Targeting GSK-3: A promising approach for cancer therapy?

Andrei V. Ougolkov, Daniel D. Billadeau

Research output: Contribution to journalReview articlepeer-review

98 Scopus citations


Glycogen synthase kinase (GSK)-3 has emerged as one of the most attractive therapeutic targets for the treatment of multiple neurological diseases, including Alzheimer's, stroke and bipolar disorders, as well as noninsulin-dependent diabetes mellitus and inflammation. Although the prominent role of GSK-3 in the adenomatous polyposis coli (APC)-β-catenin destruction complex implies that inhibition of GSK-3 could possibly lead to tumor promotion through the activation of β-catenin, several recent studies have shed new light on the activity of GSK-3 in cancer and provide insight into the molecular mechanisms by which it regulates tumor cell proliferation and survival of multiple human malignancies. In fact, GSK-3β is a critical regulator of nuclear factor (NF)κB nuclear activity, suggesting that inhibition of GSK-3β could be effective in the treatment of a wide variety of tumors with constitutively active NFκB. Herein, the authors will discuss the current understanding of the role of GSK-3 in human cancer and its potential as a therapeutic target.

Original languageEnglish (US)
Pages (from-to)91-100
Number of pages10
JournalFuture Oncology
Issue number1
StatePublished - Feb 2006


  • Cancer
  • Glycogen synthase kinase (GSK)-3
  • Nuclear factor (NF)κB

ASJC Scopus subject areas

  • Oncology
  • Cancer Research


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