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Updated: Feb 16, 2026

High-throughput Analysis of Mammalian Olfactory Receptors: Measurement of Receptor Activation via Luciferase Activity
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The Anticancer Potential of Peroxisome Proliferator-Activated Receptor Antagonists

Laura De Lellis1,2, Annamaria Cimini3,4,5, Serena Veschi1,2

  • 1Department of Pharmacy, University of Chieti, Via dei Vestini 31, 66100, Chieti, Italy.

Chemmedchem
|December 26, 2017
PubMed

Insights

PPAR antagonists show potential antitumor activity. This review highlights recent findings on their in vitro and in vivo effects against various tumors, supporting their use in cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Peroxisome proliferator-activated receptors (PPARs) role in cancer cell proliferation and differentiation is extensively studied.
  • Pleiotropic outcomes reported across diverse cancer models and experimental conditions.
  • Limited preclinical evidence supports the antitumor potential of PPAR antagonists.

Purpose of the Study:

  • To review recent findings on the antitumor effects of PPAR antagonists.
  • To explore in vitro and in vivo evidence for compounds inhibiting PPAR subtypes.
  • To provide a rationale for using PPAR antagonists in specific tumor treatments.

Main Methods:

  • Literature review of preclinical studies.
  • Analysis of compounds inhibiting PPAR subtypes (PPARα, PPARγ, PPARδ).
  • Examination of effects in various cancer models.

Main Results:

  • Compounds inhibiting PPARs demonstrate antitumor activity in vitro and in vivo.
  • Evidence supports efficacy across different tumor types.
  • PPAR antagonist activity is linked to tumor expression of PPAR subtypes.

Conclusions:

  • PPAR antagonists represent a promising therapeutic strategy for certain cancers.
  • Further research is warranted to translate preclinical findings into clinical applications.
  • Targeting PPARs offers a novel approach to cancer treatment.
Keywords:
PPAR antagonistsantitumor agentscytotoxicitymetabolic drugsnuclear receptors

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