Inhibition of Glycogen Synthase Kinase-3

  • Andrei V. Ougolkov
  • Daniel D. Billadeau
Part of the Methods in Molecular Biology™ book series (MIMB, volume 468)


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.

Key words

Glycogen synthase kinase-3 β-catenin glycogen synthase 



This work was supported in part by the Mayo Foundation, and a Specialized Program of Research Excellence (SPORE) grant in pancreatic cancer (P50 CA102701) to DDB.


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Copyright information

© Humana Press, a part of Springer Science+Business Media, LLC 2008

Authors and Affiliations

  • Andrei V. Ougolkov
    • 1
  • Daniel D. Billadeau
    • 1
  1. 1.Division of Oncology ResearchMayo Clinic College of MedicineRochester MNUSA

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