Abstract: Glycogen synthase kinase-3 (GSK-3) is a serine / threonine kinase, originally identified as a protein kinase by its ability to phosphorylate and inactivate glycogen synthase. It was found that the overexpression of GSK-3 is associated with some diseases, such as diabetes, Alzheimer disease and other neurodegenerative diseases. Some pharmacological inhibitors of GSK-3 have been demonstrated to mimic insulin signaling, adjust glycogen synthesis and glucose metabolism, and improve insulin resistance. So GSK-3 inhibitors are realized as a new approach of treating diabetes. This review summarizes current advances in research of GSK-3 inhibitors as a new therapeutic approach for diabetes.