Role of GSK-3 in the Regulation of Insulin Release and Glucose Metabolism

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Protein kinase (PK) has always been an attractive target for the discovery of new drugs. However, this year is significant for PK therapeutics since it marks the 20th anniversary of the FDA’s approval of the first PK drug, imatinib, which was approved in 2001 as the first protein kinase drug. GSK-3 is a serin protease protein kinase that plays a key role in glucose homeostasis in our body. It also regulates insulin resistance and the expression of glucose transporter. In type 2 diabetes mellitus (T2DM), glucose homeostasis in our body becomes jeopardized due to poor glucose utilization by the liver, muscle, and adipose tissue. GSK-3 is generally overexpressed among obese diabetics; therefore, the GSK-3 inhibitor might be a better therapeutic target for the discovery of new antidiabetic treatment. The lithium salt was experimented with as a GSK-3 inhibitor using different animal models to evaluate its antidiabetic activity and prove its action on glucose regulation inside cells. However, owing to the significant toxicity of lithium salt in the development of colorectal cancer, the WNT signalling pathway is inhibited. Currently, the major pharmaceutical companies are trying to design and synthesize some GSK-3 inhibitors that are safe and effective for diabetics. Some of these molecules are in the initial stages of the clinical trial to assess their effectiveness. In this chapter, the role of GSK3 in the regulation of insulin release and glucose metabolism was explained with a number of schematic representations in order to facilitate biomedical scientists in the drug discovery process.