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.
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Apoptosis: A Key in Neurodegenerative Disorders
Current Neurovascular Research Peptides or Small Molecules? Different Approaches to Develop More Effective CDK Inhibitors
Current Medicinal Chemistry Impact of Diabetes in Blood-Testis and Blood-Brain Barriers: Resemblances and Differences
Current Diabetes Reviews The Development of Epigenetics and Related Inhibitors for Targeted Drug Design in Cancer Therapy
Current Topics in Medicinal Chemistry Medicinal and Beneficial Health Applications of Tinospora cordifolia (Guduchi): A Miraculous Herb Countering Various Diseases/Disorders and its Immunomodulatory Effects
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) The Design and Synthesis of Novel Phenothiazine Derivatives as Potential Cytotoxic Agents
Letters in Drug Design & Discovery Lopinavir/Ritonavir Treatment Induces Oxidative Stress and Caspaseindependent Apoptosis in Human Glioblastoma U-87 MG Cell Line
Current HIV Research Recent Developments on 1,2,4-Triazole Nucleus in Anticancer Compounds: A Review
Anti-Cancer Agents in Medicinal Chemistry Sorting Mechanism of Peptide Hormones and Biogenesis Mechanism of Secretory Granules by Secretogranin III, a Cholesterol-Binding Protein, in Endocrine Cells
Current Diabetes Reviews Aging and Inflammation: Etiological Culprits of Cancer
Current Aging Science Current Drugs and Potential Future Neuroprotective Compounds for Parkinson’s Disease
Current Neuropharmacology Computational Studies on the Prion Protein
Current Topics in Medicinal Chemistry Immunomodulatory Roles of VIP and PACAP in Models of Multiple Sclerosis
Current Pharmaceutical Design Protein Arginine Methyltransferase 1 and its Dynamic Regulation Associated with Cellular Processes and Diseases
Protein & Peptide Letters AMPK as a New Attractive Therapeutic Target for Disease Prevention: The Role of Dietary Compounds AMPK and Disease Prevention
Current Drug Targets LGI1 Affects Survival of Neuroblastoma Cells by Inhibiting Signalling through Phosphoinositide 3-Kinase
Current Signal Transduction Therapy The Basic Biology of BACE1: A Key Therapeutic Target for Alzheimers Disease
Current Genomics Target Driven Preclinical Screening for New Antimitotic Chemotherapy Agents
Current Topics in Medicinal Chemistry Meloxicam Prevents Load-Induced Cardiac Hypertrophy in Mice
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Molecular Mechanisms Mediating Nociceptin/Orphanin FQ Receptor Signaling, Desensitization and Internalization
Current Molecular Pharmacology