PPARgamma agonists attenuate proliferation and modulate Wnt/beta-catenin signalling in melanoma cells

Int J Biochem Cell Biol. 2009 Apr;41(4):844-52. doi: 10.1016/j.biocel.2008.08.037. Epub 2008 Sep 6.

Abstract

Peroxisome proliferator-activated receptor-gamma (PPARgamma) is a member of the nuclear hormone receptor (NHR) superfamily of ligand-activated transcriptional regulators. Accumulating evidence suggests that PPARgamma agonists such as the thiazolidinediones (TZDs) may prove to be useful anti-cancer agents exhibiting anti-proliferative and/or pro-apoptotic affects in a range of cancer cell types including melanoma, however, the mechanisms underlying this effect remain unclear. We have demonstrated the anti-proliferative effects of full and partial PPARgamma modulators in human melanoma cell lines. Ablation of PPARgamma expression in the MM96L melanoma cell line by siRNA mediated mechanisms attenuates the anti-proliferative effect of these agents suggesting this effect is directly mediated by PPARgamma. The mechanisms underlying the anti-proliferative effects of PPARgamma in melanoma cells involve the regulation of expression of a number of critical cell cycle genes and beta-catenin. Moreover, our data indicate that PPARgamma modulates Wnt/beta-catenin mediated signalling in melanoma cells in an agonist dependent manner.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • COS Cells
  • Cell Cycle / drug effects
  • Cell Cycle / genetics
  • Cell Growth Processes / drug effects
  • Cell Growth Processes / physiology
  • Cell Line, Tumor
  • Chlorocebus aethiops
  • Chromans / pharmacology
  • Halofenate / pharmacology
  • Humans
  • Melanoma / drug therapy*
  • Melanoma / genetics
  • Melanoma / metabolism
  • Melanoma / pathology
  • PPAR gamma / agonists*
  • PPAR gamma / biosynthesis
  • PPAR gamma / genetics
  • RNA, Messenger / biosynthesis
  • RNA, Messenger / genetics
  • RNA, Small Interfering / genetics
  • Rosiglitazone
  • Signal Transduction / drug effects
  • Thiazolidinediones / pharmacology
  • Troglitazone
  • Wnt Proteins / agonists*
  • Wnt Proteins / genetics
  • Wnt Proteins / metabolism*
  • beta Catenin / genetics
  • beta Catenin / metabolism*

Substances

  • Antineoplastic Agents
  • Chromans
  • PPAR gamma
  • RNA, Messenger
  • RNA, Small Interfering
  • Thiazolidinediones
  • Wnt Proteins
  • beta Catenin
  • Rosiglitazone
  • Troglitazone
  • Halofenate