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Abstract
Background: Glycogen synthase kinase 3 beta (GSK3β) is a multifunctional serine/threonine kinase, which plays a major role in various signaling pathways. More than two decades after its discovery, various pharmaceutical companies are focusing on this protein as a target of interest for various therapeutic conditions. Objective: To discuss the major developments in the area of GSK3β as a therapeutic target globally and its role in disease physiology and give an overview of the classes of compounds designed for its inhibition. Results: Data generated by various workers has helped the pharmaceutical players to put GSK3β in their portfolio. Since it is involved in various pathways of disease physiologies, understanding of the full spectrum of the role of GSK3β in relation to its structure and function is necessary to put successful modulators into clinical use.