1. GSK-3 Inhibitors: A New Class of Drugs for Alzheimer’s Disease Treatment
- Author
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In-ho Song, Dilipkumar Pal, Souvik Mukherjee, and Satish Balasaheb Nimse
- Subjects
Pharmacology ,Drug ,business.industry ,Drug discovery ,media_common.quotation_subject ,Clinical Biochemistry ,tau Proteins ,macromolecular substances ,Disease ,Type 2 diabetes ,medicine.disease ,Bioinformatics ,Glycogen Synthase Kinase 3 ,Alzheimer Disease ,GSK-3 ,Drug Discovery ,Humans ,Molecular Medicine ,Medicine ,Dementia ,Bipolar disorder ,Phosphorylation ,business ,Stroke ,media_common - Abstract
Alzheimer’s disease (AD), a chronic neurodegenerative disease, is the most common form of dementia that causes cognitive function impairment, including memory, thinking, and behavioral changes that ultimately lead to death. The overactivation of GSK-3, an enzyme from the proline/serine Ki NS family, has been associated with hyper-phosphorylation of tau proteins. The self- -assembly of hyper-phosphorylated tau proteins to form tangles of straight and helical filaments is known to be involved in AD. Therefore, GSK-3 has been considered a potential target of novel drug discovery for AD treatment. Research on the development of GSK-3 inhibitors has received enormous attention from the vast scientific community because they are targeted for AD and other diseases, including type 2 diabetes, cancers, stroke, Parkinson’s disease and bipolar disorder. Various drugs of both synthetic and natural origins have been designed to inhibit GSK-3 activity. However, there is a need to develop novel drug candidates that can selectively inhibit GSK-3. Hence, this review summarizes the potential of GSK-3 inhibitors for AD therapy and discusses the structure- activity relationship of current drug molecules and the potential problems associated with them.
- Published
- 2021
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