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Can PPAR gamma ligands be used in cancer therapy?

M A K Rumi1, S Ishihara, H Kazumori

  • 1Department of Gastroenterology and Hepatology, Shimane University School of Medicine, Izumo, Shimane 693-0021, Japan.

Current Medicinal Chemistry. Anti-Cancer Agents
|December 8, 2004
PubMed

Insights

Peroxisome-proliferator activated receptor (PPAR)gamma ligands show debated anti-tumor effects. Recent studies question their efficacy and role in cancer therapy, highlighting conflicting evidence on tumor suppression versus promotion.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Peroxisome-proliferator activated receptor (PPAR)gamma ligands have demonstrated anti-tumorigenic properties in vitro and in animal models.
  • Evidence suggests PPARgamma ligands possess anti-proliferative, pro-differentiation, and anti-angiogenic effects, potentially inhibiting cancer growth.
  • PPARgamma ligands have also shown preventive effects against chemical carcinogenesis in animal studies.

Purpose of the Study:

  • To review and address the controversies surrounding the role of PPARgamma ligands in cancer therapy.
  • To evaluate the conflicting evidence regarding PPARgamma's function as a tumor suppressor or promoter.
  • To discuss the clinical efficacy of PPARgamma ligands in various cancer types.

Main Methods:

  • Literature review of in vitro, xenograft, and animal model studies on PPARgamma ligands and cancer.
  • Analysis of clinical trial data investigating PPARgamma ligands for cancer treatment.
  • Examination of genetic studies involving PPARgamma mutations and cancer susceptibility.

Main Results:

  • PPARgamma ligands exhibit anti-tumorigenic effects, but their growth inhibitory actions are sometimes independent of PPARgamma activation.
  • Conflicting results exist, with some studies indicating growth-promoting effects of PPARgamma activation, particularly in genetically predisposed models.
  • While initial trials showed promise in liposarcoma and prostate cancer, later studies reported limited therapeutic value in advanced colorectal and breast cancers.

Conclusions:

  • The role of PPARgamma in cancer remains debated, with evidence supporting both tumor-suppressive and tumor-promoting functions.
  • PPARgamma ligands may not be universally effective cancer therapeutics, and their clinical utility requires further investigation.
  • Recent findings challenge the notion of PPARgamma as a straightforward tumor suppressor gene, necessitating a nuanced approach to its therapeutic targeting.

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