Inhibition of glycogen synthase kinase-3

There are two homologous forms of glycogen synthase kinase (GSK)-3, GSK-3α and GSK-3β, which play overlapping roles in the regulation of Wnt, Hedgehog, and insulin pathways, as well as the activation of nuclear factor (NF)-kB-mediated gene transcription. These signaling pathways regulate gene transcription, cell cycle, apoptosis, inflammation, glucose metabolism, stem-cell renewal, and differentiation. More than 50 GSK-3 inhibitors representing a wide range of chemical structures have already been identified, and their utility in the treatment of type II diabetes mellitus, Alzheimer's disease, bipolar diseases, cancer, and other human pathologies is currently being investigated. Here, we discuss two methods of GSK-3 inhibition, which can be used to determine the involvement of GSK-3 in a cellular process of interest.