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Glycogen synthase kinase-3 beta (GSK-3β) is a desired pharmacological target for cancer treatment. Despite its role in the development of various cancers, any target directing GSK-3 inhibitors have not been authorized for cancer treatment. The therapeutic importance of this enzyme is reflected in its monitoring character in autophagy, genetic material mismatch correction, tumor development, and invasion, which justifies medication combinations. GSK-3 controls various cell processes, including metabolism, signaling, and structural proteins. It modulates programmed cell death-ligand 1 (PD-L1) by phosphorylating target pro-oncogenes. New evidence on GSK-3 as a modulator of the antineoplastic immune response further highlights the potential uses of new GSK-3β selective antagonists currently being tested in humans. Indole, indazole, oxadiazole, isothiazolidinedione, and morpholine congeners are the …