Glycogen synthase kinase 3 as an anticancer drug target: novel experimental findings and trends in the design of inhibitors

Curr Pharm Des. 2013;19(4):665-79.


Glycogen synthase kinase 3 (GSK-3) is a ubiquitous serine/threonine protein kinase participating in numerous pathways. Very important among them are cancer-related pathways, such as Wnt pathway and nuclear factor κB pathway. The recent findings concerning possible applicability of GSK-3 inhibitors as anticancer agents are summarized in this review, and controversies in the data are highlighted. The most actual concepts of GSK-3 inhibitor design are also thoroughly discussed.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Drug Design
  • Enzyme Inhibitors / pharmacology
  • Glycogen Synthase Kinase 3 / antagonists & inhibitors*
  • Glycogen Synthase Kinase 3 / metabolism
  • Humans
  • Molecular Targeted Therapy
  • NF-kappa B / metabolism
  • Neoplasms / drug therapy
  • Neoplasms / enzymology
  • Wnt Signaling Pathway / physiology


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • NF-kappa B
  • Glycogen Synthase Kinase 3