摘要
在印度乃至全球,糖尿病都是一种高风险疾病,仅次于心血管疾病。据世界卫生组织预测,到2030年,糖尿病患病风险将增加5.11亿人。在寻找II型糖尿病新靶点的过程中,已经阐明了许多靶点,如糖原合成酶激酶3 (GSK-3)、二肽基肽酶(DPP-IV)、PPAR-γ、α-葡萄糖苷酶、α-淀粉酶、GLP-1和SGLT。在这些靶点中,GSK-3被报道是治疗糖尿病的有效靶点。在糖原代谢中,GSK是糖原生物合成的调节酶(glycogenesis)。它催化合成具有1,4-α-糖苷键的线性不支链分子。GSK-3家族有两种同工酶α和β,它们的Nand C端序列不同,是半保守的多功能丝氨酸/苏氨酸激酶酶。在本章中,我们讨论一般糖尿病机制的概述,以及GSK-3调节如何影响这些过程。GSK-3复合体的突变会导致糖尿病。合成和天然支架可调节GSK-3抗糖尿病,并优化GSK-3抑制剂的开发。这篇综述主要集中在GSK-3抑制剂的发展,并强调了当前和潜在的未来治疗方法,支持以新的抗糖尿病药物靶向葡萄糖代谢的概念。
关键词: 糖尿病,Target
图形摘要
Current Drug Targets
Title:GSK-3 Inhibitors as New Leads to Treat Type-II Diabetes
Volume: 22 Issue: 13
关键词: 糖尿病,Target
摘要: In India as well as globally, diabetes is in a state of high risk and next to cardiovascular disease. As per the WHO, the risk of diabetes is expected to rise about 511 million by 2030. In quest of novel targets for type-2 diabetes, many targets were elucidated, such as Glycogen Synthase Kinase-3 (GSK-3), Dipeptidyl Peptidase (DPP-IV), PPAR-γ, α-Glucosidase, α-Amylase, GLP-1, and SGLT. Among the targets, GSK-3 was reported to be an effective target for the treatment of diabetes. In the metabolism of glycogen, GSK is a regulatory enzyme for the biosynthesis of glycogen (glycogenesis). It catalyzes the synthesis of a linear unbranched molecule with 1,4-α-glycosidic linkages. GSK-3 family has two isoenzymes, namely α and β, which differ in their Nand C- terminal sequences and are semi-conservative multifunctional serine/threonine kinase enzymes. In this chapter, we discuss an overview of general diabetic mechanisms and how GSK-3 modulation may influence these processes. Mutation in the GSK-3 complex causes diabetes. Synthetic and natural scaffolds modulate GSK-3 against diabetes and leading to its optimization for the development of GSK-3 inhibitors. This review mainly focuses on the development of GSK-3 inhibitors and highlights current and potential future therapeutic approaches that support the notion of targeting glucose metabolism with novel antidiabetic agents.
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Cite this article as:
GSK-3 Inhibitors as New Leads to Treat Type-II Diabetes, Current Drug Targets 2021; 22 (13) . https://dx.doi.org/10.2174/1389450122666210120144428
DOI https://dx.doi.org/10.2174/1389450122666210120144428 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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