GSK-3 promotes cell survival, growth, and PAX3 levels in human melanoma cells

Mol Cancer Res. 2012 Aug;10(8):1065-76. doi: 10.1158/1541-7786.MCR-11-0387. Epub 2012 Jun 7.

Abstract

GSK-3 is a serine/threonine kinase involved in a diverse range of cellular processes. GSK-3 exists in two isoforms, GSK-3α and GSK-3β, which possess some functional redundancy but also play distinct roles depending on developmental and cellular context. In this article, we found that GSK-3 actively promoted cell growth and survival in melanoma cells, and blocking this activity with small-molecule inhibitor SB216763 or gene-specific siRNA decreased proliferation, increased apoptosis, and altered cellular morphology. These alterations coincided with loss of PAX3, a transcription factor implicated in proliferation, survival, and migration of developing melanoblasts. We further found that PAX3 directly interacted with and was phosphorylated in vitro on a number of residues by GSK-3β. In melanoma cells, direct inhibition of PAX3 lead to cellular changes that paralleled the response to GSK-3 inhibition. Maintenance of PAX3 expression protected melanoma cells from the anti-tumor effects of SB216763. These data support a model wherein GSK-3 regulates proliferation and morphology of melanoma through phosphorylation and increased levels of PAX3.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Glycogen Synthase Kinase 3* / antagonists & inhibitors
  • Glycogen Synthase Kinase 3* / genetics
  • Glycogen Synthase Kinase 3* / metabolism
  • Humans
  • Indoles / pharmacology
  • Maleimides / pharmacology
  • Melanoma* / genetics
  • Melanoma* / metabolism
  • PAX3 Transcription Factor
  • Paired Box Transcription Factors* / genetics
  • Paired Box Transcription Factors* / metabolism
  • RNA Interference
  • Signal Transduction

Substances

  • Indoles
  • Maleimides
  • PAX3 Transcription Factor
  • PAX3 protein, human
  • Paired Box Transcription Factors
  • SB 216763
  • Glycogen Synthase Kinase 3