外,通过结构和细胞生物学研究的结合,已经阐明了这种酶的调节机制。本文综述了GSK-3的结构分析以及众多研究人员在GSK-3抑制剂设计和开发方面的分子建模报告。本文围绕GSK-3的信号通路及其作为糖尿病潜在靶点的潜力,讨论了迄今为止研究人员在开发新型GSK-3抑制剂作为II型糖尿病潜在治疗药物时使用的不同分子修饰方法的进展。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Glycogen synthase kinase-3: A potential target for diabetes

Elevated circulating glucose level due to β-cell dysfunction has been a key marker of Type-II diabetes. Glycogen synthase kinase-3 (GSK-3) has been recognized as an enzyme involved in the control of glycogen metabolism. Consequently, inhibitors of GSK-3 have been explored for anti-diabetic effects in vitro and in animal models. Further, the mechanisms governing the regulation of this enzyme have been elucidated by means of a combination of structural and cellular biological investigations. This review article examines the structural analysis of GSK-3 as well as molecular modeling reports from numerous researchers in the context of the design and development of GSK-3 inhibitors. This article centers on the signaling pathway of GSK-3 relevant to its potential as a target for diabetes and discusses advancements till date on different molecular modification approaches used by researchers in the development of novel GSK-3 inhibitors as potential therapeutics for the treatment of Type II diabetes.

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来源期刊
Bioorganic & Medicinal Chemistry
Bioorganic & Medicinal Chemistry 医学-生化与分子生物学
CiteScore
6.80
自引率
2.90%
发文量
413
审稿时长
17 days
期刊介绍: Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.
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