Glycogen synthase kinase-3 (GSK3), originally discovered as a serine/threonine protein kinase that phosphorylates and inactivates glycogen synthase, is now known to regulate a diverse array of cellular processes. Inappropriate regulation of GSK3 signaling is thought to play a role in the development of type II diabetes mellitus, neuronal cell loss in Alzheimer’s disease and cancer. The two major isoforms of GSK3 in mammalian tissues (GSK3α and 3β) are structurally similar but not functionally equivalent. GSK3β activity is relatively high in resting cells, and it can be positively or negatively regulated by various stimuli. GSK3β is a promising drug target and high-throughput study methods are in demand.


